Garcia-Carceles, Javier; Decara, Juan M.; Vazquez-Villa, Henar; Rodriguez, Ramon; Codesido, Eva; Cruces, Jacobo; Brea, Jose; Loza, Maria I.; Alen, Francisco; Botta, Joaquin; McCormick, Peter J.; Ballesteros, Juan A.; Benhamu, Bellinda; Rodriguez de Fonseca, Fernando; Lopez-Rodriguez, Maria L. published the artcile< A Positive Allosteric Modulator of the Serotonin 5-HT2C Receptor for Obesity>, Product Details of C4H5N3, the main research area is anorectic serotonin receptor modulator preparation obesity benzylindolyl methylpyridinamine.
The 5-HT2CR agonist lorcaserin, clin. approved for the treatment of obesity, causes important side effects mainly related to subtype selectivity. In the search for 5-HT2CR allosteric modulators as safer antiobesity drugs, a chem. library from Vivia Biotech was screened using ExviTech platform. Structural modifications of identified hit VA240 in synthesized analogs 6-41 afforded compound 11 (N-[(1-benzyl-1H-indol-3-yl)methyl]pyridin-3-amine, VA012), which exhibited dose-dependent enhancement of serotonin efficacy, no significant off-target activities, and low binding competition with serotonin or other orthosteric ligands. PAM 11 was very active in feeding inhibition in rodents, an effect that was not related to the activation of 5-HT2AR. A combination of 11 with the SSRI sertraline increased the anorectic effect. Subchronic administration of 11 reduced food intake and body weight gain without causing CNS-related malaise. The behavior of compound 11 identified in this work supports the interest of a serotonin 5-HT2CR PAM as a promising therapeutic approach for obesity.
Journal of Medicinal Chemistry published new progress about 5-HT2C receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Product Details of C4H5N3.
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem