l-1,2,3,4-Tetrahydro-8-methoxy-5-(methylthio)-2-naphthalenamine: a potent and selective agonist at alpha 1-adrenoceptors.
1,2,3,4-Tetrahydro-8-methoxy-5-(methylthio)-2-naphthalenamine (SK&F-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 alpha 1-agonist with an EC50 in the isolated perfused rabbit ear artery of 9 +/- 2 nM. In several preparations, it has shown an alpha 1/alpha 2 selectivity ratio of over 100 and will be a useful tool for characterizing receptor subtypes.
D000316:Adrenergic alpha-Agonists / Q000494:pharmacology*; D000818:Animals; D001158:Arteries / Q000187:drug effects / Q000378:metabolism; D003461:Crystallography; D009281:Naphthalenes / Q000494:pharmacology*; D009638:Norepinephrine / Q000378:metabolism; D011817:Rabbits; D013237:Stereoisomerism; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*; D014661:Vasoconstriction / Q000187:drug effects; D014965:X-Rays
D000316:Adrenergic alpha-Agonists; D009281:Naphthalenes; D013764:Tetrahydronaphthalenes; C039140:SK&F 89748; D009638:Norepinephrine