PT  - JOURNAL ARTICLE
AU  - P W Erhardt
AU  - A A Hagedorn, 3rd
AU  - M Sabio
TI  - Cardiotonic agents. 3. A topographical model of the cardiac cAMP phosphodiesterase receptor.
DP  - 1988 Jan 01
TA  - Molecular Pharmacology
PG  - 1--13
VI  - 33
IP  - 1
4099  - http://molpharm.aspetjournals.org/content/33/1/1.short
4100  - http://molpharm.aspetjournals.org/content/33/1/1.full
SO  - Mol Pharmacol1988 Jan 01; 33
AB  - 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.