Article
Dual agonistic and antagonistic property of nonpeptide angiotensin AT1 ligands: susceptibility to receptor mutations.
Molecular pharmacology - 1 Feb 1997
Perlman S, Costa-Neto C M, Miyakawa A A, Schambye H T, Hjorth S A, Paiva A C, Rivero R A, Greenlee W J, Schwartz T W
Abstract excerpt
Two nonpeptide ligands that differ chemically by only a single methyl group but have agonistic (L-162,782) and antagonistic (L-162,389) properties in vivo were characterized on the cloned angiotensin AT1 receptor. Both compounds bound with high affinity (K(I) = 8 and 28 nM, respectively) to the AT1 receptor expressed transiently in COS-7 cells as determined in radioligand competition assays. L-162,782 acted as a...
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