Interaction of dextrorotatory opioids with phencyclidine recognition sites in rat brain membranes

摘要: The potencies of several dextrorotatory opioids, including four pairs enantiomers, as inhibitors specific [3H]PCP binding to rat brain synaptic membranes has been determined. Of the compounds tested unlabeled phencyclidine (PCP) was most potent followed by (−)− cyclazocine > dextrorphan (+) ketamine (+)− SKF10,047 levorphanol dextromethorphan (−) (±) pentazocine and ethylketocyclazocine. opiate mu receptor ligands, morphine, naloxone naltrexone were virtually inactive competitors binding. Unlike stereostructural requirements for receptors where activity resides predominantly in levorotatory present results support contention that labeled recognition site may reside either or enantiomer. which defined total minus occurring presence 10μM found be a high affinity, saturable, reversible sensitive thermal degradation. These suggest certain morphian derivatives prove useful probes further investigations molecular characteristics membrane preparations.