PMID: 11312913Apr 21, 2001Paper

Nonpeptide cholecystokinin-2 receptor agonists

Journal of Medicinal Chemistry
S B KalindjianN P Shankley

Abstract

In the course of structural explorations around a series of potent CCK2 receptor antagonists, it was noted that simple N-methylation of the indolic N-H in the parent molecule gave rise to behavior in vivo that was consistent with the compound acting as an agonist. Exploration in vitro confirmed this property, and it was shown that the agonist action could be blocked by the reference CCK2 receptor antagonist, L-365,260. Further examples of this type of modification were explored, and a common theme with regard to agonist behavior was uncovered. Some molecular modeling is also presented in an attempt to throw light on the nature of the ligand receptor interactions that may be giving rise to the differing properties of these, apparently, structurally similar molecules.

References

Nov 1, 1990·Journal of Medicinal Chemistry·K ShiosakiA M Nadzan
Sep 1, 1991·Journal of Medicinal Chemistry·K ShiosakiA M Nadzan
Apr 26, 1996·Journal of Medicinal Chemistry·S B KalindjianJ G Vinter
Aug 1, 1996·British Journal of Pharmacology·E A HarperJ W Black
Jun 24, 2000·Bioorganic & Medicinal Chemistry Letters·N BernadM C Pritchard

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Citations

Apr 17, 2003·Proceedings of the National Academy of Sciences of the United States of America·Alan S KopinMartin Beinborn
Apr 12, 2003·Pharmacology & Toxicology·James W Black, S Barret Kalindjian
Sep 22, 2015·Journal of Medicinal Chemistry·Peter I Dosa, Elizabeth Ambrose Amin
Dec 26, 2007·European Journal of Pharmacology·Elaine A HarperS Barrett Kalindjian
Jun 27, 2007·British Journal of Pharmacology·E A HarperS B Kalindjian
Jun 6, 2003·Medicinal Research Reviews·Rosario Herranz
Jul 4, 2006·Physiological Reviews·Marlène DufresneDaniel Fourmy
Oct 22, 2008·The Journal of Biological Chemistry·Magali FoucaudDaniel Fourmy
Jan 19, 2008·Journal of Medicinal Chemistry·Caroline M R Low, J G Vinter
Mar 5, 2004·Journal of Medicinal Chemistry·Andrea CappelliMarina Ziche

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