Target Validation Information
Target ID T60693
Target Name Kappa-type opioid receptor
Target Type
Successful
Drug Potency against Target 1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 1712 nM [528785]
4-Phenylspiro[chromene-2,4'-piperidine] Drug Info Ki = 3400 nM [529689]
1-benzhydryl-4-hexylpiperidin-4-ol Drug Info Ki = 9221 nM [528781]
1-benzhydryl-4-o-tolylpiperidin-4-ol Drug Info Ki = 818 nM [528781]
1-benzhydryl-4-p-tolylpiperidin-4-ol Drug Info Ki = 4054 nM [528781]
1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol Drug Info Ki = 3412 nM [528781]
Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info Ki = 576 nM [528875]
1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 1028 nM [528785]
1-benzhydryl-4-cyclohexylpiperidin-4-ol Drug Info Ki = 387 nM [528781]
ZYKLOPHIN Drug Info Ki = 30.3 nM [530428]
4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol Drug Info Ki = 2687 nM [528785]
4-phenyl-1-(1-phenylpropyl)piperidin-4-ol Drug Info Ki = 1427 nM [528785]
Salvinorin B 2-methoxyethoxymethyl ether Drug Info Ki = 141 nM [529133]
LY-255582 Drug Info Ki = 28 nM [534631]
1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol Drug Info Ki = 3668 nM [528781]
4-phenyl-1-(1-phenylheptyl)piperidin-4-ol Drug Info Ki = 335 nM [528785]
1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol Drug Info Ki = 1801 nM [528781]
1-benzhydryl-4-tert-butylpiperidin-4-ol Drug Info Ki = 1073 nM [528781]
1-benzhydryl-4-isopropylpiperidin-4-ol Drug Info Ki = 7390 nM [528781]
4-phenyl-1-(1-phenylhexyl)piperidin-4-ol Drug Info Ki = 220 nM [528785]
2-THIOSALVINORIN B Drug Info Ki = 54.5 nM [528678]
2-EPI-2-THIOSALVINORIN B Drug Info Ki = 546 nM [528678]
HERKINORIN Drug Info Ki = 90 nM [529401]
Clocinnamox Drug Info Ki = 1.4 nM [529991]
14-O-phenylpropylnaltrexone Drug Info Ki = 0.41 nM [529991]
LOFENTANIL Drug Info IC50 = 0.25 nM [533543]
Salvinicin A Drug Info Ki = 390 nM [528906]
SALVINICIN B Drug Info Ki = 7020 nM [528906]
CLIOQUINOL Drug Info IC50 = 5790 nM [531262]
RTI-5989-31 Drug Info Ki = 14.5 nM [528947]
12-EPI-SALVINORIN A Drug Info Ki = 41 nM [529925]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH Drug Info Ki = 3960 nM [528875]
N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea Drug Info Ki = 280 nM [530529]
SN-11 Drug Info Ki = 0.36 nM [530073]
Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate Drug Info Ki = 10 nM [527951]
MCL-458 Drug Info Ki = 1.9 nM [528787]
MCL-448 Drug Info Ki = 0.61 nM [528787]
MCL-434 Drug Info Ki = 3.4 nM [528655]
SALVINORIN B Drug Info Ki = 280 nM [529401]
N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine Drug Info Ki = 0.34 nM [530529]
METAZOCINE Drug Info Ki = 9.9 nM [529816]
SN-23 Drug Info Ki = 4.41 nM [530073]
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide Drug Info IC50 = 20 nM [531109]
CHLOROXINE Drug Info IC50 = 4560 nM [531262]
4-phenyl-4-[1H-imidazol-2-yl]-piperidine Drug Info Ki = 126 nM [527810]
Dmt-Pro-Mmp-Phe-NH2 Drug Info Ki = 176 nM [528832]
Dmt-Pro-Emp-Phe-NH2 Drug Info Ki = 278 nM [528832]
Dmt-Pro-Phe-Phe-NH2 Drug Info Ki = 489 nM [528832]
Dmt-Pro-3,5Dmp-Phe-NH2 Drug Info Ki = 830 nM [528832]
O-DESMETHYL TRAMADOL Drug Info Ki = 450 nM [529816]
Naltrexone-6-beta-ol Drug Info Ki = 0.48 nM [529816]
Dmt-Pro-Dmt-Phe-NH2 Drug Info Ki = 998 nM [528832]
H-Cpa-Gly-Gly-Phe-Met-NH2 Drug Info Ki = 460 nM [528724]
H-Cdp-Gly-Gly-Phe-Leu-OH Drug Info Ki = 1300 nM [528724]
H-Cdp-ala-Gly-Phe-leu-OH Drug Info Ki = 2400 nM [528724]
Benzyl derivative of M6G Drug Info Ki = 15.8 nM [527461]
C[L-Phe-D-pro-L-Tyr-D-trp] Drug Info Ki = 140 nM [530160]
ENDOMORPHIN 2 Drug Info Ki = 10.6 nM [526937]
H-Tyr-Gly-Gly-Phe-Met-NH2 Drug Info Ki = 210 nM [528724]
1-benzhydryl-4-(pyridin-2-yl)piperidin-4-ol Drug Info Ki = 13180 nM [528781]
1-benzhydryl-4-butylpiperidin-4-ol Drug Info Ki = 4563 nM [528781]
1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol Drug Info Ki = 11355 nM [528781]
C[L-Tyr-D-pro-L-Phe-D-trp] Drug Info Ki = 220 nM [530160]
Salvinorin B 1-ethoxyethyl ether Drug Info Ki = 6.6 nM [529133]
H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 Drug Info Ki = 44.9 nM [528692]
Salvinorin B methoxymethyl ether Drug Info Ki = 0.6 nM [529133]
N,N-diallyl[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 64.6 nM [534450]
Salvinorin B 2,2,2-trifluoroethoxymethyl ether Drug Info Ki = 31 nM [529133]
Salvinorin B butoxymethyl ether Drug Info Ki = 5.3 nM [529133]
Salvinorin B ethoxymethyl ether Drug Info Ki = 0.32 nM [529133]
1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol Drug Info Ki = 19695 nM [528781]
Salvinorin B methylthiomethyl ether Drug Info Ki = 13 nM [529133]
Salvinorin B tetrahydropyran-2-yl ether Drug Info Ki = 4 nM [529133]
Salvinorin B 2-methoxy-2-propyl ether Drug Info Ki = 72 nM [529133]
[Dcp1]Dyn A(1-11)-NH2 Drug Info Ki = 32 nM [528376]
1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol Drug Info Ki = 1702 nM [528781]
Salvinorin B isopropoxymethyl ether Drug Info Ki = 1.6 nM [529133]
Salvinorin B propoxymethyl ether Drug Info Ki = 2.2 nM [529133]
Salvinorin B 2-fluoroethoxymethyl ether Drug Info Ki = 1.9 nM [529133]
4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol Drug Info Ki = 1095 nM [528785]
Salvinorin B benzyloxymethyl ether Drug Info Ki = 147 nM [529133]
4-phenyl-1-(1-phenylbutyl)piperidin-4-ol Drug Info Ki = 245 nM [528785]
1-benzhydryl-4-(benzyloxy)-4-phenylpiperidine Drug Info Ki = 13390 nM [528785]
1-benzhydryl-4-ethoxy-4-phenylpiperidine Drug Info Ki = 488 nM [528785]
1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol Drug Info Ki = 1738 nM [528781]
Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info Ki = 74.8 nM [528875]
17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine Drug Info Ki = 1.5 nM [530529]
1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol Drug Info Ki = 1994 nM [528781]
Dimepheptanol Drug Info Ki = 230 nM [533539]
2-Hydroxymethyl-3-hydroxymorphinan Drug Info Ki = 40 nM [530529]
4-phenyl-1-(1-phenylethyl)piperidin-4-ol Drug Info Ki = 4149 nM [528785]
1-benzhydryl-4-phenyl-4-propoxypiperidine Drug Info Ki = 1484 nM [528785]
5-(4-((phenethylamino)methyl)phenoxy)picolinamide Drug Info Ki = 69.27 nM [528996]
1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol Drug Info Ki = 288 nM [528785]
Salvinorin B tert-butoxymethyl ether Drug Info Ki = 35 nM [529133]
M3P6S Drug Info Ki = 1940 nM [551379]
M3A6S Drug Info Ki = 1165 nM [551379]
MC-CAM Drug Info Ki = 16.4 nM [530461]
Deprotected cogener of M6G Drug Info Ki = 574.9 nM [527461]
ENDOMORPHIN-1 Drug Info Ki = 52.7 nM [526937]
ELAEOCARPENINE Drug Info Ki = 12000 nM [530705]
ETONITAZENE Drug Info Ki = 0.6 nM [531519]
N-(17-Methylmorphinan-3-yl)-N'-phenylurea Drug Info Ki = 340 nM [530529]
N-isobutylnoroxymorphone Drug Info Ki = 6.12 nM [529662]
KNT-62 Drug Info Ki = 0.152 nM [530556]
MCL-183 Drug Info Ki = 0.79 nM [528787]
MCL-444 Drug Info Ki = 0.14 nM [528655]
MCL-446 Drug Info Ki = 2.3 nM [528787]
MCL-449 Drug Info Ki = 0.14 nM [528655]
MCL-435 Drug Info Ki = 0.81 nM [528655]
RTI-5989-25 Drug Info Ki = 38.9 nM [534631]
ANISOCOUMARIN H Drug Info Ki = 2600 nM [529238]
MCL-154 Drug Info Ki = 120 nM [530707]
Dmt-Pro-Imp-Phe-NH2 Drug Info Ki = 205 nM [528832]
H-Cpa-Gly-Gly-Phe-Met-OH Drug Info Ki = 1030 nM [528724]
C[L-Phe-D-pro-L-Tyr(OMe)-D-trp] Drug Info Ki = 14 nM [530160]
N-allyl[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 229 nM [534450]
N,N-dibenzyl[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 391 nM [534450]
1-benzhydryl-4-benzylpiperidin-4-ol Drug Info Ki = 1438 nM [528781]
1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol Drug Info Ki = 10298 nM [528781]
4-(4-((phenethylamino)methyl)phenoxy)benzamide Drug Info Ki = 15.04 nM [528996]
1-benzhydryl-4-(furan-2-yl)piperidin-4-ol Drug Info Ki = 9644 nM [528781]
6-(4-((benzylamino)methyl)phenoxy)nicotinamide Drug Info Ki = 2.47 nM [528996]
17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate Drug Info Ki = 5.2 nM [530529]
2-Benzylaminomethyl-3-hydroxymorphinan Drug Info Ki = 380 nM [530529]
6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide Drug Info Ki = 45.83 nM [528996]
1-benzhydryl-4-methoxy-4-phenylpiperidine Drug Info Ki = 343 nM [528785]
6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide Drug Info Ki = 136.26 nM [529132]
RTI-5989-23 Drug Info Ki = 35.8 nM [534631]
DYNORPHIN A Drug Info Ki = 0.21 nM [529478]
[Leu5]enkephalin Drug Info Ki = 4570 nM [530780]
MK-1925 Drug Info IC50 = 9800 nM [530242]
MR-1526 Drug Info IC50 = 70 nM [528070]
MCL-153 Drug Info Ki = 18 nM [530707]
M3Pr6S Drug Info Ki = 252 nM [551379]
SB-213698 Drug Info Ki = 732.45 nM [530073]
M6S Drug Info Ki = 1192 nM [551379]
NalBzOH Drug Info Ki = 0.4 nM [551379]
DAMGO Drug Info Ki = 1841 nM [551379]
MCL-433 Drug Info Ki = 3.3 nM [528655]
MCL-432 Drug Info Ki = 4.3 nM [528655]
MR-1029 Drug Info IC50 = 5.7 nM [528070]
MCL-450 Drug Info Ki = 0.28 nM [528412]
MCL-431 Drug Info Ki = 36 nM [528655]
Naltrexone-6-alpha-ol Drug Info Ki = 0.56 nM [529816]
MR-2266 Drug Info IC50 = 1.6 nM [528070]
MCL-149 Drug Info Ki = 0.18 nM [528787]
KNT-63 Drug Info Ki = 0.111 nM [530556]
TRK-820 Drug Info Ki = 0.225 nM [530556]
M3IBu6S Drug Info Ki = 4558 nM [551379]
MCL-182 Drug Info Ki = 1.8 nM [528787]
MCL-445 Drug Info Ki = 20 nM [528787]
MCL-457 Drug Info Ki = 47 nM [528787]
HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 Drug Info Ki = 0.57 nM [530428]
6-(4-((phenethylamino)methyl)phenoxy)nicotinamide Drug Info Ki = 8.38 nM [529132]
KETOCYCLAZOCINE Drug Info Ki = 1 nM [529816]
Dynorphin(1-8) Drug Info Ki = 40 nM [533377]
6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol Drug Info Ki = 150 nM [533539]
NORBINALTORPHIMINE Drug Info Ki = 0.861 nM [531086]
Dmt-Pro-Dmp-Phe-NH2 Drug Info Ki = 94.2 nM [528832]
Dmt-Pro-Tmp-Phe-NH2 Drug Info Ki = 172 nM [528832]
CCDC 710249, HCl salt Drug Info IC50 = 38 nM [530013]
C[L-Ala-D-pro-L-Phe-D-trp] Drug Info IC50 = 5 nM [530160]
C[L-Phe-D-pro-L-mTyr-D-trp] Drug Info Ki = 20 nM [530160]
C[L-Phe-D-pro-L-Phe-L-trp] Drug Info IC50 = 47 nM [530160]
C[L-Phe-D-pro-L-Phe-D-trp] Drug Info IC50 = 140 nM [530160]
C[L-mTyr-D-pro-L-Phe-D-trp] Drug Info Ki = 78 nM [530160]
C[L-Tyr(OMe)-D-pro-L-Phe-D-trp] Drug Info Ki = 66 nM [530160]
6-desoxonaltrexone Drug Info IC50 = 13 nM [530013]
1-benzhydryl-4-m-tolylpiperidin-4-ol Drug Info Ki = 1151 nM [528781]
Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info Ki = 299 nM [528376]
Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info Ki = 980 nM [528376]
1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol Drug Info Ki = 4160 nM [528781]
1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol Drug Info Ki = 2612 nM [528781]
PHENAZOCINE Drug Info Ki = 2 nM [529816]
Oxymorphone semicarbazone hydrochloride Drug Info Ki = 179 nM [533377]
N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine Drug Info Ki = 2.8 nM [530529]
H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 Drug Info Ki = 40.1 nM [528692]
4-phenyl-1-(1-phenylpentyl)piperidin-4-ol Drug Info Ki = 36 nM [528785]
Salvinorin B fluoromethyl ether Drug Info Ki = 50 nM [529133]
3-desoxy-3-carboxamidonaltrexone Drug Info Ki = 11 nM [530013]
SALVINORIN A Drug Info Ki = 17.5 nM [529331]
N-benzyl[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 93.7 nM [534450]
2-(2-methylquinolin-4-ylamino)-N-phenylacetamide Drug Info IC50 = 1.03 nM [530283]
SN-28 Drug Info Ki = 49.4 nM [531165]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide Drug Info Ki = 560 nM [530324]
3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole Drug Info Ki = 330 nM [528151]
ICI-199441 Drug Info IC50 = 2.5 nM [534134]
N,N-diCPM[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 29.1 nM [534450]
OXYMORPHINDOLE Drug Info Ki = 2170 nM [529414]
DPDPE Drug Info IC50 = 2.8 nM [526762]
2-EPI-2-THIOSALVINORIN A Drug Info Ki = 151 nM [528678]
MCL-443 Drug Info Ki = 0.3 nM [528655]
MCL-447 Drug Info Ki = 8.9 nM [528787]
DM6S Drug Info Ki = 3129 nM [551379]
SPIROINDANYLOXYMORPHONE Drug Info Ki = 588 nM [530268]
1-benzhydryl-4-phenylpiperidin-4-ol Drug Info Ki = 364 nM [530052]
6beta-naltrexol HCl Drug Info Ki = 7.42 nM [530077]
U-69593 Drug Info Ki = 0.97 nM [530889]
1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol Drug Info Ki = 759 nM [528781]
17-methyl-4'-methyldihydromorphinone Drug Info Ki = 1.5 nM [528375]
N-CPM[D-Pro-10]Dyn A-(1-11) Drug Info IC50 = 27.1 nM [534450]
Salvinorin A (ester) Drug Info Ki = 140 nM [528254]
DEOXY SALVINORIN A Drug Info Ki = 7.9 nM [528254]
FALCARINDIOL Drug Info Ki = 2515 nM [529238]
3-(1-benzylpiperidin-4-yloxy)benzamide Drug Info IC50 = 585 nM [531117]
References
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 529689J Med Chem. 2008 Oct 9;51(19):5893-6. Epub 2008 Sep 13.Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859).
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528875J Med Chem. 2007 Jun 28;50(13):3138-42. Epub 2007 Jun 1.Synthesis of stable and potent delta/mu opioid peptides: analogues of H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-OH by ring-closing metathesis.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 530428J Med Chem. 2009 Nov 12;52(21):6814-21.The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 534631J Med Chem. 1998 May 21;41(11):1980-90.Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528678Bioorg Med Chem Lett. 2007 Apr 15;17(8):2229-32. Epub 2007 Feb 2.Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.
Ref 528678Bioorg Med Chem Lett. 2007 Apr 15;17(8):2229-32. Epub 2007 Feb 2.Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.
Ref 529401J Med Chem. 2008 Apr 24;51(8):2421-31. Epub 2008 Apr 2.Herkinorin analogues with differential beta-arrestin-2 interactions.
Ref 529991J Med Chem. 2009 Mar 26;52(6):1553-7.14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
Ref 529991J Med Chem. 2009 Mar 26;52(6):1553-7.14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity.
Ref 533543J Med Chem. 1982 Aug;25(8):913-9.Potential affinity labels for the opiate receptor based on fentanyl and related compounds.
Ref 528906J Med Chem. 2007 Jul 26;50(15):3596-603. Epub 2007 Jun 20.Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.
Ref 528906J Med Chem. 2007 Jul 26;50(15):3596-603. Epub 2007 Jun 20.Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 528947J Med Chem. 2007 Aug 9;50(16):3765-76. Epub 2007 Jul 11.Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.
Ref 529925Bioorg Med Chem. 2009 Feb 1;17(3):1370-80. Epub 2008 Dec 14.Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor.
Ref 528875J Med Chem. 2007 Jun 28;50(13):3138-42. Epub 2007 Jun 1.Synthesis of stable and potent delta/mu opioid peptides: analogues of H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-OH by ring-closing metathesis.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 530073Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5. Epub 2009 Mar 26.Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
Ref 527951J Med Chem. 2006 Jan 12;49(1):256-62.Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 529401J Med Chem. 2008 Apr 24;51(8):2421-31. Epub 2008 Apr 2.Herkinorin analogues with differential beta-arrestin-2 interactions.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 529816Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Ref 530073Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5. Epub 2009 Mar 26.Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
Ref 531109Bioorg Med Chem Lett. 2010 Sep 15;20(18):5405-10. Epub 2010 Aug 3.SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 527810Bioorg Med Chem Lett. 2006 Jan 1;16(1):146-9. Epub 2005 Oct 19.4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 529816Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Ref 529816Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 527461Bioorg Med Chem Lett. 2005 Mar 15;15(6):1583-6.Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 526937J Med Chem. 2004 Jan 29;47(3):735-43.Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 528692J Med Chem. 2007 Mar 22;50(6):1414-7. Epub 2007 Feb 22.Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 534450J Med Chem. 1997 Aug 15;40(17):2733-9.Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 528376J Med Chem. 2006 Aug 24;49(17):5382-5.Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528875J Med Chem. 2007 Jun 28;50(13):3138-42. Epub 2007 Jun 1.Synthesis of stable and potent delta/mu opioid peptides: analogues of H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-OH by ring-closing metathesis.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 533539J Med Chem. 1981 Jul;24(7):903-6.Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 528996Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. Epub 2007 Aug 11.Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 551379Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13.
Ref 551379Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13.
Ref 530461J Med Chem. 2009 Nov 12;52(21):6926-30.14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists.
Ref 527461Bioorg Med Chem Lett. 2005 Mar 15;15(6):1583-6.Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide.
Ref 526937J Med Chem. 2004 Jan 29;47(3):735-43.Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
Ref 530705Bioorg Med Chem Lett. 2010 Mar 1;20(5):1601-3. Epub 2010 Jan 22.Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs.
Ref 531519J Med Chem. 1990 Sep;33(9):2456-64.Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 529662Bioorg Med Chem Lett. 2008 Sep 15;18(18):4978-81. Epub 2008 Aug 12.Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction.
Ref 530556Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4. Epub 2009 Nov 13.Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 534631J Med Chem. 1998 May 21;41(11):1980-90.Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Ref 529238Bioorg Med Chem. 2008 Mar 15;16(6):3218-23. Epub 2007 Dec 31.Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.
Ref 530707Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. Epub 2010 Jan 25.Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528724Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60. Epub 2007 Feb 2.Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 534450J Med Chem. 1997 Aug 15;40(17):2733-9.Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Ref 534450J Med Chem. 1997 Aug 15;40(17):2733-9.Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528996Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. Epub 2007 Aug 11.Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528996Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. Epub 2007 Aug 11.Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 528996Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. Epub 2007 Aug 11.Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 529132Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6. Epub 2007 Oct 17.Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Ref 534631J Med Chem. 1998 May 21;41(11):1980-90.Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Ref 529478Bioorg Med Chem Lett. 2008 Jun 15;18(12):3667-71. Epub 2007 Dec 4.Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor.
Ref 530780J Med Chem. 2010 Apr 8;53(7):2875-81."Carba"-analogues of fentanyl are opioid receptor agonists.
Ref 530242Bioorg Med Chem Lett. 2009 Aug 15;19(16):4729-32. Epub 2009 Jun 17.Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.
Ref 528070J Med Chem. 1991 Aug;34(8):2438-44.Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.
Ref 530707Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9. Epub 2010 Jan 25.Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
Ref 551379Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13.
Ref 530073Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5. Epub 2009 Mar 26.Design and synthesis of novel delta opioid receptor agonists and their pharmacologies.
Ref 551379Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13.
Ref 551379Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13.
Ref 551379Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 528070J Med Chem. 1991 Aug;34(8):2438-44.Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.
Ref 528412J Med Chem. 2006 Sep 7;49(18):5640-3.New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 529816Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Ref 528070J Med Chem. 1991 Aug;34(8):2438-44.Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 530556Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4. Epub 2009 Nov 13.Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
Ref 530556Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4. Epub 2009 Nov 13.Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
Ref 551379Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 530428J Med Chem. 2009 Nov 12;52(21):6814-21.The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues.
Ref 529132Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6. Epub 2007 Oct 17.Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Ref 529816Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Ref 533377J Med Chem. 1986 Jul;29(7):1222-5.Peptides as receptor selectivity modulators of opiate pharmacophores.
Ref 533539J Med Chem. 1981 Jul;24(7):903-6.Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists.
Ref 531086Bioorg Med Chem Lett. 2010 Sep 1;20(17):5035-8. Epub 2010 Jul 13.Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 528832J Med Chem. 2007 Jun 14;50(12):2753-66. Epub 2007 May 12.Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mixed mu-agonist/delta-antagonist and dual mu-agonist/delta-agonist opioid ligands.
Ref 530013Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94. Epub 2009 Feb 25.Syntheses of novel high affinity ligands for opioid receptors.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 530160Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50. Epub 2009 May 3.Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208.
Ref 530013Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94. Epub 2009 Feb 25.Syntheses of novel high affinity ligands for opioid receptors.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528376J Med Chem. 2006 Aug 24;49(17):5382-5.Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
Ref 528376J Med Chem. 2006 Aug 24;49(17):5382-5.Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 529816Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8. Epub 2008 Nov 7.Syntheses and opioid receptor binding properties of carboxamido-substituted opioids.
Ref 533377J Med Chem. 1986 Jul;29(7):1222-5.Peptides as receptor selectivity modulators of opiate pharmacophores.
Ref 530529J Med Chem. 2010 Jan 14;53(1):402-18.Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Ref 528692J Med Chem. 2007 Mar 22;50(6):1414-7. Epub 2007 Feb 22.Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.
Ref 528785Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.
Ref 529133Bioorg Med Chem. 2008 Feb 1;16(3):1279-86. Epub 2007 Oct 24.Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers.
Ref 530013Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94. Epub 2009 Feb 25.Syntheses of novel high affinity ligands for opioid receptors.
Ref 529331J Med Chem. 2008 Mar 27;51(6):1824-30. Epub 2008 Feb 23.Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.
Ref 534450J Med Chem. 1997 Aug 15;40(17):2733-9.Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Ref 530283Bioorg Med Chem. 2009 Aug 15;17(16):5782-90. Epub 2009 Jul 18.Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence.
Ref 531165Bioorg Med Chem Lett. 2010 Nov 1;20(21):6302-5. Epub 2010 Aug 21.Design and synthesis of KNT-127, a |A-opioid receptor agonist effective by systemic administration.
Ref 530324J Med Chem. 2009 Sep 24;52(18):5685-702.Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).
Ref 528151Bioorg Med Chem Lett. 2006 Jul 1;16(13):3524-8. Epub 2006 Apr 24.3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.
Ref 534134J Med Chem. 1996 Apr 12;39(8):1729-35.Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse microglial cells.
Ref 534450J Med Chem. 1997 Aug 15;40(17):2733-9.Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Ref 529414Eur J Med Chem. 2008 Nov;43(11):2307-15. Epub 2008 Feb 29.Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?.
Ref 526762J Med Chem. 1992 Nov 13;35(23):4325-9.Opioid agonist and antagonist activities of morphindoles related to naltrindole.
Ref 528678Bioorg Med Chem Lett. 2007 Apr 15;17(8):2229-32. Epub 2007 Feb 2.Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.
Ref 528655Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11. Epub 2007 Jan 17.High-affinity carbamate analogues of morphinan at opioid receptors.
Ref 528787Bioorg Med Chem. 2007 Jun 15;15(12):4106-12. Epub 2007 Mar 30.In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Ref 551379Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5. Epub 2006 Jun 13.
Ref 530268Bioorg Med Chem. 2009 Aug 15;17(16):5983-8. Epub 2009 Jul 3.Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normorphinan derivative.
Ref 530052Bioorg Med Chem Lett. 2009 May 1;19(9):2519-23. Epub 2009 Mar 14.The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
Ref 530077Bioorg Med Chem Lett. 2009 May 15;19(10):2811-4. Epub 2009 Mar 26.Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes.
Ref 530889J Med Chem. 2010 May 27;53(10):4212-22.Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Ref 528781Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.
Ref 528375J Med Chem. 2006 Aug 24;49(17):5333-8.Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
Ref 534450J Med Chem. 1997 Aug 15;40(17):2733-9.Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution.
Ref 528254Bioorg Med Chem Lett. 2006 Sep 1;16(17):4679-85. Epub 2006 Jun 13.Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18).
Ref 528254Bioorg Med Chem Lett. 2006 Sep 1;16(17):4679-85. Epub 2006 Jun 13.Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18).
Ref 529238Bioorg Med Chem. 2008 Mar 15;16(6):3218-23. Epub 2007 Dec 31.Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.
Ref 531117Bioorg Med Chem Lett. 2010 Oct 1;20(19):5847-52. Epub 2010 Jul 30.Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1.

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