YM-348 is an
indazole
Indazole, also called isoindazole, is a heterocyclic aromatic organic compound. This bicyclic compound consists of the fusion of benzene and pyrazole.
Indazole is an amphoteric molecule which can be protonated to an indazolium cation or deproton ...
derivative drug which acts as a potent and selective
5-HT2C receptor
Receptor may refer to:
* Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse
*Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a ...
agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...
, with an EC
50 of 1nM and 15x selectivity over
5-HT2A, although it only has moderate selectivity of 3x over the closely related
5-HT2B receptor. It has
thermogenic
Thermogenic means tending to produce heat, and the term is commonly applied to drugs which increase heat through metabolic stimulation, or to microorganisms which create heat within organic waste. Approximately all enzymatic reaction in the human b ...
and
anorectic
An anorectic or anorexic is a drug which reduces appetite, resulting in lower food consumption, leading to weight loss. By contrast, an appetite stimulant is referred to as orexigenic.
The term is (from the Greek ''ἀν-'' (an-) = "without" a ...
effects in animal studies, making it potentially useful 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 ...
.
See also
*
AL-34662
AL-34662 is an indazole derivative drug that is being developed for the treatment of glaucoma. It acts as a selective 5-HT2A receptor agonist, the same target as that of psychedelic drugs like psilocin, but unlike these drugs, AL-34662 was desi ...
*
AL-38022A
AL-38022A is an indazole derivative drug which is one of a range of similar drugs developed for scientific research and with some possible clinical applications. It acts as a potent and selective agonist for the 5-HT2 family of serotonin recept ...
*
Ro60-0175
Ro60-0175 is a drug developed by Hoffmann–La Roche, which has applications in scientific research. It acts as a potent and selective agonist for both the 5-HT2B and 5-HT2C serotonin receptor subtypes, with good selectivity over the closely re ...
*
VER-3323
VER-3323 is a drug which acts as a selective agonist for both the 5-HT2B and 5-HT2C serotonin receptor subtypes, with moderate selectivity for 5-HT2C, but relatively low affinity for 5-HT2A. It has potent anorectic effects in animal studies.
...
References
Amines
Serotonin receptor agonists
Indazoles
Benzofurans
Heterocyclic compounds with 3 rings
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