TM-38837 is a small molecule
inverse agonist
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist.
A neutral antagonist has no activity in the absence of an agonist or inverse agon ...
/
antagonist
An antagonist is a character in a story who is presented as the chief foe of the protagonist.
Etymology
The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ...
of the
CB1 cannabinoid receptor, with peripheral selectivity. It is being developed for the treatment of
obesity
Obesity is a medical condition, sometimes considered a disease, in which excess body fat has accumulated to such an extent that it may negatively affect health. People are classified as obese when their body mass index (BMI)—a person's we ...
and metabolic disorders by 7TM Pharma. The company has announced
phase I Phase 1, Phase I or Phase One may refer to:
Media
* Marvel Cinematic Universe: Phase One, six American superhero films from 2008–2012
* ''Phase One'' (Art Ensemble of Chicago album), 1971
* ''Phase One'' (Saga album), 1998
* ''Phase One'', r ...
clinical trials.
TM-38837 is among the first of a new generation of
cannabinoid receptor antagonist designed to avoid the
central nervous system
The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain and spinal cord. The CNS is so named because the brain integrates the received information and coordinates and influences the activity of all par ...
liabilities of the first generation CB
1 receptor antagonists such as
rimonabant
Rimonabant (also known as SR141716; trade names Acomplia, Zimulti) is an anorectic antiobesity drug that was first approved in Europe in 2006 but was withdrawn worldwide in 2008 due to serious psychiatric side effects; it was never approved in t ...
.
See also
*
AM-6545
AM-6545 is a drug which acts as a peripherally selective silent antagonist for the CB1 receptor, and was developed for the treatment of obesity. Other cannabinoid antagonists such as rimonabant have been marketed for this application, but have s ...
References
External links
Experimental obesity drug avoids brain effects that troubled predecessors press release
Anorectics
CB1 receptor antagonists
Peripherally selective drugs
Alkyne derivatives
Thiophenes
Chloroarenes
Trifluoromethyl compounds
Pyrazoles
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