CARDIOTONIC AGENTS .3. A TOPOGRAPHICAL MODEL OF THE CARDIAC CAMP PHOSPHODIESTERASE RECEPTOR
- 1 January 1988
- journal article
- research article
- Vol. 33 (1) , 1-13
Abstract
Based on the pharmacophoric relationship heterocycle-phenyl-imidazole (H-P-I) and upon consideration of several potent inhibitors of cardiac cAMP phosphodiesterase, a topographical model of this receptor is proposed. The model consists of two binding sites which interact with H, two steric features, preferential rotation of P away from coplanarity with H, and a binding site for an electron-rich system (I). It is supported by molecular modeling studies and accommodates a variety of inhibitors. It also encompasses the active site of the enzyme and can distinguish cAMP from cGMP as substrates.This publication has 3 references indexed in Scilit:
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