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5-HT3 antagonist 5

  Cat. No.:  DC60308   Featured
Chemical Structure
901599-43-7
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Field of application
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].
Cas No.: 901599-43-7
Chemical Name: 5-HT3 antagonist 5
Synonyms: 2-Quinoxalinecarboxamide, N-(4-methoxyphenyl)-;WAY-327157;N-(4-Methoxyphenyl)-2-quinoxalinecarboxamide (ACI);5-HT3 antagonist 5
SMILES: O=C(C1C=NC2C(=CC=CC=2)N=1)NC1C=CC(OC)=CC=1
Formula: C16H13N3O2
M.Wt: 279.293323278427
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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].
Target: 5-HT3 Receptor
In Vivo: 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.
In Vitro: 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].
References: [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.
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