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[3H]ICS 205 - 930标记猫和兔迷走神经及颈上神经节膜中的5 - HT3识别位点。

[3H]ICS 205-930 labels 5-HT3 recognition sites in membranes of cat and rabbit vagus nerve and superior cervical ganglion.

作者信息

Hoyer D, Waeber C, Karpf A, Neijt H, Palacios J M

机构信息

Preclinical Research, Sandoz Ltd., Basel, Switzerland.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1989 Oct;340(4):396-402. doi: 10.1007/BF00167040.

DOI:10.1007/BF00167040
PMID:2586633
Abstract

The binding characteristics of [3H]ICS 205-930, a 5-hydroxytryptamine 5-HT3 receptor antagonist, were investigated in membranes prepared from cat and rabbit vagus nerve (VN) and superior cervical ganglion (SCG). The autoradiographic localisation of 5-HT3 recognition sites was also assessed using [3H]ICS 205-930 in slices from cat medulla oblongata, nodose ganglion and vagus nerve. [3H]ICS 205-930 bound to a homogeneous population of high affinity recognition sites in cat VN: Bmax = 201 +/- 43 fmol/mg protein, pKD = 9.26 +/- 0.17 and SCG: Bmax = 291 +/- 40 fmol/mg, pKD = 9.35 +/- 0.80 (n = 3). Competition experiments performed in membranes from cat VN and SCG with agonists and antagonists suggested the presence of a homogeneous population of [3H]ICS 205-930 recognition sites. Competition curves were steep and monophasic and were best fitted by a 1 receptor site model. The following rank order of affinity for [3H]ICS 205-930 binding sites was observed with antagonists: SDZ 206-830 = ICS 205-930 greater than BRL 43694 greater than SDZ 206-792 greater than quipazine greater than MDL 72222 greater than metoclopramide greater than mCPP and agonists: 2-methyl-5-HT = 5-HT greater than phenylbiguanide. A similar profile was observed for a limited series of compounds in rabbit membranes. Drugs acting at 5-HT1, 5-HT2 and dopamine receptors (domperidone, spiperone and metergoline) showed very low affinities for [3H]ICS 205-930 recognition sites. The sites labelled with [3H]ICS 205-930 in vagus nerve and superior cervical ganglion of both species displayed the pharmacological profile of a 5-HT3 receptor.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

研究了5-羟色胺5-HT3受体拮抗剂[3H]ICS 205-930在猫和兔迷走神经（VN）及颈上神经节（SCG）制备的膜中的结合特性。还使用[3H]ICS 205-930在猫延髓、结状神经节和迷走神经切片中评估了5-HT3识别位点的放射自显影定位。[3H]ICS 205-930与猫VN中高亲和力识别位点的同质群体结合：Bmax = 201 +/- 43 fmol/mg蛋白，pKD = 9.26 +/- 0.17；与SCG结合：Bmax = 291 +/- 40 fmol/mg，pKD = 9.35 +/- 0.80（n = 3）。在猫VN和SCG的膜中用激动剂和拮抗剂进行的竞争实验表明存在[3H]ICS 205-930识别位点的同质群体。竞争曲线陡峭且单相，最适合用1受体位点模型拟合。观察到拮抗剂对[3H]ICS 205-930结合位点的亲和力顺序如下：SDZ 206-830 = ICS 205-930 > BRL 43694 > SDZ 206-792 > 喹哌嗪 > MDL 72222 > 甲氧氯普胺 > mCPP；激动剂顺序为：2-甲基-5-HT = 5-HT > 苯基胍。在兔膜中对有限系列的化合物观察到类似的情况。作用于5-HT1、5-HT2和多巴胺受体的药物（多潘立酮、螺哌隆和麦角乙脲）对[3H]ICS 205-930识别位点的亲和力非常低。在两种动物的迷走神经和颈上神经节中用[3H]ICS 205-930标记的位点显示出5-HT3受体的药理学特征。（摘要截短于250字）

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