Datasheet Inhibitors / Agonists / Screening Libraries A DRUG SCREENING EXPERT

Product Name : Zatosetron maleate Catalog Number : T17285 CAS Number : 123482-23-5 Molecular Formula : C23H29ClN2O6 Molecular Weight : 464.94

Description: Zatosetron maleate is an effective and selective antagonist of the 5HT3 receptor.

Storage: 2 years -80°C in solvent; 3 years -20°C powder;

Receptor (IC50) 5HT3 receptor

In vivo Activity Zatosetron maleate inhibits the activity of A10 dopamine cells following i.v. administration (ED50=0.12 mg/kg, n=8). Acute administration of 0.1 (n=21) and 0.3 (n=5) mg/kg Zatosetron maleate in male rats, but not 0.01, 0.05, 1.0 or 10 mg/kg (n=5, 3, 6 and 4, respectively) Zatosetron maleate or saline (n=5), leads to a significant reduction in the number of spontaneously active A10 dopamine cells. Zatosetron maleate (0.1 mg/kg) administration, shows a significant decrease by 60 to 90 min (0.65±0.11, P=0.03, n=5), a larger decrease by 90 to120 min (0.53±0.08, P=0.004, n=5) and remains at this significantly decreased level from 2 to 3 h (0.50+0.05, P=0.0004, n=5). Chronic administration of 0.1 mg/kg (n=16) Zatosetron maleate, but not 0.01, 1.0 or 10 mg/kg (n=4, 8 and 7, respectively) Zatosetron maleate or saline (n=5), leads to a significant reduction in the number of spontaneously active A10 dopamine cells [2].

Reference 1. Robertson DW, et al. Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure- activity relationships. J Med Chem. 1992 Jan 24;35(2):310-9. 2. Rasmussen K, et al. The 5-HT3 receptor antagonist zatosetron decreases the number of spontaneously active A10 dopamine neurons. Eur J Pharmacol. 1991 Nov 19; 205 (1):113-6.

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