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Irreversible action of the opioid agonist alpha-CAM and its reaction with SH groups at opioid receptor binding sites

  
@article{APS5341,
	author = {Jian-guo Li and Ling-yuan Li and Cai-ying Ye and Yin-chang Jin and Xin-hong Yu},
	title = {Irreversible action of the opioid agonist alpha-CAM and its reaction with SH groups at opioid receptor binding sites},
	journal = {Acta Pharmacologica Sinica},
	volume = {10},
	number = {2},
	year = {2016},
	keywords = {},
	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.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/5341}
}