Conformational analysis of the calcium-antagonist gallopamil

Biochemical Pharmacology
R BrasseurW J Malaisse

Abstract

Conformational analysis of gallopamil was performed in order to gain insight into the molecular determinant of its calcium-antagonistic property. Whereas the neutral form of gallopamil was characterized by a single, largely predominant configuration, the protonated form of the drugs yielded several conformers, some of which were characterized by a readily accessible ionized site. The capacity of gallopamil to inhibit ionophore-mediated calcium translocation in a two-phase bulk system was inversely related to the pH of the aqueous phase. These findings indicate that the capacity of gallopamil to interfere with the transport of cations is critically dependent on the availability of a protonated configuration of the drug.

References

Aug 15, 1977·Experientia·W J MalaisseG Somers
Apr 1, 1974·Proceedings of the National Academy of Sciences of the United States of America·E RalstonR Walter
May 1, 1982·Proceedings of the National Academy of Sciences of the United States of America·R BrasseurJ M Ruysschaert

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Citations

Jan 1, 1988·Annals of the New York Academy of Sciences·W J Malaisse
Oct 11, 2005·Bioorganic & Medicinal Chemistry Letters·Anamika Awasthi, Arpita Yadav
Nov 1, 1985·Biochemical Pharmacology·M DeleersR Brasseur
Nov 1, 1983·Pharmacological Research Communications·R Brasseur, M Deleers

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