Binding of yohimbine stereoisomers to alpha-adrenoceptors in rat liver and human platelets

1--Displacement of tritiated prazosin binding to rat liver plasma membranes and tritiated yohimbine human platelet membranes shows that (+)-yohimbine, alloyohimbine and alpha-yohimbine (rauwolscine) are selective alpha 2-adrenoceptor antagonists (KD alpha 1/KD alpha 2:635, 46.6 and 112 respectively) whereas corynanthine is more alpha 1-selective (KD alpha 1/KD alpha 2:0.036). 2--11-Methoxy derivatives of alpha-yohimbine and epi-alpha-yohimbine are very weak alpha-adrenoceptor blockers. 3--It is concluded that the aromatic A ring, the Nb atom, and the carboxymethyl moiety are important for the binding of yohimbine to the alpha-adrenoceptor, the carboxymethyl group being important for the alpha 1/alpha 2 specificity of the molecule.