Target Information

Target General Infomation
Target ID
T28330
Former ID
TTDC00082
Target Name
Cholecystokinin receptor type A
Gene Name
CCKAR
Synonyms
CCK-A receptor; CCK-AR; CCKAR
Target Type
Discontinued
Disease Bladder disease [ICD10: N30-N32]
Dyspepsia [ICD9: 536.8; ICD10: K30]
Eating disorder [ICD9: 278, 307.5, 401, 428.0; ICD10: E66, F50, I10-I16, I50]
Gastrointestinal disease [ICD10: K00-K93]
Gallstone prophylaxis; Obesity [ICD9: 278; ICD10: E66]
Obesity [ICD9: 278; ICD10: E66]
Obesity; Eating disorders [ICD9: 278, 307.5; ICD10: E66, F50]
Pancreatic disease [ICD10: K85-K86]
Pancreatic cancer; Obesity [ICD9: 140-229, 157, 278; ICD10: C25, E66]
Function
Receptor forcholecystokinin. Mediates pancreatic growth and enzyme secretion, smooth muscle contraction of the gall bladder and stomach. Has a 1000-fold higher affinity for CCK rather than for gastrin. It modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
BioChemical Class
GPCR rhodopsin
Target Validation
T28330
UniProt ID
P32238
Sequence
MDVVDSLLVNGSNITPPCELGLENETLFCLDQPRPSKEWQPAVQILLYSLIFLLSVLGNT
LVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYF
MGTSVSVSTFNLVAISLERYGAICKPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYS
NLVPFTKNNNQTANMCRFLLPNDVMQQSWHTFLLLILFLIPGIVMMVAYGLISLELYQGI
KFEASQKKSAKERKPSTTSSGKYEDSDGCYLQKTRPPRKLELRQLSTGSSSRANRIRSNS
SAANLMAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTASAERRLSGTPISFILLLSY
TSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGARGEVGEEEEGGTTGASLSRFSYSH
MSASVPPQ
Drugs and Mode of Action
Drug(s) Dexloxiglumide Drug Info Phase 2 Pancreatic disease [1]
A-71378 Drug Info Preclinical Obesity [2], [3]
A-74498 Drug Info Preclinical Obesity [2]
AR-R-1589 Drug Info Preclinical Obesity; Eating disorders [2]
FPL-14294 Drug Info Preclinical Obesity [2]
GG-8573 Drug Info Preclinical Gallstone prophylaxis; Obesity [2]
PD-170292 Drug Info Preclinical Obesity [2]
CE-326597 Drug Info Discontinued in Phase 2 Obesity [4]
GI 181771 Drug Info Discontinued in Phase 2 Obesity [5]
Lintitript Drug Info Discontinued in Phase 2 Pancreatic cancer; Obesity [6], [7]
Pranazepide Drug Info Discontinued in Phase 2 Pancreatic disease [8], [9]
Tarazepide Drug Info Discontinued in Phase 2 Gastrointestinal disease [10]
SR-146131 Drug Info Discontinued in Phase 1 Obesity [11], [12]
SSR-125180 Drug Info Discontinued in Phase 1 Obesity [13]
T-0632 Drug Info Discontinued in Phase 1 Pancreatic disease [14], [15]
UCL-2000 and butabindide Drug Info Discontinued in Phase 1 Obesity [16]
A-70276 Drug Info Terminated Gastrointestinal disease [17]
A-71623 Drug Info Terminated Obesity [18], [19]
CR-1795 Drug Info Terminated Discovery agent [20]
FR-208419 Drug Info Terminated Dyspepsia [21]
GI-248573 Drug Info Terminated Bladder disease [22]
IQM-95333 Drug Info Terminated Discovery agent [23]
Lorglumide Drug Info Terminated Pancreatic disease [24], [25]
PD-135666 Drug Info Terminated Discovery agent [26], [27]
SNF-9007 Drug Info Terminated Discovery agent [28]
SR-27950 Drug Info Terminated Eating disorder [29]
Inhibitor 1-(3,3-Diphenyl-allyl)-3-m-tolyl-urea Drug Info [30]
1-(4-Chloro-phenyl)-3-(3,3-diphenyl-allyl)-urea Drug Info [30]
1-(4-Chloro-phenyl)-3-(3-pentyl-oct-2-enyl)-urea Drug Info [30]
3,4-Dichloro-N-(3,3-diphenyl-allyl)-benzamide Drug Info [30]
Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe Drug Info [31]
Asp-Tyr(SO3H)-Met-Gly-Trp-Met-Asp-Phe-NH2 Drug Info [32]
Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 Drug Info [33]
Boc-cyclo-(Glu-Tyr-Nle-D-Lys)-Trp-Nle-Asp-Phe-NH2 Drug Info [32]
Boc-D-Glu-Tyr(SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2 Drug Info [32]
Boc-D-Glu-Tyr(SO3H)-Nle-D-Nle-Trp-Nle-Asp-Phe-NH2 Drug Info [32]
Boc-Glu-Tyr(SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2 Drug Info [32]
Boc-Tyr(SO3H)-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [32]
CR-1795 Drug Info [34]
CR-2345 Drug Info [34]
Dexloxiglumide Drug Info [35]
FR-175985 Drug Info [36]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H Drug Info [37]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H Drug Info [38]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc Drug Info [38]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H Drug Info [37]
IQM-95333 Drug Info [39]
L-708474 Drug Info [40]
L-740093 Drug Info [41]
PD-135118 Drug Info [42]
PD-135666 Drug Info [42]
PD-136621 Drug Info [42]
PD-137337 Drug Info [42]
PD-137342 Drug Info [42]
PD-138915 Drug Info [42]
PD-138916 Drug Info [42]
PD-140547 Drug Info [42]
PD-140548 Drug Info [42]
PD-140723 Drug Info [42]
Pranazepide Drug Info [36]
SNF-9007 Drug Info [43]
Tetragastrin Drug Info [44]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info [43]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [43]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc Drug Info [38]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [43]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [43]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [43]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [43]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info [43]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [43]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [43]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [43]
VL-0395 Drug Info [45]
VL-0494 Drug Info [46]
VL-0699 Drug Info [47]
VL-1499 Drug Info [45]
VL-2799 Drug Info [48]
Antagonist 2-NAP Drug Info [49]
Asperlicin Drug Info [50]
CI-1015 Drug Info [51]
Devazepide Drug Info [50]
IQM-97423 Drug Info [52]
JNJ-17156516 Drug Info [53]
KSG-504 Drug Info [54]
L-736380 Drug Info [55]
Lintitript Drug Info [56], [57]
Lorglumide Drug Info [58]
Loxiglumide Drug Info [59]
PD-135158 Drug Info [60]
proglumide Drug Info [61]
SC-50998 Drug Info [62]
T-0632 Drug Info [63]
Tarazepide Drug Info [64], [65], [66]
TP-680 Drug Info [67]
[3H]devazepide Drug Info [68]
Modulator A-70276 Drug Info [69]
A-71623 Drug Info [70]
FR-208419 Drug Info [71]
GI-248573 Drug Info [72]
SR-27950 Drug Info [62]
Agonist A-71378 Drug Info [2]
A-74498 Drug Info [2]
AR-R-1589 Drug Info [2]
CCK-33 Drug Info [73]
CCK-8 Drug Info [60]
CE-326597 Drug Info [74]
FPL-14294 Drug Info [2]
GG-8573 Drug Info [2]
GI 181771 Drug Info [75]
Glaxo-11p Drug Info [76]
GW-5823 Drug Info [77]
JMV180 Drug Info [78]
PD-170292 Drug Info [2]
SR-146131 Drug Info [79]
SSR-125180 Drug Info [72]
UCL-2000 and butabindide Drug Info [2]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
Neuroactive ligand-receptor interaction
Insulin secretion
Pancreatic secretion
Reactome Peptide ligand-binding receptors
G alpha (q) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Gastrin-CREB signalling pathway via PKC and MAPK
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
REF 1Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 2Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
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: 894).
REF 4ClinicalTrials.gov (NCT00542009) A Trial In Diabetic Patients To Assess Effect Of CE-326,597 On Glucose Control And Body Weight. U.S. National Institutes of Health.
REF 5Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013294)
REF 6(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: 890).
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004912)
REF 8(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: 874).
REF 9Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003071)
REF 10Cholecystokinin receptor-1 mediates the inhibitory effects of exogenous cholecystokinin octapeptide on cellular morphine dependence. BMC Neurosci. 2012 Jun 8;13:63.
REF 11(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: 868).
REF 12Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010439)
REF 13Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015967)
REF 14(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: 884).
REF 15Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007781)
REF 16Clinical pipeline report, company report or official report of University College London.
REF 17Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003433)
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: 858).
REF 19Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003438)
REF 20Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008170)
REF 21Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010485)
REF 22Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008844)
REF 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009097)
REF 24(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: 891).
REF 25Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000580)
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: 903).
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006308)
REF 28Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006885)
REF 29Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001260)
REF 30J Med Chem. 1992 Mar 20;35(6):1042-9.Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718.
REF 31Toward developing peptidomimetics: Successful replacement of backbone amide bonds in tetrapeptide-based CCK-A receptor agonists, Bioorg. Med. Chem. Lett. 3(5):855-860 (1993).
REF 32J Med Chem. 1989 Jun;32(6):1184-90.Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors.
REF 33J 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 34Biological properties of (R)-4-benzamido-5-oxopentanoic basic derivatives as CCK-antagonists, Bioorg. Med. Chem. Lett. 3(5):861-866 (1993).
REF 35J Med Chem. 1989 Feb;32(2):445-9.Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue.
REF 36Dual CCK-A and -B receptor antagonists (I) C9-methyl-1,4-benzodiazepines, Bioorg. Med. Chem. Lett. 7(2):169-174 (1997).
REF 37J 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 38J 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 39J 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 40J Med Chem. 1994 Mar 18;37(6):719-21.High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group.
REF 41C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists, Bioorg. Med. Chem. Lett. 5(24):3023-3026 (1995).
REF 42Selective 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 43J 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 44J 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 45Bioorg Med Chem. 2009 Jul 15;17(14):5198-206. Epub 2009 Jun 2.2D-QSAR and 3D-QSAR/CoMFA analyses of the N-terminal substituted anthranilic acid based CCK(1) receptor antagonists: 'Hic Rhodus, hic saltus'.
REF 46Bioorg Med Chem Lett. 2007 May 15;17(10):2749-55. Epub 2007 Mar 3.Synthesis and evaluation of novel benzimidazole derivative [Bz-Im] and its radio/biological studies.
REF 47J Med Chem. 2006 Apr 20;49(8):2456-62.Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their "receptor desmodynamic processes".
REF 48Bioorg Med Chem. 2009 Mar 15;17(6):2336-50. Epub 2009 Feb 14.Anthranilic acid based CCK1 receptor antagonists: blocking the receptor with the same 'words' of the endogenous ligand.
REF 49Unexpected relationship between plasma protein binding and the pharmacodynamics of 2-NAP, a CCK1-receptor antagonist. Br J Clin Pharmacol. 2007 May;63(5):618-22. Epub 2006 Oct 17.
REF 50Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
REF 51Second 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 52Pharmacological study of IQM-97,423, a potent and selective CCK1 receptor antagonist with protective effect in experimental acute pancreatitis. Pharmacology. 2004 Oct;72(2):68-76.
REF 533-[5-(3,4-Dichloro-phenyl)-1-(4-methoxy-phenyl)-1H-pyrazol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a novel, potent, and selective cholecystokinin 1 receptor antagonist: in vitro and in vivo pharmacological comparison with dexloxiglumide. J Pharmacol Exp Ther. 2007 Nov;323(2):562-9. Epub 2007 Aug 7.
REF 54Effects of KSG-504, a new CCK-A receptor antagonist, on gallbladder and gastrointestinal functions. Nihon Yakurigaku Zasshi. 1996 Jan;107(1):33-44.
REF 55Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas. J Med Chem. 1996 Feb 16;39(4):842-9.
REF 56A novel role for cholecystokinin: regulation of mesenteric vascular resistance. Regul Pept. 2004 Sep 15;121(1-3):145-53.
REF 57A cholecystokinin-1 receptor agonist (CCK-8) mediates increased permeability of brain barriers to leptin. Br J Pharmacol. 2008 Jul;154(5):1009-15. Epub 2008 Apr 21.
REF 58Behavioral and neurochemical study on the role of the brain cholecystokinin system in anxiety. Hokkaido Igaku Zasshi. 1998 Sep;73(5):463-73.
REF 59Role of CCK(A) receptors in postprandial lower esophageal sphincter function in morbidly obese subjects. Dig Dis Sci. 2002 Nov;47(11):2531-7.
REF 60Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc Natl Acad Sci U S A. 1990 Sep;87(17):6728-32.
REF 61Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung. 1987 Nov;37(11):1265-8.
REF 62(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: 76).
REF 63Effect of T-0632, a cholecystokininA receptor antagonist, on experimental acute pancreatitis. Jpn J Pharmacol. 1997 Feb;73(2):105-12.
REF 64The ghrelin pentapeptide inhibits the secretion of pancreatic juice in rats. J Physiol Pharmacol. 2006 Dec;57(4):691-700.
REF 65Melatonin as modulator of pancreatic enzyme secretion and pancreatoprotector. J Physiol Pharmacol. 2007 Dec;58 Suppl 6:65-80.
REF 66Effects of intraduodenal administration of tarazepide on pancreatic secretion and duodenal EMG in neonatal calves. Regul Pept. 1998 Nov 30;78(1-3):113-23.
REF 67Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist. Br J Pharmacol. 1996 Apr;117(7):1558-64.
REF 68Characterization of the binding of [3H]-(+/-)-L-364,718: a new potent, nonpeptide cholecystokinin antagonist radioligand selective for peripheral receptors. Mol Pharmacol. 1986 Sep;30(3):212-7.
REF 69Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors. J Med Chem. 1991 Dec;34(12):3350-9.
REF 70Characterization of two novel cholecystokinin tetrapeptide (30-33) analogues, A-71623 and A-70874, that exhibit high potency and selectivity for cholecystokinin-A receptors. Mol Pharmacol. 1991 Mar;39(3):346-51.
REF 71Dual 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 72US patent application no. 8,748,419, Antagonists.
REF 73Distinct cholecystokinin receptors in brain and pancreas. Proc Natl Acad Sci U S A. 1980 Nov;77(11):6917-21.
REF 74Obesity Pharmacotherapy: Current Perspectives and Future Directions. Curr Cardiol Rev. 2013 February; 9(1): 33-54.
REF 75Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506.
REF 76Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger". J Med Chem. 1996 Jan 19;39(2):562-9.
REF 77Optimization 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 78Identification of a region of the N-terminal of the human CCKA receptor essential for the high affinity interaction with agonist CCK. Biochem Biophys Res Commun. 1995 Aug 24;213(3):845-52.
REF 79SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies. J Pharmacol Exp Ther. 1999 May;289(2):742-51.

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