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5-羟色胺M受体拮抗作用预防顺铂所致呕吐。

5-Hydroxytryptamine M-receptor antagonism to prevent cisplatin-induced emesis.

作者信息

Costall B, Domeney A M, Naylor R J, Tattersall F D

出版信息

Neuropharmacology. 1986 Aug;25(8):959-61. doi: 10.1016/0028-3908(86)90030-4.

DOI:10.1016/0028-3908(86)90030-4
PMID:3774121
Abstract

The administration to the ferret of cisplatin, 10mg/kg (i.v.), caused an intense emetic response that was prevented by ICS 205-930 (0.1 and 1.0 mg/kg i.v.) and metoclopramide (4.0 mg/kg i.v.). Smaller doses of ICS 205-930 (0.01 mg/kg i.v.) and metoclopramide (2.0 mg/kg i.v.) attenuated the emetic response to cisplatin. It is concluded that the potent action of ICS 205-930 against cisplatin-induced emesis is the consequence of a 5-hydroxytryptamine M-receptor antagonism which may also contribute to the antiemetic action of metoclopramide.

摘要

给雪貂静脉注射10mg/kg顺铂会引发强烈的呕吐反应,而ICS 205 - 930(静脉注射0.1和1.0mg/kg)和甲氧氯普胺(静脉注射4.0mg/kg)可预防该反应。较小剂量的ICS 205 - 930(静脉注射0.01mg/kg)和甲氧氯普胺(静脉注射2.0mg/kg)可减弱对顺铂的呕吐反应。得出的结论是,ICS 205 - 930对顺铂诱导呕吐的强效作用是5 - 羟色胺M受体拮抗作用的结果,这也可能有助于甲氧氯普胺的止吐作用。

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