PMID: 9237427May 1, 1997Paper

Conformational flexibility of serotonin1A receptor ligands from crystallographic data. Updated model of the receptor pharmacophore

Archiv der Pharmazie
Z ChilmonczykM Gdaniec


Preparation and affinity to 5-HT1A and 5-HT2A receptors of new buspirone analogues 7-17 are reported. The compounds possess high to low affinity to 5-HT1A and moderate to low to 5-HT2A receptors. The crystal structures have been determined for compounds 11, 12, 13, and 14. For low affinity ligand (15) of 5-HT1A receptor conformational analysis was performed and compared with similar analyses performed for know high (buspirone 1) and very high (WY-48,723 2) affinity ligands of the receptor. Structure-activity relationship is discussed for the affinity to 5-HT1A receptor. A three-point pharmacophore explaining interactions of buspirone-like molecules with the receptor binding site is proposed.


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Jan 1, 1991·Psychopharmacology·R HensmanJ F Deakin
Feb 1, 1986·Japanese Journal of Pharmacology·I Shimizu, N Toda
Apr 1, 1988·Pharmacology, Biochemistry, and Behavior·J F Deakin
Nov 1, 1986·Journal of Medicinal Chemistry·R A GlennonJ D McKenney
May 20, 1983·European Journal of Pharmacology·D N Middlemiss, J R Fozard
Mar 1, 1949·Journal of the American Chemical Society·S C HARVEY

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