Target Information

Target General Infomation
Target ID
T05849
Former ID
TTDS00043
Target Name
Gastrin/cholecystokinin type B receptor
Gene Name
CCKBR
Synonyms
CCK-B receptor; CCK-BR; CCKBR
Target Type
Successful
Disease Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Caerulein stimulated gastric and pancreatic secretion [ICD code not available]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Dyspepsia [ICD9: 536.8; ICD10: K30]
Diagnostic imaging [ICD9: 331; ICD10: G30, I73.9]
Duodenal ulcers [ICD10: K25-K27]
Gallstone prophylaxis; Obesity [ICD9: 278; ICD10: E66]
Gastrointestinal disease [ICD10: K00-K93]
Gastroesophageal reflux disease [ICD9: 140-229, 530; ICD10: K21]
Intestine cancer [ICD10: C17-C20, C26]
Medullary thyroid cancer [ICD9: 193; ICD10: C73]
Obesity [ICD9: 278; ICD10: E66]
Pancreatic disease [ICD10: K85-K86]
Stomach ulcer [ICD10: K25-K27]
Stomach disease [ICD10: K30-K31]
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T05849
UniProt ID
P32239
Sequence
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL
YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF
IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL
LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL
ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS
RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG
PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL
PDEDPPTPSIASLSRLSYTTISTLGPG
Drugs and Mode of Action
Drug(s) Ceruletide Drug Info Approved Caerulein stimulated gastric and pancreatic secretion [1]
Pentagastrin Drug Info Approved Diagnostic imaging [2], [3]
Ceruletide Drug Info Phase 3 Cancer [4], [5]
GASTRAZOLE Drug Info Phase 3 Duodenal ulcers [6]
Dexloxiglumide Drug Info Phase 2 Pancreatic disease [1]
Itriglumide Drug Info Phase 2 Anxiety disorder [7], [8]
S-0509 Drug Info Phase 2 Ulcerative colitis [9]
Spiroglumide Drug Info Phase 2 Stomach disease [10]
TT-223 Drug Info Phase 2 Type 1 diabetes [11]
YF-476 Drug Info Phase 2 Stomach ulcer [12], [13]
Z 360 Drug Info Phase 2 Unspecified [14], [15]
Demogastrin Drug Info Phase 1 Medullary thyroid cancer [16]
GG-8573 Drug Info Preclinical Gallstone prophylaxis; Obesity [17]
JNJ-26070109 Drug Info Preclinical Gastroesophageal reflux disease [18], [19]
PD-170292 Drug Info Preclinical Obesity [17]
GV-150013 Drug Info Discontinued in Phase 2 Anxiety disorder [20], [21]
L-365260 Drug Info Discontinued in Phase 2 Anxiety disorder [22], [23]
PD-134308 Drug Info Discontinued in Phase 2 Anxiety disorder [24]
CR-2093 Drug Info Discontinued in Phase 1 Intestine cancer [25]
AG-041R Drug Info Terminated Ulcerative colitis [26], [27]
FR-208419 Drug Info Terminated Dyspepsia [28]
GR-199114X Drug Info Terminated Stomach ulcer [29]
IQM-95333 Drug Info Terminated Discovery agent [30]
LY288513 Drug Info Terminated Anxiety disorder [31], [32]
PD-135666 Drug Info Terminated Discovery agent [33], [34]
PD136450 Drug Info Terminated Discovery agent [35], [36]
SNF-9007 Drug Info Terminated Discovery agent [37]
YM-022 Drug Info Terminated Gastrointestinal disease [38], [39]
Inhibitor 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [40]
Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe Drug Info [41]
Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 Drug Info [42]
Cholecystokinin-9 Drug Info [43]
Dexloxiglumide Drug Info [44]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo Drug Info [45]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H Drug Info [45]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H Drug Info [46]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac Drug Info [46]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc Drug Info [46]
IQM-95333 Drug Info [44]
PD-135118 Drug Info [47]
PD-135666 Drug Info [47]
PD-136621 Drug Info [47]
PD-137337 Drug Info [47]
PD-137342 Drug Info [47]
PD-138915 Drug Info [47]
PD-138916 Drug Info [47]
PD-138917 Drug Info [47]
PD-140547 Drug Info [47]
PD-140548 Drug Info [47]
PD-140723 Drug Info [47]
SNF-9007 Drug Info [48]
Tetragastrin Drug Info [49]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc Drug Info [46]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [48]
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [48]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [48]
Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [48]
YF-476 Drug Info [50]
Modulator AG-041R Drug Info [51]
CR-2093 Drug Info [52]
Demogastrin Drug Info [53]
FR-208419 Drug Info [54]
GR-199114X Drug Info [55]
L-365260 Drug Info
PD-134308 Drug Info
RP-71483 Drug Info [56]
RP-72540 Drug Info [56]
RPR-107836 Drug Info [57]
TT-223 Drug Info [58]
Z 360 Drug Info
Agonist BC-264 Drug Info [59]
CCK-33 Drug Info [60]
CCK-8 Drug Info [60]
Ceruletide Drug Info [61]
desulfated cholecystokinin-8 Drug Info [62]
PBC-264 Drug Info [63]
PD-170292 Drug Info [17]
Pentagastrin Drug Info [64], [65], [62], [66]
RB-400 Drug Info [59]
[3H]PBC-264 Drug Info [67]
Antagonist CI-1015 Drug Info [68]
GASTRAZOLE Drug Info [69], [1]
GG-8573 Drug Info [17]
GV-150013 Drug Info [70]
GW-5823 Drug Info [71]
Itriglumide Drug Info [72]
JNJ-26070109 Drug Info [73]
LY288513 Drug Info [74]
PD-135158 Drug Info [75]
PD-149164 Drug Info [76]
PD136450 Drug Info [77]
RP-69758 Drug Info [56]
RP73870 Drug Info [78]
S-0509 Drug Info [79], [1]
Spiroglumide Drug Info [80]
tetronothiodin Drug Info [81]
TP-680 Drug Info [82]
YM-022 Drug Info [83]
[125I]-BDZ2 Drug Info [84]
[125I]PD142308 Drug Info [57]
[3H]JB-93182 Drug Info [85]
[3H]L365260 Drug Info [86]
[3H]PD140376 Drug Info [87]
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 1Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 2FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017048.
REF 3(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 4Inhibitory 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 5(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 6Gastrazole (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 7(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 8Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010503)
REF 9ClinicalTrials.gov (NCT00243074) S0509: AZD2171 in Treating Patients With Malignant Pleural Mesothelioma That Cannot Be Removed By Surgery. U.S. National Institutes of Health.
REF 10Progress medicinal chem PMC37H. Page(48).
REF 11ClinicalTrials.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 12ClinicalTrials.gov (NCT01339169) YF476 and Type I Gastric Carcinoids. U.S. National Institutes of Health.
REF 13(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 14Z-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 15Z-360, a novel cholecystokinin-2/gastrin receptor antagonist, inhibits gemcitabine-induced expression of the vascular endothelial growth factor gene in human pancreatic cancer cells.
REF 1699mTc-Demogastrin 2 for CCK 2-receptor scintigraphy in medullary thyroid carcinoma. J Nucl Med. 2008; 49 (Supplement 1):115P.
REF 17Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
REF 18(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 19Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026533)
REF 20(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 21Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005803)
REF 22(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 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001138)
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000702)
REF 25Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001442)
REF 26(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 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005071)
REF 28Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010485)
REF 29Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009210)
REF 30Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009097)
REF 31(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 32Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002176)
REF 33(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 34Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006308)
REF 35(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 36Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001217)
REF 37Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006885)
REF 38(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 39Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004033)
REF 40J 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 41The 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 42J 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 43J 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 44J 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 45J 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 46J 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 47Selective 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 48J 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 49J 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 50CCK-B receptor antagonist YF476 inhibits pancreatic enzyme secretion at a duodenal level in pigs. Scand J Gastroenterol. 2004 Sep;39(9):886-90.
REF 51AG-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 52Inhibitory 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 53Demonstration 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 54Dual 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 55Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009210)
REF 56Pharmacological 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 57(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 58The 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 59Synthesis 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 60Functional 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 61Comparison of postprandial and ceruletide serum bile acid stimulation in dogs. J Vet Intern Med. 2008 Jul-Aug;22(4):873-8.
REF 62The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization. J Biol Chem. 1993 Apr 15;268(11):8164-9.
REF 63His381 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 64Molecular 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 65Functional 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 66The 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 67[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 68Second 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 69Gastrazole (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 70The 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 71Optimization 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 72Role 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 73The 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 74Behavioral and neurochemical study on the role of the brain cholecystokinin system in anxiety. Hokkaido Igaku Zasshi. 1998 Sep;73(5):463-73.
REF 75Pharmacological characterization of a Chinese hamster ovary cell line transfected with the human CCK-B receptor gene. Neuropeptides. 1996 Aug;30(4):359-63.
REF 76Cholecystokinin 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 77Cholecystokinin 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 78Pharmacological analysis of CCK2 receptor antagonists using isolated rat stomach ECL cells. Br J Pharmacol. 1999 May;127(2):530-6.
REF 79Selective 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 80Effect 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 81Species specificity of pharmacological characteristics of CCK-B receptors. Neurosci Lett. 1993 Aug 6;158(1):1-4.
REF 82Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist. Br J Pharmacol. 1996 Apr;117(7):1558-64.
REF 83YM022, 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 84Synthesis 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 85Characterization 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 86Pharmacological 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 87[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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