Differing stereospecificities distinguish opiate receptor subtypes

摘要: Paired stereoisomers of compounds active at the proposed mu, kappa and sigma classes opiate receptors display differing stereoselectivity patterns receptor subtypes. The (-) isomers cyclazocine SKF-10047 are far more potent than (+) as displacers [3H]dihydromorphine from receptors. However, only moderately displacing [3H]ethylketocyclazocine in an assay controlled for radioligand binding to mu receptors, similar potency displacement [3H]phencyclidine (PCP) At sigma/PCP receptor, ketamine proved four times ketamine, while dioxalan derivative dexoxadrol is its nearly inactive enantiomer levoxadrol. results agreement with those behavioral studies. Stereospecificity may provide support concept subclasses biochemically distinct entities.