Chlornaltrexamine is an irreversible mixed
agonist–antagonist
In pharmacology the term agonist-antagonist or mixed agonist/antagonist is used to refer to a drug which under some conditions behaves as an agonist (a substance that fully activates the receptor that it binds to) while under other conditions, beha ...
for
μ-opioid
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioi ...
receptors, which forms a
covalent bond to the
active site. It is 22 times more potent than morphine. Its alkylating group is a bis(chloroalkyl)amino-residue similar to that of the
nitrogen mustard
Nitrogen mustards are cytotoxic organic compounds with the chloroethylamine (Cl(CH2)2NR2) functional group. Although originally produced as chemical warfare agents, they were the first chemotherapeutic agents for treatment of cancer. Nitrogen ...
s.
See also
*
Chloroxymorphamine
Chloroxymorphamine is an opioid and a derivative of oxymorphone which binds irreversibly as an agonist to the μ-opioid receptor.
See also
* Chlornaltrexamine
* Naloxazone
Naloxazone is an irreversible μ-opioid receptor antagonist which ...
, an irreversible full agonist
*
Naloxazone
Naloxazone is an irreversible μ-opioid receptor antagonist which is selective for the μ1 receptor subtype. Naloxazone produces very long lasting antagonist effects as it forms a covalent bond to the active site of the μ-opioid receptor, thus ...
, an irreversible μ-
opioid antagonist
An opioid antagonist, or opioid receptor antagonist, is a receptor antagonist that acts on one or more of the opioid receptors.
Naloxone and naltrexone are commonly used opioid antagonist drugs which are competitive antagonists that bind to the ...
*
Oxymorphazone, an irreversible full agonist
References
Alkylating agents
Organochlorides
Semisynthetic opioids
Phenols
4,5-Epoxymorphinans
Irreversible agonists
Nitrogen mustards
Chloroethyl compounds
Cyclopropyl compounds
{{analgesic-stub