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Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
Protection studies in mice suggest that CNA mediates its narcotic antagonist effects by interacting with the same receptors that are occupied by naloxone. Expand
Chloroxymorphamine, and opioid receptor site-directed alkylating agent having narcotic agonist activity.
Chloroxymorphamine, the 6beta-N,N-bis(2-chloroethyl) derivative of oxymorphone, is a potent nonequilibrium narcotic agonist in the longitudinal muscle preparation of guinea pig ileum. TheExpand
Pharmacological studies with an alkylating narcotic agonist, chloroxymorphamine, and antagonist, chlornaltrexamine.
The data suggest that CNA and COA alkylate the opioid receptors to produce antagonist and agonist-antagonist effects, respectively. Expand
Postmortem Stability of Dopamine‐Sensitive Adenylate Cyclase, Guanylate Cyclase, ATPase, and GTPase in Rat Striatum
The results are not consistent with an earlier suggestion that there is a postmortem degradation of the enzyme itself, and other kinetic parameters of dopamine‐sensitive adenylate cyclase can also be measured independently of postmortem changes. Expand
Isolation of selective 3H-chlornaltrexamine-bound complexes, possible opioid receptor components in brains of mice.
The nonequilibrium narcotic antagonist, chlornaltrexamine (CNA) was used to bind selectively and covalently pioid specific sites on brain membrane preparations to find one of these specific [ 3 H]CNA complexes elutes at the elution volume of the column and is dialyzable. Expand