l-1,2,3,4-Tetrahydro-8-methoxy-5-(methylthio)-2-naphthalenamine: A Potent and Selective Agonist at α1-Adrenoceptors

Article abstract of DOI:10.1021/jm00363a002

1,2,3,4-Tetrahydro-8-methoxy-5-(methylthio)-2-naphthalenamine (SKandF-89748) has been resolved into d and l enantiomers and characterized pharmacologically.The more active isomer is the l, which has the S configuration as established by single-crystal X-ray diffraction studies.This compound is a potent and selective α₁-agonist with an EC50 in the isolated perfused rabbit ear artery of 9 +/- 2 nM.In several preparations, it has shown an α₁/α₂ selectivity ratio of over 100 and will be a useful tool for characterizing receptor subtypes.