title: [Irreversible action of the opioid agonist alpha-CAM and its reaction with SH groups at opioid receptor binding sites].
abstract: 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.
authors.forename: J G
authors.initials: JG
authors.lastname: Li
authors.forename: L Y
authors.initials: LY
authors.lastname: Li
authors.forename: C Y
authors.initials: CY
authors.lastname: Ye
authors.forename: Y C
authors.initials: YC
authors.lastname: Jin
authors.forename: X H
authors.initials: XH
authors.lastname: Yu
authors.forename: M Q
authors.initials: MQ
authors.lastname: Liu
mesh_terms: 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
chemical_list: D000700:Analgesics; D011957:Receptors, Opioid; D013438:Sulfhydryl Compounds; C061548:7-bis(beta-chloroethyl)aminomethyl-6,14-endoethenotetrahydrooripavine; D013797:Thebaine; D005033:Ethylmaleimide