Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T05849
(Former ID: TTDS00043)
|
|||||
| Target Name |
Gastrin/cholecystokinin type B receptor (CCKBR)
|
|||||
| Synonyms |
Cholecystokinin-2 receptor; CCKRB; CCK2-R; CCK-BR; CCK-B receptor
|
|||||
| Gene Name |
CCKBR
|
|||||
| Target Type |
Successful target
|
[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Diagnostic imaging [ICD-11: N.A.] | |||||
| 2 | Pancreatic internal secretion disorder [ICD-11: 5A4Y] | |||||
| Function |
The CCK-B receptors occur throughout the central nervous system where they modulate anxiety, analgesia, arousal, and neuroleptic activity. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Receptor for gastrin and cholecystokinin.
|
|||||
| BioChemical Class |
GPCR rhodopsin
|
|||||
| UniProt ID | ||||||
| Sequence |
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL
YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL PDEDPPTPSIASLSRLSYTTISTLGPG |
|||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Ceruletide | Drug Info | Approved | Caerulein stimulated gastric and pancreatic secretion | [2] | |
| 2 | Pentagastrin | Drug Info | Approved | Diagnostic imaging | [3], [4] | |
| Clinical Trial Drug(s) | [+] 9 Clinical Trial Drugs | + | ||||
| 1 | GASTRAZOLE | Drug Info | Phase 3 | Duodenal ulcer | [5] | |
| 2 | Dexloxiglumide | Drug Info | Phase 2 | Pancreatic malfunction | [2] | |
| 3 | Itriglumide | Drug Info | Phase 2 | Anxiety disorder | [6], [7] | |
| 4 | S-0509 | Drug Info | Phase 2 | Ulcerative colitis | [8] | |
| 5 | Spiroglumide | Drug Info | Phase 2 | Stomach disease | [9] | |
| 6 | TT-223 | Drug Info | Phase 2 | Type-1 diabetes | [10] | |
| 7 | YF-476 | Drug Info | Phase 2 | Stomach ulcer | [11], [12] | |
| 8 | Z 360 | Drug Info | Phase 2 | Discovery agent | [13], [14] | |
| 9 | Demogastrin | Drug Info | Phase 1 | Thyroid cancer | [15] | |
| Discontinued Drug(s) | [+] 9 Discontinued Drugs | + | ||||
| 1 | GV-150013 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [16], [17] | |
| 2 | L-365260 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [18], [19] | |
| 3 | PD-134308 | Drug Info | Discontinued in Phase 2 | Anxiety disorder | [20] | |
| 4 | CR-2093 | Drug Info | Discontinued in Phase 1 | Intestine cancer | [21] | |
| 5 | AG-041R | Drug Info | Terminated | Ulcerative colitis | [25], [26] | |
| 6 | FR-208419 | Drug Info | Terminated | Dyspepsia | [27] | |
| 7 | GR-199114X | Drug Info | Terminated | Stomach ulcer | [28] | |
| 8 | LY288513 | Drug Info | Terminated | Anxiety disorder | [29], [30] | |
| 9 | YM-022 | Drug Info | Terminated | Gastrointestinal disease | [31], [32] | |
| Preclinical Drug(s) | [+] 3 Preclinical Drugs | + | ||||
| 1 | GG-8573 | Drug Info | Preclinical | Obesity | [22] | |
| 2 | JNJ-26070109 | Drug Info | Preclinical | Gastroesophageal reflux disease | [23], [24] | |
| 3 | PD-170292 | Drug Info | Preclinical | Obesity | [22] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Agonist | [+] 10 Agonist drugs | + | ||||
| 1 | Ceruletide | Drug Info | [33] | |||
| 2 | Pentagastrin | Drug Info | [1], [34], [35], [36] | |||
| 3 | PD-170292 | Drug Info | [22] | |||
| 4 | BC-264 | Drug Info | [62] | |||
| 5 | CCK-33 | Drug Info | [64] | |||
| 6 | CCK-8 | Drug Info | [64] | |||
| 7 | desulfated cholecystokinin-8 | Drug Info | [36] | |||
| 8 | PBC-264 | Drug Info | [70] | |||
| 9 | RB-400 | Drug Info | [62] | |||
| 10 | [3H]PBC-264 | Drug Info | [81] | |||
| Antagonist | [+] 22 Antagonist drugs | + | ||||
| 1 | GASTRAZOLE | Drug Info | [37], [2] | |||
| 2 | Itriglumide | Drug Info | [39] | |||
| 3 | S-0509 | Drug Info | [40], [2] | |||
| 4 | Spiroglumide | Drug Info | [41] | |||
| 5 | GV-150013 | Drug Info | [45] | |||
| 6 | GG-8573 | Drug Info | [22] | |||
| 7 | JNJ-26070109 | Drug Info | [51] | |||
| 8 | LY288513 | Drug Info | [55] | |||
| 9 | PD136450 | Drug Info | [57] | |||
| 10 | YM-022 | Drug Info | [59] | |||
| 11 | CI-1015 | Drug Info | [66] | |||
| 12 | GW-5823 | Drug Info | [67] | |||
| 13 | PD-135158 | Drug Info | [71] | |||
| 14 | PD-149164 | Drug Info | [72] | |||
| 15 | RP-69758 | Drug Info | [73] | |||
| 16 | RP73870 | Drug Info | [74] | |||
| 17 | tetronothiodin | Drug Info | [77] | |||
| 18 | TP-680 | Drug Info | [78] | |||
| 19 | [125I]-BDZ2 | Drug Info | [79] | |||
| 20 | [125I]PD142308 | Drug Info | [75] | |||
| 21 | [3H]JB-93182 | Drug Info | [80] | |||
| 22 | [3H]PD140376 | Drug Info | [82] | |||
| Inhibitor | [+] 41 Inhibitor drugs | + | ||||
| 1 | Dexloxiglumide | Drug Info | [38] | |||
| 2 | YF-476 | Drug Info | [43] | |||
| 3 | IQM-95333 | Drug Info | [38] | |||
| 4 | PD-135666 | Drug Info | [56] | |||
| 5 | SNF-9007 | Drug Info | [58] | |||
| 6 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [60] | |||
| 7 | Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe | Drug Info | [61] | |||
| 8 | Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 | Drug Info | [63] | |||
| 9 | Cholecystokinin-9 | Drug Info | [65] | |||
| 10 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo | Drug Info | [68] | |||
| 11 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H | Drug Info | [68] | |||
| 12 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H | Drug Info | [69] | |||
| 13 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac | Drug Info | [69] | |||
| 14 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc | Drug Info | [69] | |||
| 15 | PD-135118 | Drug Info | [56] | |||
| 16 | PD-136621 | Drug Info | [56] | |||
| 17 | PD-137337 | Drug Info | [56] | |||
| 18 | PD-137342 | Drug Info | [56] | |||
| 19 | PD-138915 | Drug Info | [56] | |||
| 20 | PD-138916 | Drug Info | [56] | |||
| 21 | PD-138917 | Drug Info | [56] | |||
| 22 | PD-140547 | Drug Info | [56] | |||
| 23 | PD-140548 | Drug Info | [56] | |||
| 24 | PD-140723 | Drug Info | [56] | |||
| 25 | Tetragastrin | Drug Info | [76] | |||
| 26 | Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 27 | Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 28 | Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc | Drug Info | [69] | |||
| 29 | Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 30 | Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 31 | Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 32 | Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 33 | Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 34 | Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 35 | Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 36 | Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 37 | Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 38 | Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 39 | Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 40 | Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [58] | |||
| 41 | Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [58] | |||
| Modulator | [+] 12 Modulator drugs | + | ||||
| 1 | TT-223 | Drug Info | [42] | |||
| 2 | Z 360 | Drug Info | [13], [14] | |||
| 3 | Demogastrin | Drug Info | [44] | |||
| 4 | L-365260 | Drug Info | [46], [47] | |||
| 5 | PD-134308 | Drug Info | [48], [49] | |||
| 6 | CR-2093 | Drug Info | [50] | |||
| 7 | AG-041R | Drug Info | [52] | |||
| 8 | FR-208419 | Drug Info | [53] | |||
| 9 | GR-199114X | Drug Info | [54] | |||
| 10 | RP-71483 | Drug Info | [73] | |||
| 11 | RP-72540 | Drug Info | [73] | |||
| 12 | RPR-107836 | Drug Info | [75] | |||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | Calcium signaling pathway | |||||
| 2 | Neuroactive ligand-receptor interaction | |||||
| 3 | Gastric acid secretion | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | CCKR signaling map ST | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Gastric Acid Production | |||||
| Reactome | [+] 3 Reactome Pathways | + | ||||
| 1 | Peptide ligand-binding receptors | |||||
| 2 | G alpha (q) signalling events | |||||
| 3 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| WikiPathways | [+] 7 WikiPathways | + | ||||
| 1 | GPCRs, Class A Rhodopsin-like | |||||
| 2 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| 3 | Secretion of Hydrochloric Acid in Parietal Cells | |||||
| 4 | Peptide GPCRs | |||||
| 5 | GPCR ligand binding | |||||
| 6 | GPCR downstream signaling | |||||
| 7 | GPCRs, Other | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Functional interactions between endocannabinoid and CCK neurotransmitter systems may be critical for extinction learning. Neuropsychopharmacology. 2009 Jan;34(2):509-21. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | URL: 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 4 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017048. | |||||
| REF 5 | 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 6 | URL: 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 7 | 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 8 | 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 9 | Progress medicinal chem PMC37H. Page(48). | |||||
| REF 10 | 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 11 | URL: 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 12 | ClinicalTrials.gov (NCT01339169) YF476 and Type I Gastric Carcinoids. U.S. National Institutes of Health. | |||||
| REF 13 | Z-360, a novel cholecystokinin-2/gastrin receptor antagonist, inhibits gemcitabine-induced expression of the vascular endothelial growth factor gen... Biol Pharm Bull. 2010;33(2):216-22. | |||||
| REF 14 | Z-360, a novel therapeutic agent for pancreatic cancer, prevents up-regulation of ephrin B1 gene expression and phosphorylation of NR2B via suppression of interleukin-1 production in a cancer-induced pain model in mice.Mol Pain.2010 Oct 28;6:72. | |||||
| REF 15 | 99mTc-Demogastrin 2 for CCK 2-receptor scintigraphy in medullary thyroid carcinoma. J Nucl Med. 2008; 49 (Supplement 1):115P. | |||||
| REF 16 | URL: 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 17 | 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 18 | URL: 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 19 | 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 20 | 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 21 | 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 22 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | |||||
| REF 23 | URL: 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 24 | 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 25 | URL: 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 26 | 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 27 | 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 28 | 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 29 | URL: 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 30 | 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 31 | URL: 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 32 | 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 33 | Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8. | |||||
| REF 34 | 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 35 | 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 36 | The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization. J Biol Chem. 1993 Apr 15;268(11):8164-9. | |||||
| REF 37 | 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 38 | Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecy... J Med Chem. 1997 Oct 10;40(21):3402-7. | |||||
| REF 39 | 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 40 | 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 41 | 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 42 | 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 43 | 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 44 | 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 45 | 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 46 | 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 47 | A placebo-controlled trial of L-365,260, a CCKB antagonist, in panic disorder. Biol Psychiatry. 1995 Apr 1;37(7):462-6. | |||||
| REF 48 | Comparison of the effects of the cholecystokinin-B receptor antagonist, PD 134308, and the cholecystokinin-A receptor antagonist, L-364,718, on dop... Synapse. 1993 Feb;13(2):117-22. | |||||
| REF 49 | Evaluation of the effects of PD 134308 (CI-988), a CCK-B antagonist, on the punished responding of squirrel monkeys. Neuropeptides. 1991 Jul;19 Suppl:75-8. | |||||
| REF 50 | 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 51 | 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 52 | 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 53 | 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 54 | 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 55 | Behavioral and neurochemical study on the role of the brain cholecystokinin system in anxiety. Hokkaido Igaku Zasshi. 1998 Sep;73(5):463-73. | |||||
| REF 56 | 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 57 | 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 58 | Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. J Med Chem. 2006 May 18;49(10):2868-75. | |||||
| REF 59 | 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 60 | 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 rec... J Med Chem. 2010 Sep 9;53(17):6386-97. | |||||
| REF 61 | 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). | |||||
| REF 62 | 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 63 | Synthesis and biological activities of pseudopeptide analogues of the C-terminal heptapeptide of cholecystokinin. On the importance of the peptide ... J Med Chem. 1987 Aug;30(8):1366-73. | |||||
| REF 64 | 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 65 | 5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectiv... J Med Chem. 2004 Oct 7;47(21):5318-29. | |||||
| REF 66 | 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 67 | 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 68 | Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors. J Med Chem. 2007 Jan 11;50(1):165-8. | |||||
| REF 69 | Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists. J Med Chem. 2006 Mar 9;49(5):1773-80. | |||||
| REF 70 | 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 71 | 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 72 | 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 73 | 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 74 | Pharmacological analysis of CCK2 receptor antagonists using isolated rat stomach ECL cells. Br J Pharmacol. 1999 May;127(2):530-6. | |||||
| REF 75 | URL: 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 76 | Synthesis and binding affinities of analogues of cholecystokinin-(30-33) as probes for central nervous system cholecystokinin receptors. J Med Chem. 1987 Apr;30(4):729-32. | |||||
| REF 77 | Species specificity of pharmacological characteristics of CCK-B receptors. Neurosci Lett. 1993 Aug 6;158(1):1-4. | |||||
| REF 78 | Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist. Br J Pharmacol. 1996 Apr;117(7):1558-64. | |||||
| REF 79 | 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 80 | 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 81 | [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 82 | [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. | |||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Wang and Dr. Li.