1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. Zatosetron maleate

Zatosetron maleate  (Synonyms: 扎托司琼马来酸盐; LY 277359 maleate)

目录号: HY-U00234
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Zatosetron maleate 是一个有效且有选择性的 5HT3 受体拮抗剂。

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Zatosetron maleate Chemical Structure

Zatosetron maleate Chemical Structure

CAS No. : 123482-23-5

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  • 生物活性

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  • 参考文献

生物活性

Zatosetron maleate is a potent and selective 5HT3 receptor antagonist.

IC50 & Target

5-HT3 Receptor

 

体内研究
(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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

464.94

Formula

C23H29ClN2O6

CAS 号
中文名称

扎托司琼马来酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
Animal Administration
[2]

Male rats are used and Zatosetron maleate (Zatosetron) is prepared as an aqueous solution. Acutely treated animals receive i.p. injections of Zatosetron maleate or saline 2 h before electrophysiological recordings; Chronically treated animals receive injections (i.p.) of Zatosetron maleate or saline once daily for 21 days, and receive their last injection 2 h before electrophysiological recordings. After completion of nine tracks, some animals are administered either apomorphine HCI (0.14 or 0.01 mg/kg i.v.) or haloperidol (0.1 mg/kg i.v.) and the number of dopamine cells is then counted in three additional tracks[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Zatosetron maleate 相关分类

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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