人类5-hydroxytryptamine2B的药理学和分销(5-HT2B)受体基因产品:5-HT2A与5-HT2C受体。

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Bonhaus DW,巴赫C, DeSouza,萨拉查跳频,松岗BD, Zuppan P,成龙HW, Eglen RM

人类5-hydroxytryptamine2B的药理学和分销(5-HT2B)受体基因产品:5-HT2A与5-HT2C受体。

Br J杂志。1995年6月,115 (4):622 - 8。

PubMed ID

7582481 (在PubMed

]

文摘

1。全长克隆人类5-HT2B受体隔绝人类肝脏、肾脏和胰腺。克隆人类5-HT2B受体有高度的同源性(大约80%)5-HT2B受体鼠和老鼠。2。PCR扩增被用来确定人类5-HT2B受体信使rna的组织分布。信使rna编码5-HT2B受体表达了最大的丰富人类的肝脏和肾脏。低水平的表达是在大脑皮层中发现,整个大脑,胰腺,脾脏。表达式中没有检测到心脏。3所示。北部污点分析证实5-HT2B受体信使rna的存在(2.4 kB大小的乐队)在胰腺,肝和肾。 An additional 3.2 kB sized band of hybridization was detected in liver and kidney. This raises the possibility of a splice variant of the receptor or the presence of an additional homologous receptor. 4. The human 5-HT2B receptor was expressed in Cos-7 cells and its ligand binding characteristics were compared to similarly expressed human 5-HT2A and 5-HT2C receptors. The ligand specificity of the human 5-HT2B receptor (5-HT > ritanserin > SB 204741 > spiperone) was distinct from that of the human 5-HT2A (ritanserin > spiperone > 5-HT > SB 204741) and 5-HT2C (ritanserin > 5-HT > spiperone = SB 204741) receptors. On the basis of a higher affinity for ketanserin and a lower affinity for yohimbine the human 5-HT2B receptor also appeared to differ from the rat 5-HT2B receptor. 5. These findings confirm the sequence of the human 5-HT2B receptor and they demonstrate that the receptor has a widespread tissue distribution. In addition, these data suggest that there are differences in ligand affinities between different species homologues of the receptor. Finally, the finding of two distinct bands on the Northern blots of liver and kidney raises the possibility of splice variants or subtypes of 5-HT2B receptors, within these tissues.

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绑定属性

药物	目标	财产	测量	pH值	温度(°C)
二甲麦角新碱	5 -羟色胺受体2	Ki (nM)	3.98	N /一个	N /一个	细节
二甲麦角新碱	5 -羟色胺受体2摄氏度	Ki (nM)	1.58	N /一个	N /一个	细节
米安色林	5 -羟色胺受体2	Ki (nM)	6.3	N /一个	N /一个	细节
米安色林	5 -羟色胺受体2	Ki (nM)	3.98	N /一个	N /一个	细节
米安色林	5 -羟色胺受体2摄氏度	Ki (nM)	5.01	N /一个	N /一个	细节
育亨宾	5 -羟色胺受体2	Ki (nM)	> 10000	N /一个	N /一个	细节
育亨宾	5 -羟色胺受体2	Ki (nM)	1000年	N /一个	N /一个	细节
育亨宾	5 -羟色胺受体2摄氏度	Ki (nM)	> 10000	N /一个	N /一个	细节