[Irreversible action of the opioid agonist alpha-CAM and its reaction with SH groups at opioid receptor binding sites].
7 alpha-Bis (beta-chloroethyl)amino-methyl-6,14-endoethenotetrahydrooripavine (alpha-CAM) was found to bind to opioid receptors irreversibly and react directly with sulfhydryl (SH) groups in P2 preparations of rat brain. The P2 preparations were pretreated as follows: protection of the SH groups at the opioid receptor binding sites by morphine or etorphine, and inactivation of the SH groups outside the binding sites by N-ethylmaleimide (NEM), followed by removal of the morphine or etorphine by washing. alpha-CAM was still able to bind the pretreated P2 preparations in an irreversible manner. The results indicate that the formation of covalent bonds between alpha-CAM and the SH groups of opioid receptor binding sites is possibly one of the biochemical mechanisms of the irreversible action of alpha-CAM.
Li
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Li
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Jin
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Yu
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Liu
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D000700:Analgesics; D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D001921:Brain / Q000378:metabolism*; D005033:Ethylmaleimide / Q000494:pharmacology; D005260:Female; D008297:Male; D051381:Rats; D011957:Receptors, Opioid / Q000187:drug effects*; D013438:Sulfhydryl Compounds / Q000378:metabolism; D013797:Thebaine / Q000031:analogs & derivatives* / Q000494:pharmacology
D000700:Analgesics; D011957:Receptors, Opioid; D013438:Sulfhydryl Compounds; C061548:7-bis(beta-chloroethyl)aminomethyl-6,14-endoethenotetrahydrooripavine; D013797:Thebaine; D005033:Ethylmaleimide