Comparison of Displacemental Potencies of Terazosin Enantiomers for .ALPHA.1-Adrenoceptor Subtypes.

Abstract
The present study was designed to assess displacemental potencies of terazosin and its isomers for alpha 1 High and alpha 1 Low adrenoceptor subtypes in rat brain, heart, bovine prostate and canine aorta using a radioligand binding assay method. Although no significant difference in pKi values of each terazosin isomer for alpha 1 High in canine aorta and rat brain were observed, the displacemental potency of (S-)terazosin for those in rat heart and bovine prostate was stronger than that of (R+)isomer (p < 0.01). On the other hand, only in alpha 1 Low subtypes of bovine prostate was stronger displacemental potency of (S-)terazosin than (R+)isomer (p < 0.05) observed. Thus, these results imply that there is a different affinity between (S-)terazosin and (R+)isomer on the alpha 1 High in bovine prostate and rat heart and alpha 1 Low in bovine prostate.

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