Target Information
Target General Infomation | |||||
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Target ID |
T05849
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Former ID |
TTDS00043
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Target Name |
Gastrin/cholecystokinin type B receptor
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Gene Name |
CCKBR
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Synonyms |
CCK-B receptor; CCK-BR; CCKBR
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Target Type |
Successful
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Disease | Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42] | ||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Caerulein stimulated gastric and pancreatic secretion [ICD code not available] | |||||
Duodenal ulcers [ICD10: K25-K27] | |||||
Dyspepsia [ICD9: 536.8; ICD10: K30] | |||||
Diagnostic imaging [ICD9: 331; ICD10: G30, I73.9] | |||||
Gastroesophageal reflux disease [ICD9: 140-229, 530; ICD10: K21] | |||||
Gallstone prophylaxis; Obesity [ICD9: 278; ICD10: E66] | |||||
Gastrointestinal disease [ICD10: K00-K93] | |||||
Intestine cancer [ICD10: C17-C20, C26] | |||||
Medullary thyroid cancer [ICD9: 193; ICD10: C73] | |||||
Obesity [ICD9: 278; ICD10: E66] | |||||
Pancreatic disease [ICD10: K85-K86] | |||||
Stomach disease [ICD10: K30-K31] | |||||
Stomach ulcer [ICD10: K25-K27] | |||||
Type 1 diabetes [ICD9: 250; ICD10: E10] | |||||
Ulcerative colitis [ICD9: 556; ICD10: K51] | |||||
Unspecified [ICD code not available] | |||||
Function |
Isoform 2 is constitutively activated and may regulate cancer cell proliferation via a gastrin-independent mechanism.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T05849
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UniProt ID | |||||
Sequence |
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL
YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL PDEDPPTPSIASLSRLSYTTISTLGPG |
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Drugs and Mode of Action | |||||
Drug(s) | Ceruletide | Drug Info | Approved | Caerulein stimulated gastric and pancreatic secretion | [551871] |
Pentagastrin | Drug Info | Approved | Diagnostic imaging | [538484], [543256] | |
Ceruletide | Drug Info | Phase 3 | Cancer | [526774], [542579] | |
GASTRAZOLE | Drug Info | Phase 3 | Duodenal ulcers | [528144] | |
Dexloxiglumide | Drug Info | Phase 2 | Pancreatic disease | [551871] | |
Itriglumide | Drug Info | Phase 2 | Anxiety disorder | [543299], [546827] | |
S-0509 | Drug Info | Phase 2 | Ulcerative colitis | [521748] | |
Spiroglumide | Drug Info | Phase 2 | Stomach disease | [551837] | |
TT-223 | Drug Info | Phase 2 | Type 1 diabetes | [522421] | |
YF-476 | Drug Info | Phase 2 | Stomach ulcer | [523439], [543278] | |
Z 360 | Drug Info | Phase 2 | Unspecified | [1560000], [1560439] | |
Demogastrin | Drug Info | Phase 1 | Medullary thyroid cancer | [549943] | |
GG-8573 | Drug Info | Preclinical | Gallstone prophylaxis; Obesity | [536122] | |
JNJ-26070109 | Drug Info | Preclinical | Gastroesophageal reflux disease | [541770], [548549] | |
PD-170292 | Drug Info | Preclinical | Obesity | [536122] | |
GV-150013 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [540443], [546000] | |
L-365260 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [543269], [544796] | |
PD-134308 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [544714] | |
CR-2093 | Drug Info | Discontinued in Phase 1 | Intestine cancer | [544899] | |
AG-041R | Drug Info | Terminated | Ulcerative colitis | [543292], [545856] | |
FR-208419 | Drug Info | Terminated | Dyspepsia | [546824] | |
GR-199114X | Drug Info | Terminated | Stomach ulcer | [546618] | |
IQM-95333 | Drug Info | Terminated | Discovery agent | [546593] | |
LY288513 | Drug Info | Terminated | Anxiety disorder | [543293], [545116] | |
PD-135666 | Drug Info | Terminated | Discovery agent | [543294], [546092] | |
PD136450 | Drug Info | Terminated | Discovery agent | [543235], [544817] | |
SNF-9007 | Drug Info | Terminated | Discovery agent | [546204] | |
YM-022 | Drug Info | Terminated | Gastrointestinal disease | [543279], [545651] | |
Inhibitor | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [531079] | ||
Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe | Drug Info | [551255] | |||
Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 | Drug Info | [532617] | |||
Cholecystokinin-9 | Drug Info | [527234] | |||
Dexloxiglumide | Drug Info | [534494] | |||
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo | Drug Info | [528606] | |||
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H | Drug Info | [528606] | |||
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H | Drug Info | [528058] | |||
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac | Drug Info | [528058] | |||
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc | Drug Info | [528058] | |||
IQM-95333 | Drug Info | [534494] | |||
PD-135118 | Drug Info | [551254] | |||
PD-135666 | Drug Info | [551254] | |||
PD-136621 | Drug Info | [551254] | |||
PD-137337 | Drug Info | [551254] | |||
PD-137342 | Drug Info | [551254] | |||
PD-138915 | Drug Info | [551254] | |||
PD-138916 | Drug Info | [551254] | |||
PD-138917 | Drug Info | [551254] | |||
PD-140547 | Drug Info | [551254] | |||
PD-140548 | Drug Info | [551254] | |||
PD-140723 | Drug Info | [551254] | |||
SNF-9007 | Drug Info | [528193] | |||
Tetragastrin | Drug Info | [533465] | |||
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc | Drug Info | [528058] | |||
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [528193] | |||
YF-476 | Drug Info | [527273] | |||
Modulator | AG-041R | Drug Info | [526056] | ||
CR-2093 | Drug Info | [533774] | |||
Demogastrin | Drug Info | [525622] | |||
FR-208419 | Drug Info | [525711] | |||
GR-199114X | Drug Info | [546619] | |||
L-365260 | Drug Info | ||||
PD-134308 | Drug Info | ||||
RP-71483 | Drug Info | [533750] | |||
RP-72540 | Drug Info | [533750] | |||
RPR-107836 | Drug Info | [543961] | |||
TT-223 | Drug Info | [525743] | |||
Z 360 | Drug Info | ||||
Agonist | BC-264 | Drug Info | [526915] | ||
CCK-33 | Drug Info | [533991] | |||
CCK-8 | Drug Info | [533991] | |||
Ceruletide | Drug Info | [536741] | |||
desulfated cholecystokinin-8 | Drug Info | [537852] | |||
PBC-264 | Drug Info | [534165] | |||
PD-170292 | Drug Info | [536122] | |||
Pentagastrin | Drug Info | [535744], [536753], [537852], [537987] | |||
RB-400 | Drug Info | [526915] | |||
[3H]PBC-264 | Drug Info | [527728] | |||
Antagonist | CI-1015 | Drug Info | [534543] | ||
GASTRAZOLE | Drug Info | [544049], [551871] | |||
GG-8573 | Drug Info | [536122] | |||
GV-150013 | Drug Info | [538152] | |||
GW-5823 | Drug Info | [534449] | |||
Itriglumide | Drug Info | [544087] | |||
JNJ-26070109 | Drug Info | [531786] | |||
LY288513 | Drug Info | [538145] | |||
PD-135158 | Drug Info | [534269] | |||
PD-149164 | Drug Info | [534279] | |||
PD136450 | Drug Info | [537923] | |||
RP-69758 | Drug Info | [533750] | |||
RP73870 | Drug Info | [525523] | |||
S-0509 | Drug Info | [525745], [551871] | |||
Spiroglumide | Drug Info | [537982] | |||
tetronothiodin | Drug Info | [533945] | |||
TP-680 | Drug Info | [534172] | |||
YM-022 | Drug Info | [534373] | |||
[125I]-BDZ2 | Drug Info | [530004] | |||
[125I]PD142308 | Drug Info | [543961] | |||
[3H]JB-93182 | Drug Info | [525478] | |||
[3H]L365260 | Drug Info | [526218] | |||
[3H]PD140376 | Drug Info | [534047] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
Gastric acid secretion | |||||
PANTHER Pathway | CCKR signaling map ST | ||||
PathWhiz Pathway | Gastric Acid Production | ||||
Reactome | Peptide ligand-binding receptors | ||||
G alpha (q) signalling events | |||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
Secretion of Hydrochloric Acid in Parietal Cells | |||||
Peptide GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
GPCRs, Other | |||||
References | |||||
Ref 521748 | ClinicalTrials.gov (NCT00243074) S0509: AZD2171 in Treating Patients With Malignant Pleural Mesothelioma That Cannot Be Removed By Surgery. U.S. National Institutes of Health. | ||||
Ref 522421 | ClinicalTrials.gov (NCT00743002) A Trial of TT223 in Patients With Type 2 Diabetes Who Are Taking Metformin and/or Thiazolidinedione. U.S. National Institutes of Health. | ||||
Ref 523439 | ClinicalTrials.gov (NCT01339169) YF476 and Type I Gastric Carcinoids. U.S. National Institutes of Health. | ||||
Ref 526774 | Inhibitory effect of CCK-8 and ceruletide on glutamate-induced rises in intracellular free calcium concentrations in rat neuron cultures. Brain Res. 1992 Aug 21;588(2):223-8. | ||||
Ref 528144 | Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 Apr 24;94(8):1107-15. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 538484 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017048. | ||||
Ref 540443 | (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: 3503). | ||||
Ref 541770 | (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: 6665). | ||||
Ref 542579 | (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: 7589). | ||||
Ref 543235 | (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: 867). | ||||
Ref 543256 | (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: 870). | ||||
Ref 543269 | (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: 879). | ||||
Ref 543278 | (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: 887). | ||||
Ref 543279 | (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: 888). | ||||
Ref 543292 | (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: 901). | ||||
Ref 543293 | (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: 902). | ||||
Ref 543294 | (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: 903). | ||||
Ref 543299 | (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: 909). | ||||
Ref 544714 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000702) | ||||
Ref 544796 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001138) | ||||
Ref 544817 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001217) | ||||
Ref 544899 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001442) | ||||
Ref 545116 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002176) | ||||
Ref 545651 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004033) | ||||
Ref 545856 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005071) | ||||
Ref 546000 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005803) | ||||
Ref 546092 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006308) | ||||
Ref 546204 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006885) | ||||
Ref 546593 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009097) | ||||
Ref 546618 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009210) | ||||
Ref 546824 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010485) | ||||
Ref 546827 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010503) | ||||
Ref 548549 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026533) | ||||
Ref 549943 | 99mTc-Demogastrin 2 for CCK 2-receptor scintigraphy in medullary thyroid carcinoma. J Nucl Med. 2008; 49 (Supplement 1):115P. | ||||
Ref 551871 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
Ref 525478 | Characterization of the binding of a novel radioligand to CCKB/gastrin receptors in membranes from rat cerebral cortex. Br J Pharmacol. 1999 Mar;126(6):1504-12. | ||||
Ref 525523 | Pharmacological analysis of CCK2 receptor antagonists using isolated rat stomach ECL cells. Br J Pharmacol. 1999 May;127(2):530-6. | ||||
Ref 525622 | Demonstration of new sites of expression of the CCK-B/gastrin receptor in pancreatic acinar AR42J cells using immunoelectron microscopy. Regul Pept. 1999 Oct 22;84(1-3):81-9. | ||||
Ref 525711 | Dual CCK-A and CCK-B receptor antagonists (II). Preparation and structure activity relationships of 5-alkyl-9-methyl-1,4-benzodiazepines and discovery of FR208419. Chem Pharm Bull (Tokyo). 2000 Jan;48(1):1-15. | ||||
Ref 525743 | The effect of glucagon-like peptide-1 on energy expenditure and substrate metabolism in humans. Int J Obes Relat Metab Disord. 2000 Mar;24(3):288-98. | ||||
Ref 525745 | Selective action of a CCK-B/gastrin receptor antagonist, S-0509, on pentagastrin-, peptone meal- and beer-stimulated gastric acid secretion in dogs. Aliment Pharmacol Ther. 2000 Apr;14(4):479-88. | ||||
Ref 526056 | AG-041R, a gastrin/CCK-B antagonist, stimulates chondrocyte proliferation and metabolism in vitro. Biochem Biophys Res Commun. 2001 May 25;283(5):1118-23. | ||||
Ref 526218 | Pharmacological analysis of CCK(2) receptor ligands using COS-7 and SK-N-MC cells, expressing the human CCK(2) receptor. Regul Pept. 2002 Jan 15;103(1):29-37. | ||||
Ref 526915 | Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties. Bioorg Med Chem Lett. 2004 Jan 19;14(2):369-72. | ||||
Ref 527234 | J Med Chem. 2004 Oct 7;47(21):5318-29.5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors. | ||||
Ref 527273 | CCK-B receptor antagonist YF476 inhibits pancreatic enzyme secretion at a duodenal level in pigs. Scand J Gastroenterol. 2004 Sep;39(9):886-90. | ||||
Ref 527728 | [3H]pBC 264, a suitable probe for studying cholecystokinin-B receptors: binding characteristics in rodent brains and comparison with [3H]SNF 8702. Mol Pharmacol. 1992 Jun;41(6):1089-95. | ||||
Ref 528058 | J Med Chem. 2006 Mar 9;49(5):1773-80.Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists. | ||||
Ref 528193 | J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. | ||||
Ref 528606 | J Med Chem. 2007 Jan 11;50(1):165-8.Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors. | ||||
Ref 530004 | Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors. J Med Chem. 2009 Apr 9;52(7):2138-47. | ||||
Ref 531079 | J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. | ||||
Ref 531786 | The cholecystokinin CCK2 receptor antagonist, JNJ-26070109, inhibits gastric acid secretion and prevents omeprazole-induced acid rebound in the rat. Br J Pharmacol. 2012 Jul;166(5):1684-93. | ||||
Ref 532617 | J Med Chem. 1987 Aug;30(8):1366-73.Synthesis and biological activities of pseudopeptide analogues of the C-terminal heptapeptide of cholecystokinin. On the importance of the peptide bonds. | ||||
Ref 533465 | J Med Chem. 1987 Apr;30(4):729-32.Synthesis and binding affinities of analogues of cholecystokinin-(30-33) as probes for central nervous system cholecystokinin receptors. | ||||
Ref 533750 | Pharmacological properties of ureido-acetamides, new potent and selective non-peptide CCKB/gastrin receptor antagonists. Eur J Pharmacol. 1994 Sep 12;262(3):233-45. | ||||
Ref 533774 | Inhibitory effects of the gastrin receptor antagonist CR2093 on basal, gastrin-stimulated and growth factor-stimulated growth of the rat pancreatic cell line AR42J. Anticancer Drugs. 1994 Oct;5(5):591-7. | ||||
Ref 533945 | Species specificity of pharmacological characteristics of CCK-B receptors. Neurosci Lett. 1993 Aug 6;158(1):1-4. | ||||
Ref 533991 | Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin. J Biol Chem. 1993 Aug 25;268(24):18300-5. | ||||
Ref 534047 | [3H]PD 140376: a novel and highly selective antagonist radioligand for the cholecystokininB/gastrin receptor in guinea pig cerebral cortex and gastric mucosa. Mol Pharmacol. 1993 Apr;43(4):595-602. | ||||
Ref 534165 | His381 of the rat CCKB receptor is essential for CCKB versus CCKA receptor antagonist selectivity. Eur J Pharmacol. 1996 Jan 18;296(1):97-106. | ||||
Ref 534172 | Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist. Br J Pharmacol. 1996 Apr;117(7):1558-64. | ||||
Ref 534269 | Pharmacological characterization of a Chinese hamster ovary cell line transfected with the human CCK-B receptor gene. Neuropeptides. 1996 Aug;30(4):359-63. | ||||
Ref 534279 | Cholecystokinin B antagonists. Synthesis and quantitative structure-activity relationships of a series of C-terminal analogues of CI-988. Bioorg Med Chem. 1996 Oct;4(10):1733-45. | ||||
Ref 534373 | YM022, a potent and selective gastrin/CCK-B receptor antagonist, inhibits peptone meal-induced gastric acid secretion in Heidenhain pouch dogs. Dig Dis Sci. 1997 Apr;42(4):707-14. | ||||
Ref 534449 | Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists. J Med Chem. 1997 Aug 15;40(17):2706-25. | ||||
Ref 534494 | J Med Chem. 1997 Oct 10;40(21):3402-7.Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists. | ||||
Ref 534543 | Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile. J Med Chem. 1998 Jan 1;41(1):38-45. | ||||
Ref 535744 | Molecular cloning of the human brain and gastric cholecystokinin receptor: structure, functional expression and chromosomal localization. Biochem Biophys Res Commun. 1992 Nov 30;189(1):296-303. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 536741 | Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8. | ||||
Ref 536753 | Functional interactions between endocannabinoid and CCK neurotransmitter systems may be critical for extinction learning. Neuropsychopharmacology. 2009 Jan;34(2):509-21. Epub 2008 Jun 25. | ||||
Ref 537852 | The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization. J Biol Chem. 1993 Apr 15;268(11):8164-9. | ||||
Ref 537923 | Cholecystokinin type B receptor antagonist PD-136,450 is a partial secretory agonist in the stomach and a full agonist in the pancreas of the rat. Gut. 1994 Feb;35(2):270-4. | ||||
Ref 537982 | Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo. Aliment Pharmacol Ther. 1996 Jun;10(3):411-9. | ||||
Ref 537987 | The effects of central administration of the CCK-B receptor agonist pentagastrin on feeding and cortisol release in sheep. Methods Find Exp Clin Pharmacol. 1996 May;18(4):235-8. | ||||
Ref 538145 | Behavioral and neurochemical study on the role of the brain cholecystokinin system in anxiety. Hokkaido Igaku Zasshi. 1998 Sep;73(5):463-73. | ||||
Ref 538152 | The role of cholecystokinin (CCK), CCK-A or CCK-B receptor antagonists in the spontaneous preference for drugs of abuse (alcohol or cocaine) in naive rats. Methods Find Exp Clin Pharmacol. 1998 Oct;20(8):679-97. | ||||
Ref 543961 | (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. (Target id: 77). | ||||
Ref 544049 | Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 April 24; 94(8): 1107-1115. | ||||
Ref 544087 | Role of CCK/gastrin receptors in gastrointestinal/metabolic diseases and results of human studies using gastrin/CCK receptor agonists/antagonists in these diseases. Curr Top Med Chem. 2007; 7(12): 1211-1231. | ||||
Ref 546619 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009210) | ||||
Ref 551254 | Selective ligands for cholecystokinin receptor subtypes CCK-A and CCK-B within a single structural class, Bioorg. Med. Chem. Lett. 3(5):881-884 (1993). | ||||
Ref 551255 | The rational design and synthesis of non-peptide ??hegnylogues??of CCK-26-33 - a novel series of CCK-A selective ligands, Bioorg. Med. Chem. Lett. 3(5):889-894 (1993). |
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