Target Information
Target General Infomation | |||||
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Target ID |
T28330
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Former ID |
TTDC00082
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Target Name |
Cholecystokinin receptor type A
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Gene Name |
CCKAR
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Synonyms |
CCK-A receptor; CCK-AR; CCKAR
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Target Type |
Discontinued
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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] | |||||
Gallstone prophylaxis; Obesity [ICD9: 278; ICD10: E66] | |||||
Gastrointestinal disease [ICD10: K00-K93] | |||||
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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T28330
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UniProt ID | |||||
Sequence |
MDVVDSLLVNGSNITPPCELGLENETLFCLDQPRPSKEWQPAVQILLYSLIFLLSVLGNT
LVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYF MGTSVSVSTFNLVAISLERYGAICKPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYS NLVPFTKNNNQTANMCRFLLPNDVMQQSWHTFLLLILFLIPGIVMMVAYGLISLELYQGI KFEASQKKSAKERKPSTTSSGKYEDSDGCYLQKTRPPRKLELRQLSTGSSSRANRIRSNS SAANLMAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTASAERRLSGTPISFILLLSY TSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGARGEVGEEEEGGTTGASLSRFSYSH MSASVPPQ |
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Drugs and Mode of Action | |||||
Drug(s) | Dexloxiglumide | Drug Info | Phase 2 | Pancreatic disease | [551871] |
A-71378 | Drug Info | Preclinical | Obesity | [536122], [543286] | |
A-74498 | Drug Info | Preclinical | Obesity | [536122] | |
AR-R-1589 | Drug Info | Preclinical | Obesity; Eating disorders | [536122] | |
FPL-14294 | Drug Info | Preclinical | Obesity | [536122] | |
GG-8573 | Drug Info | Preclinical | Gallstone prophylaxis; Obesity | [536122] | |
PD-170292 | Drug Info | Preclinical | Obesity | [536122] | |
CE-326597 | Drug Info | Discontinued in Phase 2 | Obesity | [522138] | |
GI 181771 | Drug Info | Discontinued in Phase 2 | Obesity | [547133] | |
Lintitript | Drug Info | Discontinued in Phase 2 | Pancreatic cancer; Obesity | [543282], [545822] | |
Pranazepide | Drug Info | Discontinued in Phase 2 | Pancreatic disease | [543265], [545379] | |
Tarazepide | Drug Info | Discontinued in Phase 2 | Gastrointestinal disease | [525387] | |
SR-146131 | Drug Info | Discontinued in Phase 1 | Obesity | [543241], [546817] | |
SSR-125180 | Drug Info | Discontinued in Phase 1 | Obesity | [547405] | |
T-0632 | Drug Info | Discontinued in Phase 1 | Pancreatic disease | [543275], [546379] | |
UCL-2000 and butabindide | Drug Info | Discontinued in Phase 1 | Obesity | [551995] | |
A-70276 | Drug Info | Terminated | Gastrointestinal disease | [545481] | |
A-71623 | Drug Info | Terminated | Obesity | [543203], [545483] | |
CR-1795 | Drug Info | Terminated | Discovery agent | [546448] | |
FR-208419 | Drug Info | Terminated | Dyspepsia | [546824] | |
GI-248573 | Drug Info | Terminated | Bladder disease | [546536] | |
IQM-95333 | Drug Info | Terminated | Discovery agent | [546593] | |
Lorglumide | Drug Info | Terminated | Pancreatic disease | [543283], [544685] | |
PD-135666 | Drug Info | Terminated | Discovery agent | [543294], [546092] | |
SNF-9007 | Drug Info | Terminated | Discovery agent | [546204] | |
SR-27950 | Drug Info | Terminated | Eating disorder | [544831] | |
Inhibitor | 1-(3,3-Diphenyl-allyl)-3-m-tolyl-urea | Drug Info | [527275] | ||
1-(4-Chloro-phenyl)-3-(3,3-diphenyl-allyl)-urea | Drug Info | [527275] | |||
1-(4-Chloro-phenyl)-3-(3-pentyl-oct-2-enyl)-urea | Drug Info | [527275] | |||
3,4-Dichloro-N-(3,3-diphenyl-allyl)-benzamide | Drug Info | [527275] | |||
Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe | Drug Info | [551252] | |||
Asp-Tyr(SO3H)-Met-Gly-Trp-Met-Asp-Phe-NH2 | Drug Info | [533338] | |||
Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 | Drug Info | [532617] | |||
Boc-cyclo-(Glu-Tyr-Nle-D-Lys)-Trp-Nle-Asp-Phe-NH2 | Drug Info | [533338] | |||
Boc-D-Glu-Tyr(SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2 | Drug Info | [533338] | |||
Boc-D-Glu-Tyr(SO3H)-Nle-D-Nle-Trp-Nle-Asp-Phe-NH2 | Drug Info | [533338] | |||
Boc-Glu-Tyr(SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2 | Drug Info | [533338] | |||
Boc-Tyr(SO3H)-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [533338] | |||
CR-1795 | Drug Info | [551253] | |||
CR-2345 | Drug Info | [551253] | |||
Dexloxiglumide | Drug Info | [532711] | |||
FR-175985 | Drug Info | [551329] | |||
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-Boc | Drug Info | [528058] | |||
H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H | Drug Info | [528606] | |||
IQM-95333 | Drug Info | [534494] | |||
L-708474 | Drug Info | [533911] | |||
L-740093 | Drug Info | [551292] | |||
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-140547 | Drug Info | [551254] | |||
PD-140548 | Drug Info | [551254] | |||
PD-140723 | Drug Info | [551254] | |||
Pranazepide | Drug Info | [551329] | |||
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-NMeNle-Asp-Phe-NH2 | Drug Info | [528193] | |||
Tyr-D-Nle-Gly-Trp-Nle-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] | |||
VL-0395 | Drug Info | [530208] | |||
VL-0494 | Drug Info | [528737] | |||
VL-0699 | Drug Info | [528132] | |||
VL-1499 | Drug Info | [530208] | |||
VL-2799 | Drug Info | [529998] | |||
Antagonist | 2-NAP | Drug Info | [528483] | ||
Asperlicin | Drug Info | [536549] | |||
CI-1015 | Drug Info | [534543] | |||
Devazepide | Drug Info | [536549] | |||
IQM-97423 | Drug Info | [527185] | |||
JNJ-17156516 | Drug Info | [528980] | |||
KSG-504 | Drug Info | [534164] | |||
L-736380 | Drug Info | [534125] | |||
Lintitript | Drug Info | [535989], [536755] | |||
Lorglumide | Drug Info | [538145] | |||
Loxiglumide | Drug Info | [535619] | |||
PD-135158 | Drug Info | [530383] | |||
proglumide | Drug Info | [533453] | |||
SC-50998 | Drug Info | [543960] | |||
T-0632 | Drug Info | [534344] | |||
Tarazepide | Drug Info | [536339], [536595], [538151] | |||
TP-680 | Drug Info | [534172] | |||
[3H]devazepide | Drug Info | [533408] | |||
Modulator | A-70276 | Drug Info | [528964] | ||
A-71623 | Drug Info | [528494] | |||
FR-208419 | Drug Info | [525711] | |||
GI-248573 | Drug Info | [550839] | |||
SR-27950 | Drug Info | [543960] | |||
Agonist | A-71378 | Drug Info | [536122] | ||
A-74498 | Drug Info | [536122] | |||
AR-R-1589 | Drug Info | [536122] | |||
CCK-33 | Drug Info | [533534] | |||
CCK-8 | Drug Info | [530383] | |||
CE-326597 | Drug Info | [544295] | |||
FPL-14294 | Drug Info | [536122] | |||
GG-8573 | Drug Info | [536122] | |||
GI 181771 | Drug Info | [535784] | |||
Glaxo-11p | Drug Info | [534086] | |||
GW-5823 | Drug Info | [534449] | |||
JMV180 | Drug Info | [533681] | |||
PD-170292 | Drug Info | [536122] | |||
SR-146131 | Drug Info | [525475] | |||
SSR-125180 | Drug Info | [550839] | |||
UCL-2000 and butabindide | Drug Info | [536122] | |||
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 522138 | ClinicalTrials.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 525387 | Cholecystokinin receptor-1 mediates the inhibitory effects of exogenous cholecystokinin octapeptide on cellular morphine dependence. BMC Neurosci. 2012 Jun 8;13:63. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 543203 | (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 543241 | (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 543265 | (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 543275 | (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 543282 | (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 543283 | (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 543286 | (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 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 544685 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000580) | ||||
Ref 544831 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001260) | ||||
Ref 545379 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003071) | ||||
Ref 545481 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003433) | ||||
Ref 545483 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003438) | ||||
Ref 545822 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004912) | ||||
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 546379 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007781) | ||||
Ref 546448 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008170) | ||||
Ref 546536 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008844) | ||||
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 546817 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010439) | ||||
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 547133 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013294) | ||||
Ref 547405 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015967) | ||||
Ref 525475 | SR146131: 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. | ||||
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 527185 | Pharmacological 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 527275 | J Med Chem. 1992 Mar 20;35(6):1042-9.Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718. | ||||
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 528132 | J 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 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 528483 | Unexpected 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 528494 | Characterization 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 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 528737 | Bioorg 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 528964 | Cholecystokinin 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 528980 | 3-[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 529998 | Bioorg 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 530208 | Bioorg 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 530383 | Development 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 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 532711 | J Med Chem. 1989 Feb;32(2):445-9.Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue. | ||||
Ref 533338 | J 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 533408 | Characterization 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 533453 | Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung. 1987 Nov;37(11):1265-8. | ||||
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 533534 | Distinct cholecystokinin receptors in brain and pancreas. Proc Natl Acad Sci U S A. 1980 Nov;77(11):6917-21. | ||||
Ref 533681 | Identification 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 533911 | J 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 534086 | Discovery 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 534125 | Controlled 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 534164 | Effects of KSG-504, a new CCK-A receptor antagonist, on gallbladder and gastrointestinal functions. Nihon Yakurigaku Zasshi. 1996 Jan;107(1):33-44. | ||||
Ref 534172 | Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist. Br J Pharmacol. 1996 Apr;117(7):1558-64. | ||||
Ref 534344 | Effect of T-0632, a cholecystokininA receptor antagonist, on experimental acute pancreatitis. Jpn J Pharmacol. 1997 Feb;73(2):105-12. | ||||
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 535619 | Role of CCK(A) receptors in postprandial lower esophageal sphincter function in morbidly obese subjects. Dig Dis Sci. 2002 Nov;47(11):2531-7. | ||||
Ref 535989 | A novel role for cholecystokinin: regulation of mesenteric vascular resistance. Regul Pept. 2004 Sep 15;121(1-3):145-53. | ||||
Ref 536122 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | ||||
Ref 536339 | The ghrelin pentapeptide inhibits the secretion of pancreatic juice in rats. J Physiol Pharmacol. 2006 Dec;57(4):691-700. | ||||
Ref 536549 | Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19. | ||||
Ref 536595 | Melatonin as modulator of pancreatic enzyme secretion and pancreatoprotector. J Physiol Pharmacol. 2007 Dec;58 Suppl 6:65-80. | ||||
Ref 536634 | Role of CCK and potential utility of CCK1 receptor antagonism in the treatment of pancreatitis induced by biliary tract obstruction. Br J Pharmacol. 2008 Apr;153(8):1650-8. Epub 2008 Feb 25. | ||||
Ref 536639 | Regulation of fat-stimulated neurotensin secretion in healthy subjects. J Clin Endocrinol Metab. 2008 May;93(5):1964-70. Epub 2008 Feb 26. | ||||
Ref 536755 | A 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 537400 | Prokinetic drugs for feed intolerance in critical illness: current and potential therapies. Crit Care Resusc. 2009 Jun;11(2):132-43. | ||||
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