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Cholecystokinin (CCK) Receptor Antagonists

Autor: R. M. Freidinger, M. G. Bock, S. B. Freedman, V. G. Matassa

Publikováno v: Current Pharmaceutical Design. 1:279-294

Receptor antagonists of the endogenous peptide CCK have potential therapeutic utility for the treatment of a number of gastrointestinal and central nervous system disorders. This article reviews recent developments in the general area of CCK receptor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7cfb57afcfd4a3dc40e9692910e72e81
https://doi.org/10.2174/1381612801666220918150825

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1-(((7,7-Dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo[2.2.1]heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperazine (L-368,899): An Orally Bioavailable, Non-Peptide Oxytocin Antagonist with Potential Utility for Managing Preterm Labor

Autor: P D, Williams, P S, Anderson, R G, Ball, M G, Bock, L, Carroll, S H, Chiu, B V, Clineschmidt, J C, Culberson, J M, Erb, B E, Evans

Publikováno v: Journal of Medicinal Chemistry. 37:565-571

Modifications to the previously reported spiroindenylpiperidine camphor-sulfonamide oxytocin (OT) antagonist L-366,509 have produced a new series of o-tolylpiperazine (TP) camphor-sulfonamides. A number of analogues in the TP series that incorporate

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cbee35be16d415185dfe2956648b8b43
https://doi.org/10.1021/jm00031a004

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Progress in the development of oxytocin antagonists for use in preterm labor

Autor: P D, Williams, M G, Bock, B E, Evans, R M, Freidinger, D J, Pettibone

Publikováno v: Advances in experimental medicine and biology. 449

There is currently a need for new therapeutic agents for treating preterm labor which could offer improved safety and efficacy beyond what has been achieved with the widely employed beta-mimetics. In this regard, the longstanding hypothesis of oxytoc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::648356078258bdc2868e5825097cfbe0
https://pubmed.ncbi.nlm.nih.gov/10026841

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Progress in the development of oxytocin antagonists for use in preterm labor

Autor: D J, Pettibone, M, Guidotti, C M, Harrell, J R, Jasper, E V, Lis, J A, O'Brien, D R, Reiss, C J, Woyden, M G, Bock, B E, Evans

Publikováno v: Advances in experimental medicine and biology. 395

From a targeted screening effort and medicinal chemistry program, L-368,899 was selected as the first orally-active oxytocin (OT) antagonist to enter clinical trials. In animal studies, L-368,899 was shown to be a potent and selective OT antagonist a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::7bb48ac51478f41355019368a957d0e0
https://pubmed.ncbi.nlm.nih.gov/8714024

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Development of 1,4-benzodiazepine cholecystokinin type B antagonists

Autor: M G, Bock, R M, DiPardo, B E, Evans, K E, Rittle, W L, Whitter, V M, Garsky, K F, Gilbert, J L, Leighton, K L, Carson, E C, Mellin

Publikováno v: Journal of medicinal chemistry. 36(26)

A series of 3-(arylureido)-5-phenyl-1,4-benzodiazepines, nonpeptidal antagonists of the peptide hormone cholecystokinin (CCK), are described. Derived by reasoned modification of the CCK-A selective 3-carboxamido-1,4-benzodiazepine, MK-329, this paper

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0aedb47e6d5ddb3fdbefec3bd6fac16
https://pubmed.ncbi.nlm.nih.gov/8277510

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Nanomolar-affinity, non-peptide oxytocin receptor antagonists

Autor: B E, Evans, G F, Lundell, K F, Gilbert, M G, Bock, K E, Rittle, L A, Carroll, P D, Williams, J M, Pawluczyk, J L, Leighton, M B, Young

Publikováno v: Journal of medicinal chemistry. 36(25)

Non-peptide antagonists of the peptide hormone oxytocin (OT) with nanomolar OT receptor affinities are described. These compounds incorporate novel amido- and amidoalkylcamphor variations to the lead structure L-366,509 (1) to achieve receptor affini

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3adb35f406f6b71bca5c35af1603733
https://pubmed.ncbi.nlm.nih.gov/8258821

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Antagonism of oxytocin in rats and pregnant rhesus monkeys by the novel cyclic hexapeptides, L-366,682 and L-366,948

Autor: B V, Clineschmidt, D J, Pettibone, D R, Reiss, E V, Lis, G J, Haluska, M J, Novy, M J, Cook, M A, Cukierski, M J, Kaufman, M G, Bock

Publikováno v: The Journal of pharmacology and experimental therapeutics. 256(3)

Two cyclic hexapeptides unrelated in chemical structure to oxytocin (OT) were shown in vivo to be antagonists of the contractile action of OT on the uterus. In anesthetized rats challenged with OT (1 micrograms/kg) administered as an i.v. bolus, L-36

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::3bc80ee4c24aa903d6788c559ded54ee
https://pubmed.ncbi.nlm.nih.gov/2005582

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