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Binding of yohimbine stereoisomers to α‐adrenoceptors in rat liver and human platelets
Author(s) -
Ferry Nicolas,
Goodhardt Michele,
Hanoune Jacques,
Sevenet Thierry
Publication year - 1983
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1983.tb09401.x
Subject(s) - yohimbine , platelet , adrenergic receptor , pharmacology , chemistry , endocrinology , medicine , receptor , antagonist
1 Displacement of tritiated prazosin binding to rat liver plasma membranes and tritiated yohimbine human platelet membranes shows that (+)‐yohimbine, alloyohimbine and α‐yohimbine (rauwolscine) are selective α 2 ‐adrenoceptor antagonists ( K Dα1 / K Dα2 :635, 46.6 and 112 respectively) whereas corynanthine is more α 1 ‐selective ( K Dα1 / K Dα2 :0.036). 2 11‐Methoxy derivatives of α‐yohimbine and epi‐α‐yohimbine are very weak α‐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 α‐adrenoceptor, the carboxymethyl group being important for the α 1 /α 2 specificity of the molecule.