Target Information

Target General Infomation
Target ID
T60693
Former ID
TTDS00127
Target Name
Kappa-type opioid receptor
Gene Name
OPRK1
Synonyms
KOR; KOR-1; Kappa opioid receptor; Opioid receptor Kappa; OPRK1
Target Type
Successful
Disease Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Bipolar disorder [ICD9: 296.0, 296.1, 296.4, 296.5, 296.6, 296.7, 296.8, 300; ICD10: F31, F40-F42]
Coronary artery restenosis; Multiple myeloma [ICD9:203; ICD10: I51.89, C90]
Diarrhea-predominant IBS [ICD9: 564.1; ICD10: K58.0]
Erythema [ICD9: 695; ICD10: L51-L54]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Neurodegenerative disease [ICD9: 330-337; ICD10: G30-G32]
Opiate dependence [ICD9: 304; ICD10: F11]
Obesity [ICD9: 278; ICD10: E66]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Substance dependence [ICD10: F10-F19]
Unspecified [ICD code not available]
Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain. Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic opioids.May play a role in arousal and regulation of autonomic and neuroendocrine functions.
BioChemical Class
GPCR rhodopsin
Target Validation
T60693
UniProt ID
P41145
Sequence
MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG
STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV
RNTVQDPAYLRDIDGMNKPV
Drugs and Mode of Action
Drug(s) CHLOROXINE Drug Info Approved Erythema [551871]
Dezocine Drug Info Approved Pain [536361]
Nalbuphine Drug Info Approved Pain [538227], [539027]
Rapamycin Drug Info Approved Coronary artery restenosis; Multiple myeloma [545206], [551871]
Asimadoline Drug Info Phase 3 Diarrhea-predominant IBS [536224]
Nalbuphine hydrochloride ER Drug Info Phase 3 Pain [521828]
TRK-820 Drug Info Phase 3 Discovery agent [523764]
CR-845 iv infusion Drug Info Phase 2/3 Pain [525310]
PHN-131 Drug Info Phase 2/3 Pain [548815]
Apadoline Drug Info Phase 2 Pain [527613]
Carfentanil Drug Info Phase 2 Discovery agent [524366]
CR-665 Drug Info Phase 2 Pain [529725]
Enadoline Drug Info Phase 2 Pain [525469], [539017]
MAL formulation Drug Info Phase 2 Opiate dependence [550591]
Niravoline Drug Info Phase 2 Pain [545439]
TPM-1/Morphine Drug Info Phase 2 Pain [548201]
BRL-52656 Drug Info Phase 1 Pain [534016]
LY-2456302 Drug Info Phase 1 Alcohol use disorders [524877]
MCP-201 Drug Info Phase 1 Pain [547634]
PF-4455242 Drug Info Phase 1 Bipolar disorder [522809]
GNTI Drug Info Preclinical Obesity [536122]
CLIOQUINOL Drug Info Withdrawn from market Discovery agent [522766]
ADL 10-0101 Drug Info Discontinued in Phase 2 Pain [546982]
DYNORPHIN A Drug Info Discontinued in Phase 2 Discovery agent [538995], [546012]
E-2078 Drug Info Discontinued in Phase 2 Pain [539019], [545374]
R-84760 Drug Info Discontinued in Phase 2 Pain [546014]
VP004 Drug Info Discontinued in Phase 1 Substance dependence [548458]
Fedotozine Drug Info Terminated Discovery agent [544798]
GR-89696 Drug Info Terminated Neurodegenerative disease [539020], [545442]
GR-94839 Drug Info Terminated Pain [545572]
KT-95 Drug Info Terminated Inflammatory bowel disease [546410]
LY-255582 Drug Info Terminated Discovery agent [545880]
SB-213698 Drug Info Terminated Discovery agent [546084]
Inhibitor (-)-cyclorphan Drug Info [527951]
1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol Drug Info [528785]
1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol Drug Info [528785]
1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol Drug Info [528785]
1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(benzyloxy)-4-phenylpiperidine Drug Info [528785]
1-benzhydryl-4-(furan-2-yl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(pyridin-2-yl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-benzylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-butylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-cyclohexylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-ethoxy-4-phenylpiperidine Drug Info [528785]
1-benzhydryl-4-hexylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-isopropylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-m-tolylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-methoxy-4-phenylpiperidine Drug Info [528785]
1-benzhydryl-4-o-tolylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-p-tolylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-phenyl-4-propoxypiperidine Drug Info [528785]
1-benzhydryl-4-phenylpiperidin-4-ol Drug Info [530052]
1-benzhydryl-4-tert-butylpiperidin-4-ol Drug Info [528781]
12-EPI-SALVINORIN A Drug Info [529925]
14-O-phenylpropylnaltrexone Drug Info [529991]
17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine Drug Info [530529]
17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine Drug Info [530529]
17-methyl-4'-methyldihydromorphinone Drug Info [528375]
17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate Drug Info [530529]
2-(2-methylquinolin-4-ylamino)-N-phenylacetamide Drug Info [530283]
2-Benzylaminomethyl-3-hydroxymorphinan Drug Info [530529]
2-EPI-2-THIOSALVINORIN A Drug Info [528678]
2-EPI-2-THIOSALVINORIN B Drug Info [528678]
2-Hydroxymethyl-3-hydroxymorphinan Drug Info [530529]
2-THIOSALVINORIN B Drug Info [528678]
3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole Drug Info [528151]
3-(1-benzylpiperidin-4-yloxy)benzamide Drug Info [531117]
3-desoxy-3-carboxamidonaltrexone Drug Info [530013]
4-(4-((phenethylamino)methyl)phenoxy)benzamide Drug Info [528996]
4-(p-Tolyl)spiro[chromene-2,4'-piperidine] Drug Info [529689]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide Drug Info [530324]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol Drug Info [529689]
4-phenyl-1-(1-phenylbutyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(1-phenylethyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(1-phenylheptyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(1-phenylhexyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(1-phenylpentyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(1-phenylpropyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(phenyl(o-tolyl)methyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol Drug Info [528785]
4-phenyl-4-[1H-imidazol-2-yl]-piperidine Drug Info [527810]
4-Phenylspiro[chromene-2,4'-piperidine] Drug Info [529689]
5-(4-((phenethylamino)methyl)phenoxy)picolinamide Drug Info [528996]
6-(4-((benzylamino)methyl)phenoxy)nicotinamide Drug Info [528996]
6-(4-((phenethylamino)methyl)phenoxy)nicotinamide Drug Info [529132]
6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide Drug Info [529132]
6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide Drug Info [528996]
6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol Drug Info [533539]
6-desoxonaltrexone Drug Info [530013]
6beta-naltrexol HCl Drug Info [530077]
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide Drug Info [531109]
8-carboxamidocyclazocine Drug Info [529429]
ANISOCOUMARIN H Drug Info [529238]
Benzyl derivative of M6G Drug Info [527461]
Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate Drug Info [527951]
BUTORPHAN Drug Info [525672]
CCDC 710249, HCl salt Drug Info [530013]
CHLOROXINE Drug Info [531262]
Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info [528875]
CLIOQUINOL Drug Info [531262]
Clocinnamox Drug Info [529991]
CYCLAZOCINE Drug Info [525672]
CYCLORPHAN Drug Info [525672]
C[L-Ala-D-pro-L-Phe-D-trp] Drug Info [530160]
C[L-mTyr-D-pro-L-Phe-D-trp] Drug Info [530160]
C[L-Phe-D-pro-L-mTyr-D-trp] Drug Info [530160]
C[L-Phe-D-pro-L-Phe-D-trp] Drug Info [530160]
C[L-Phe-D-pro-L-Phe-L-trp] Drug Info [530160]
C[L-Phe-D-pro-L-Tyr(OMe)-D-trp] Drug Info [530160]
C[L-Phe-D-pro-L-Tyr-D-trp] Drug Info [530160]
C[L-Tyr(OMe)-D-pro-L-Phe-D-trp] Drug Info [530160]
C[L-Tyr-D-pro-L-Phe-D-trp] Drug Info [530160]
DAMGO Drug Info [528255]
Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info [528376]
Delta-kappa opioid heterodimer Drug Info [527089]
DEOXY SALVINORIN A Drug Info [528254]
Deprotected cogener of M6G Drug Info [527461]
Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info [528376]
Dimepheptanol Drug Info [533539]
DM6S Drug Info [528255]
Dmt-Pro-3,5Dmp-Phe-NH2 Drug Info [528832]
Dmt-Pro-Dmp-Phe-NH2 Drug Info [528832]
Dmt-Pro-Dmt-Phe-NH2 Drug Info [528832]
Dmt-Pro-Emp-Phe-NH2 Drug Info [528832]
Dmt-Pro-Imp-Phe-NH2 Drug Info [528832]
Dmt-Pro-Mmp-Phe-NH2 Drug Info [528832]
Dmt-Pro-Phe-Phe-NH2 Drug Info [528832]
Dmt-Pro-Tmp-Phe-NH2 Drug Info [528832]
DPDPE Drug Info [526762]
DYNORPHIN A Drug Info [529478]
Dynorphin(1-8) Drug Info [533377]
ELAEOCARPENINE Drug Info [530705]
ENDOMORPHIN 2 Drug Info [526937]
ENDOMORPHIN-1 Drug Info [526937]
ETONITAZENE Drug Info [531519]
FALCARINDIOL Drug Info [529238]
H-Cdp-ala-Gly-Phe-leu-OH Drug Info [528724]
H-Cdp-Gly-Gly-Phe-Leu-OH Drug Info [528724]
H-Cpa-Gly-Gly-Phe-Met-NH2 Drug Info [528724]
H-Cpa-Gly-Gly-Phe-Met-OH Drug Info [528724]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH Drug Info [528875]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]NH2 Drug Info [528692]
H-Tyr-c[D-Allylgly-Gly-Phe-L-Allylgly]NH2 Drug Info [528692]
H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 Drug Info [528692]
H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 Drug Info [528692]
H-Tyr-Gly-Gly-Phe-Met-NH2 Drug Info [528724]
HERKINORIN Drug Info [529401]
HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 Drug Info [530428]
ICI-199441 Drug Info [534134]
KETOCYCLAZOCINE Drug Info [529816]
KNT-62 Drug Info [530556]
KNT-63 Drug Info [530556]
LOFENTANIL Drug Info [533543]
LY-255582 Drug Info [534631]
M3A6S Drug Info [528255]
M3IBu6S Drug Info [528255]
M3P6S Drug Info [528255]
M3Pr6S Drug Info [528255]
M6G thiosaccharide analogue Drug Info [527461]
M6S Drug Info [528255]
MC-CAM Drug Info [530461]
MCL-117 Drug Info [527951]
MCL-139 Drug Info [527951]
MCL-144 Drug Info [530279]
MCL-145 Drug Info [527951]
MCL-147 Drug Info [528787]
MCL-149 Drug Info [528787]
MCL-153 Drug Info [530707]
MCL-154 Drug Info [530707]
MCL-182 Drug Info [528787]
MCL-183 Drug Info [528787]
MCL-428 Drug Info [528655]
MCL-429 Drug Info [528655]
MCL-431 Drug Info [528655]
MCL-432 Drug Info [528655]
MCL-433 Drug Info [528655]
MCL-434 Drug Info [528655]
MCL-435 Drug Info [528655]
MCL-443 Drug Info [528655]
MCL-444 Drug Info [528655]
MCL-445 Drug Info [528787]
MCL-446 Drug Info [528787]
MCL-447 Drug Info [528787]
MCL-448 Drug Info [528787]
MCL-449 Drug Info [528655]
MCL-450 Drug Info [528412]
MCL-451 Drug Info [528412]
MCL-457 Drug Info [528787]
MCL-458 Drug Info [528787]
METAZOCINE Drug Info [529816]
MK-1925 Drug Info [530242]
Morphinan Cyclic Imine analogue Drug Info [551291]
MR-1029 Drug Info [528070]
MR-1526 Drug Info [528070]
MR-2034 Drug Info [529816]
MR-2266 Drug Info [528070]
N,N-diallyl[D-Pro-10]Dyn A-(1-11) Drug Info [534450]
N,N-dibenzyl[D-Pro-10]Dyn A-(1-11) Drug Info [534450]
N,N-diCPM[D-Pro-10]Dyn A-(1-11) Drug Info [534450]
N-(17-Methylmorphinan-3-yl)-N'-phenylurea Drug Info [530529]
N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea Drug Info [530529]
N-allyl[D-Pro-10]Dyn A-(1-11) Drug Info [534450]
N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine Drug Info [530529]
N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine Drug Info [530529]
N-benzyl[D-Pro-10]Dyn A-(1-11) Drug Info [534450]
N-CPM[D-Pro-10]Dyn A-(1-11) Drug Info [534450]
N-isobutylnoroxymorphone Drug Info [529662]
NalBzOH Drug Info [528255]
Naltrexone-6-alpha-ol Drug Info [529816]
Naltrexone-6-beta-ol Drug Info [529816]
NORBINALTORPHIMINE Drug Info [531086]
Norbinaltorphimine derivative Drug Info [527459]
O-DESMETHYL TRAMADOL Drug Info [529816]
OXYMORPHINDOLE Drug Info [529414]
Oxymorphone semicarbazone hydrochloride Drug Info [533377]
PHENAZOCINE Drug Info [529816]
RTI-5989-23 Drug Info [534631]
RTI-5989-25 Drug Info [534631]
RTI-5989-31 Drug Info [528947]
Salvinicin A Drug Info [528906]
SALVINICIN B Drug Info [528906]
SALVINORIN A Drug Info [529331]
Salvinorin A (ester) Drug Info [528254]
SALVINORIN B Drug Info [529401]
Salvinorin B 1-ethoxyethyl ether Drug Info [529133]
Salvinorin B 2,2,2-trifluoroethoxymethyl ether Drug Info [529133]
Salvinorin B 2-fluoroethoxymethyl ether Drug Info [529133]
Salvinorin B 2-methoxy-2-propyl ether Drug Info [529133]
Salvinorin B 2-methoxyethoxymethyl ether Drug Info [529133]
Salvinorin B benzyloxymethyl ether Drug Info [529133]
Salvinorin B butoxymethyl ether Drug Info [529133]
Salvinorin B ethoxymethyl ether Drug Info [529133]
Salvinorin B fluoromethyl ether Drug Info [529133]
Salvinorin B isopropoxymethyl ether Drug Info [529133]
Salvinorin B methoxymethyl ether Drug Info [529133]
Salvinorin B methylthiomethyl ether Drug Info [529133]
Salvinorin B propoxymethyl ether Drug Info [529133]
Salvinorin B tert-butoxymethyl ether Drug Info [529133]
Salvinorin B tetrahydropyran-2-yl ether Drug Info [529133]
SB-213698 Drug Info [530073]
SN-11 Drug Info [530073]
SN-23 Drug Info [530073]
SN-28 Drug Info [531165]
SPIROINDANYLOXYMORPHONE Drug Info [530268]
TPM-1/Morphine Drug Info [544320]
Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info [528875]
TRK-820 Drug Info [530556]
U-69593 Drug Info [530889]
ZYKLOPHIN Drug Info [530428]
[Dcp1]Dyn A(1-11)-NH2 Drug Info [528376]
[Leu5]enkephalin Drug Info [530780]
Agonist 3-Methylfentanyl Drug Info [551402]
3-Methylthiofentanyl Drug Info [551408]
ADL 10-0101 Drug Info [526497]
Apadoline Drug Info [527613]
Asimadoline Drug Info [536224]
BRL 52537 hydrochloride Drug Info [535870]
BRL 52974 Drug Info [534953]
BRL-52656 Drug Info [525670]
Carfentanil Drug Info [551406]
CR-665 Drug Info [530309]
CR-845 iv infusion Drug Info [544079]
Dihydromorphine Drug Info [551379]
dynorphin B Drug Info [534018]
Enadoline Drug Info [525469]
ethyketazocine Drug Info [534443]
ethylketocyclazocine Drug Info [543763]
Fedotozine Drug Info [535539]
MAL formulation Drug Info [550590]
MCP-201 Drug Info [550920]
Nalorphine Drug Info [534939]
normorphine Drug Info [543763]
NRP290 Drug Info [543763]
PHN-131 Drug Info [533353]
R-84760 Drug Info [534614]
spiradoline Drug Info [534018]
tifluadom Drug Info [534443]
U50,488H Drug Info [534904], [535113]
[3H]enadoline Drug Info [525997]
[3H]U69593 Drug Info [533399]
Antagonist 5'-guanidinonaltrindole Drug Info [525829]
Beta-endorphin Drug Info [537931]
Dezocine Drug Info [536176]
Diprenorphine Drug Info [551387]
Drug 7684380 Drug Info [537853]
GNTI Drug Info [536122]
L-685,818 Drug Info [537853]
LY-2456302 Drug Info [532492]
naltriben Drug Info [543763]
Nor-binaltorphimine dihydrochloride Drug Info [535870]
quadazocine Drug Info [543763]
Rapamycin Drug Info [538126]
[3H]diprenorphine Drug Info [533664]
[U-13C]ascomycin Drug Info [535822]
Modulator E-2078 Drug Info [525491]
GR-38414 Drug Info
GR-45809 Drug Info
GR-86014 Drug Info
GR-89696 Drug Info [526244]
GR-91272 Drug Info
GR-94839 Drug Info [526749]
ICI-204448 Drug Info
KT-95 Drug Info [543763]
Nalbuphine Drug Info [556264]
Nalbuphine hydrochloride ER Drug Info
Niravoline Drug Info
PF-4455242 Drug Info [531552]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Neuroactive ligand-receptor interaction
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Opioid prodynorphin pathway
Reactome Peptide ligand-binding receptors
G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 521828ClinicalTrials.gov (NCT00323154) Nalbuphine for the Treatment of Opioid Induced Pruritus in Children. U.S. National Institutes of Health.
Ref 522766ClinicalTrials.gov (NCT00963495) Study Evaluating the Tolerance and Biological Activity of Oral Clioquinol in Patients With Relapsed or Refractory Hematological Malignancy. U.S. National Institutes of Health.
Ref 522809ClinicalTrials.gov (NCT00988949) Proof Of Mechanism Study To Determine Efficacy Of PF-04455242 In Blocking Spiradoline (PF-00345768) Stimulated Prolactin Release. U.S. National Institutes of Health.
Ref 523764ClinicalTrials.gov (NCT01513161) Efficacy and Safety Study of TRK-820 to Treat Conventional-treatment-resistant Pruritus in Patients Receiving Hemodialysis. U.S. National Institutes of Health.
Ref 524366ClinicalTrials.gov (NCT01899170) Towards Individualized Deep Brain Stimulation Treatment of Chronic Neuropathic Pain. U.S. National Institutes of Health.
Ref 524877ClinicalTrials.gov (NCT02218775) FASTMAS (New Experimental Medicine Studies: Fast-Fail Trials in Mood and Anxiety Spectrum Disorders) Kappa Opioid Receptor (KOR) Phase 1 Study. U.S. National Institutes of Health.
Ref 525310ClinicalTrials.gov (NCT02542384) A Study Evaluating the Overall Pain Relief and Safety of Intravenous (IV) CR845 in Patients Undergoing Abdominal Surgery.
Ref 525469Enadoline, a selective kappa-opioid receptor agonist shows potent antihyperalgesic and antiallodynic actions in a rat model of surgical pain. Pain. 1999 Mar;80(1-2):383-9.
Ref 527613Novel developments with selective, non-peptidic kappa-opioid receptor agonists. Expert Opin Investig Drugs. 1997 Oct;6(10):1351-68.
Ref 529725Effect of a kappa-opioid agonist, i.v. JNJ-38488502, on sensation of colonic distensions in healthy male volunteers. Neurogastroenterol Motil. 2009 Mar;21(3):281-90.
Ref 534016Opiate receptors within the blood-brain barrier mediate kappa agonist-induced water diuresis. J Pharmacol Exp Ther. 1993 Jul;266(1):164-71.
Ref 536122Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
Ref 536224Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 538227FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070692.
Ref 538995(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1620).
Ref 539017(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1646).
Ref 539019(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1648).
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