Description
A 5-HT2C receptor antagonist; binds to 5-HT2C receptors (Ki = 3.8 nM for the recombinant human receptor) and is selective for 5-HT2C receptors over 5-HT2A and 5-HT2B receptors (Kis = 1,122.02 and 812.83 nM, respectively), as well as a panel of additional neurotransmitter receptors and ion channels (Kis = ≥316.23 nM for all); inhibits 5-HT-induced increases in the extracellular media acidification rate of CHO-K1 cells expressing human 5-HT2C receptors (pA2 = 8.1); increases food intake and weight gain in rats at 2 mg/kg; increases the time spent in the light compartment in the light-dark exploration test in mice at 2 mg/kg; reduces prepulse inhibition of the startle reflex in mice at 1 mg/kg
Formal name: N-[5-[5-(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)-1-oxopentyl]-2,4-dimethoxyphenyl]-4-(trifluoromethyl)-benzenesulfonamide, monohydrochloride
Synonyms:
Molecular weight: 649.1
CAS: 187397-18-8
Purity: ≥98%
Formulation: A solid
