Target General Infomation
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
GASR_HUMAN
Sequence
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL
YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF
IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL
LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL
ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS
RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG
PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL
PDEDPPTPSIASLSRLSYTTISTLGPG
Drugs and Modes of Action
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
Target-regulating microRNAs
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Affiliated Biological Pathways
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
Target Validation
Target QSAR Model
References
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.

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