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Datasheet Inhibitors / Agonists / Screening Libraries a DRUG SCREENING EXPERT 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. FOR RESEARCH PURPOSES ONLY. NOT FOR DIAGNOSTIC OR THERAPEUTIC USE. Information for product storage and handling is indicated on the product datasheet. Targetmol products are stable for long term under the recommended storage conditions. Our products may be shipped under different conditions as many of them are stable in the short-term at higher or even room temperatures. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, please follow the storage recommendations on the product data sheet. [email protected] | Tel: +1-781-999-4286 | www.targetmol.com.
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