受体激动剂的功能描述重组人类5-HT2A 5-HT2B和CHO-K1 5-HT2C受体细胞。
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波特RH Benwell KR、羊肉H,马尔科姆·c·艾伦NH,瑞DF,亚当斯博士,Sheardown乔丹
受体激动剂的功能描述重组人类5-HT2A 5-HT2B和CHO-K1 5-HT2C受体细胞。
Br J杂志。1999年9月,128 (1):13-20。
- PubMed ID
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10498829 (在PubMed]
- 文摘
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1。本研究的目的是描述人类5-HT2A的兴奋剂药理学,5-HT2B和5-HT2C水疱性口炎病毒()受体表达CHO-K1(中国仓鼠卵巢细胞。2。我们使用荧光成像板读者(FLIPR),允许在细胞内钙含量检测的快速上涨的受体激动剂。3所示。刺激引起的所有三个受体通过5 -一个健壮的浓度依赖的细胞内钙含量的增加。没有这样的效果观察从non-transfected控制CHO-K1细胞。4所示。效力的等级次序不同受体亚型受体激动剂。成份,bw - 723 c86 d-norfenfluramine, Ro 60 - 0175和迷幻药表现出以下等级次序的效力; 5-HT2B>5-HT2C>5-HT2A. Piperazines such as m-Chlorophenylpiperazine (mCPP), ORG-12962, MK-212 and also ORG-37684 exhibited a rank order of potency of 5-HT2C>5-HT2B>5-HT2A. The phenylisopropylamines DOI and DOB had a rank order of 5-HT2A>5-HT2B>5-HT2C. 5. Many agonists tested had partial agonist actions when compared to 5-HT, and a wide range of relative efficacies were exhibited, which was cell line dependent. For example, mCPP had a relative efficacy of 65% at 5-HT2C receptors but <25% at either 5-HT2A or 5-HT2B receptors. 6. Interpretation of literature values of functional assays using different cell lines, different receptor expression levels and different receptor isoforms, is complex. Species differences and the previous use of antagonist radioligands to characterize agonist potency in binding assays emphasizes the importance of studying agonists in the same experiment using the same assay conditions and parental cell lines.