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超激动剂
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超级激动剂(英语:superagonist)在药理学中是指一种能作用于受体的激动剂,它产生的最大反应比内源激动剂更大。因此超级激动剂的内在活性大于100%。[1][2]例如戈舍瑞林(英语:goserelin)就是一种促性腺激素释放激素受体(英语:Gonadotropin-releasing hormone receptor)的超级激动剂。[3]
参见
参考资料
- Carlier PR, Chow ES, Barlow RL, Bloomquist JR. Discovery of non-zwitterionic GABAA receptor full agonists and a superagonist. Bioorg. Med. Chem. Lett. August 2002, 12 (15): 1985–8. PMID 12113824. doi:10.1016/S0960-894X(02)00299-8.
- Tan CM, Wilson MH, MacMillan LB, Kobilka BK, Limbird LE. Heterozygous α2A-adrenergic receptor mice unveil unique therapeutic benefits of partial agonists. Proc. Natl. Acad. Sci. U.S.A. September 2002, 99 (19): 12471–6. PMC 129469
. PMID 12205290. doi:10.1073/pnas.122368499.
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