β-Chlornaltrexamine
β-Chlornaltrexamine (β-CNA) is a non-selective irreversible antagonist of the μ-opioid receptor (MOR), the δ-opioid receptor (DOR), and the κ-opioid receptor (KOR), which forms a covalent bond to the binding sites of these receptors and has ultra-long-lasting opioid antagonist effects. Although it is predominantly antagonistic, β-CNA also shows some irreversible mixed agonist–antagonist activity at the MOR and KOR and some associated analgesic effects. Its alkylating group is a bis(chloroalkyl)amino-residue similar to that of the nitrogen mustards. The drug was first described by 1978. It should not be confused with its epimer and related drug α-chlornaltrexamine (α-CNA), which is likewise predominantly an irreversible antagonist of the opioid receptors but also shows some irreversible mixed agonist–antagonist activity. See also * Naltrexamine, an opioid receptor antagonist and the parent compound * β-Funaltrexamine, a related irreversible opioid receptor antag ...
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Chloroxymorphamine
Chloroxymorphamine is an opioid and a derivative of oxymorphone which binds irreversibly as an agonist to the μ-opioid receptor. See also * β-Chlornaltrexamine * Naloxazone * Oxymorphazone Oxymorphazone is an opioid analgesic drug related to oxymorphone. Oxymorphazone is a potent and long acting μ-opioid agonist which binds irreversibly to the receptor, forming a covalent bond which prevents it from detaching once bound. This gi ... References Opioids Alkylating agents Mu-opioid receptor agonists Irreversible agonists Nitrogen mustards Chloroethyl compounds Tertiary alcohols Cyclohexanols {{analgesic-stub ...
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