Metaphit, a receptor acylator, inactivates cocaine binding sites in striatum and antagonizes cocaine-induced locomotor stimulation in rodents.
The PCP analog metaphit, a proposed PCP receptor acylator, produced a concentration-dependent loss of the number of high-affinity [3H]cocaine binding sites in rodent striatum. In addition, 24 h after administration of metaphit, a dose of 25 mg/kg of cocaine was not effective in stimulating locomotor behavior of rodents. The results suggest that metaphit antagonizes cocaine-induced locomotor stimulation by acylating cocaine binding sites on dopaminergic nerve terminals.
D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D003042:Cocaine / Q000037:antagonists & inhibitors* / Q000378:metabolism; D003342:Corpus Striatum / Q000187:drug effects* / Q000378:metabolism; D005260:Female; D008297:Male; D009043:Motor Activity / Q000187:drug effects*; D010622:Phencyclidine / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains
C044705:metaphit; D003042:Cocaine; D010622:Phencyclidine