5-HT3 antagonist 5

5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice[1].

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

5-HT3 Receptor

5-HT3 antagonist 5 (compound 4c) exhibits 5-HT3 receptor antagonisms in longitudinal muscle myenteric plexus preparation from guinea pig ileum against 5-HT3 agonist, 2-methyl-5-HT, with pA2 value of 5[1].

5-HT3 antagonist 5 (compound 4c) (1 mg/kg; i.p.; single dose) decreases the duration of immobility and shows anti-depressant effect in FST mice[1]. Animal Model: Swiss albino mice (23 ± 2 g)[1] Dosage: 1 mg/kg Administration: Intraperitoneal injection; single dose; locomotor scores tested 10 min after administration Result: Reduced the duration of immobility as compared to the vehicle-treated (control) group. Showed no effect on the locomotion of mice as observed in spontaneous locomotor activity.

[1]. Mahesh R, et al. Design, synthesis and structure-activity relationship of novel quinoxalin-2-carboxamides as 5-HT3 receptor antagonists for the management of depression. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6773-6.