Description
Zatosetron maleate is a potent and selective 5HT3 receptor antagonist.
Product information
CAS Number: 123482-23-5
Molecular Weight: 464.94
Formula: C23H29ClN2O6
Chemical Name: (2Z)-but-2-enedioic acid; 5-chloro-2,2-dimethyl-N-[(1R,3S,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]-2,3-dihydro-1-benzofuran-7-carboxamide
Smiles: CN1[C@@H]2C[C@H](C[C@H]1CC2)NC(=O)C1=CC(Cl)=CC2CC(C)(C)OC=21.OC(=O)/C=C\C(O)=O
InChiKey: HAFQATMFFHYNPN-QRPZPOMXSA-N
InChi: InChI=1S/C19H25ClN2O2.C4H4O4/c1-19(2)10-11-6-12(20)7-16(17(11)24-19)18(23)21-13-8-14-4-5-15(9-13)22(14)3;5-3(6)1-2-4(7)8/h6-7,13-15H,4-5,8-10H2,1-3H3,(H,21,23);1-2H,(H,5,6)(H,7,8)/b;2-1-/t13-,14+,15-;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vivo:
Acute administration of 0.1 (n=21) and 0.3 (n=5) mg/kg Zatosetron maleate (Zatosetron) 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. The number of spontaneously active A10 dopamine cells is not significantly different from 30 to 60 min post i.p. 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). Single-unit recordings show that Zatosetron maleate inhibits the activity of A10 dopamine cells following i.v. administration (ED50=0.12 mg/kg, n=8). 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.
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