Gemazocine (R-15,497), also known as cyclogemine, is a non-selective
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 ...
of the
benzomorphan
Benzomorphan is a chemical compound that is the base for a series of drugs which variably act on the opioid kappa and sigma receptors, including the following compounds:
* 5,9-DEHB
* 8-CAC
* Alazocine
* Anazocine
* Bremazocine
* Butinazocine ...
class.
It may have
partial agonist
In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic e ...
properties at some of the
opioid receptor
Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostatin ...
s, such as at the kappa receptor (as it induces dysphoric effects in humans), but seems to be generally
antagonistic in its actions.
References
Benzomorphans
Kappa-opioid receptor agonists
Mu-opioid receptor antagonists
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