进一步描述的5 -羟色胺受体(假定的5-HT2B)在大鼠胃底纵肌。

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巴克斯特GS,墨菲OE,布莱克本TP

进一步描述的5 -羟色胺受体(假定的5-HT2B)在大鼠胃底纵肌。

Br杂志。1994;112(1):323 - 31所示。

PubMed ID

8032658 (在PubMed

]

文摘

1。本研究进行隔离并描述药物均匀的5 -羟色胺(5 -)从人口可能混合受体受体调节浓度鼠胃纵行肌的眼底。我们的目标是扩展的药理特性5-HT2B受体表达准备报道。2。最小化自发活动和任何圆形肌肉收缩反应的影响,狭窄(1 - 1.5 x 20 mm)段mucosa-denuded纵肌。在这种情况下,单胺氧化酶的封锁与优降宁(100 microM 15分钟)引起了左侧的位移的浓度效应曲线5-methoxytryptamine (5-MeO-T)和色胺。无论是优降宁还是5 -吸收抑制剂影响反应。3所示。在优降宁进行准备工作,订单的效力色胺类似物数量如下:5-MeO-T >或= alpha-Me-5-HT > = 5 - > 5-carboxamidotryptamine (5-CT) >色胺> 2-Me-5-HT。除了几个已知配体作为受体激动剂或5-HT2A 5-HT2C受体包括1-m-chlorophenylpiperazine (m-CPP),俄罗斯24969年,可212年和23390年原理图也受体激动剂在大鼠眼底舒马曲坦同时renzapride和8-hydroxy-2——(di-n-propylamino)萘满(8-OH-DPAT)很弱或不活跃。 With the exception of 2-Me-5-HT and m-CPP, most agonists produced monophasic concentration-effect curves consistent with an interaction at a single site. High concentrations of 2-Me-5-HT evoked relaxations which were blocked by phentolamine (1 MicroM) suggesting an interaction with alpha-adrenoceptors. m-CPP often evoked biphasic concentration-effect curves with a second contractile phase which was insensitive to yohimbine at concentrations higher than required for antagonism of responses to 5-HT.4. LY 53857, methiothepin, methysergide, ritanserin and ICI 170809 were potent but non-surmountable antagonists of 5-HT in rat fundus. In contrast, several ligands behaved as surmountable antagonists with the following order of potency: rauwolscine >yohimbine = mesulergine > mianserin = SB 204070 >WY 26703 > SB 200646> pirenpirone> renzapride. DAU 6285, granisetron, spiperone, ketanserin,phentolamine and GR 127935 did not affect responses to 5-HT at concentrations up to 1 pM. The agonist and concentration independent profile of antagonism supported a single site interaction for both agonists and antagonists.5. We conclude that despite small differences concerning the enantiomeric selectivity and affinity of rauwolscine and yohimbine, the close pharmacological identity of 5-HT receptors in rat stomach fundus and the recently cloned 5-HT2B receptor is maintained. SB 200646, which demonstrates some selectivity for 5-HT receptors in rat stomach fundus, should provide a useful ligand for confirmation of this view and allow discrimination of 5-HT2B function both in vitro and in vivo.

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药物靶点

药物	目标	类	生物	药理作用	行动
育亨宾	5 -羟色胺受体2	蛋白质	人类	未知的	拮抗剂	细节
育亨宾	5 -羟色胺受体2 b	蛋白质	人类	未知的	拮抗剂	细节
育亨宾	5 -羟色胺受体2摄氏度	蛋白质	人类	未知的	拮抗剂	细节