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强效5-羟色胺3（5-HT3）受体拮抗剂（R）-扎考必利在中枢神经系统中标记出另一个高亲和力位点。

The potent 5-HT3 receptor antagonist (R)-zacopride labels an additional high affinity site in the central nervous system.

作者信息

Kidd E, Bouchelet de Vendegies I, Levy J C, Hamon M, Gozlan H

机构信息

INSERM U288, Neurobiologie Cellulaire et Fonctionnelle, Faculté de Médecine Pitié-Salpêtrière, Paris, France.

出版信息

Eur J Pharmacol. 1992 Jan 28;211(1):133-6. doi: 10.1016/0014-2999(92)90276-a.

DOI:10.1016/0014-2999(92)90276-a
PMID:1618262
Abstract

The binding characteristics of 3H- and 3H-zacopride were investigated in membranes from the rat entorhinal cortex and NG 108-15 clonal cells. In contrast to 3H-zacopride which bound solely to 5-HT3 receptors, 3H-zacopride recognized another class of binding sites, called the (R)-sites, in both membrane preparations. In addition to (R)-zacopride (Ki = 3-11 nM), only (R)-iodo-zacopride, (R)-dechloro-zacopride, prazosin and mianserin exhibited high to moderate affinity for the (R)-sites, whose possible functions remain to be established.

摘要

研究了³H-和³H-扎考必利在大鼠内嗅皮质和NG 108-15克隆细胞膜中的结合特性。与仅与5-HT₃受体结合的³H-扎考必利不同，³H-扎考必利在两种膜制剂中均识别另一类结合位点，称为(R)-位点。除了(R)-扎考必利（Ki = 3-11 nM）外，只有(R)-碘扎考必利、(R)-脱氯扎考必利、哌唑嗪和米安色林对(R)-位点表现出高至中等亲和力，其可能的功能仍有待确定。

相似文献

1
The potent 5-HT3 receptor antagonist (R)-zacopride labels an additional high affinity site in the central nervous system.强效5-羟色胺3（5-HT3）受体拮抗剂（R）-扎考必利在中枢神经系统中标记出另一个高亲和力位点。
Eur J Pharmacol. 1992 Jan 28;211(1):133-6. doi: 10.1016/0014-2999(92)90276-a.
2
Characterisation of the non-5-HT3 high-affinity 'R' binding site for (R)-zacopride in brain and other tissues.脑及其他组织中(R)-扎考必利非5-HT3高亲和力“R”结合位点的表征
Eur J Pharmacol. 1993 Sep 15;247(1):45-56. doi: 10.1016/0922-4106(93)90136-w.
3
Common pharmacological and physico-chemical properties of 5-HT3 binding sites in the rat cerebral cortex and NG 108-15 clonal cells.
Biochem Pharmacol. 1990 Oct 1;40(7):1541-50. doi: 10.1016/0006-2952(90)90452-q.
4
[(125I)iodo-zacopride: new ligand for the study by autoradiography of central 5-HT3 receptors].
C R Acad Sci III. 1990;311(6):231-7.
5
Differential binding characteristics of agonists at 5-HT3 receptor recognition sites in NG108-15 neuroblastoma-glioma cells labelled by [3H]-(S)-zacopride and [3H]granisetron.用[3H]-(S)-扎考必利和[3H]格拉司琼标记的NG108-15神经母细胞瘤-胶质瘤细胞中5-HT3受体识别位点激动剂的差异结合特性
Biochem Pharmacol. 1993 May 25;45(10):2155-8. doi: 10.1016/0006-2952(93)90030-z.
6
Distribution of S(-)-zacopride-insensitive [125I]R(+)-zacopride binding sites in the rat brain and peripheral tissues.S(-)-扎考必利不敏感的[125I]R(+)-扎考必利结合位点在大鼠脑和外周组织中的分布。
Eur J Pharmacol. 1997 Aug 13;332(3):307-12. doi: 10.1016/s0014-2999(97)01091-1.
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The (S)-isomer of [3H]zacopride labels 5-HT3 receptors with high affinity in rat brain.[3H]扎考必利的（S）-异构体在大鼠脑中以高亲和力标记5-HT3受体。
Eur J Pharmacol. 1990 Jun 8;181(3):283-7. doi: 10.1016/0014-2999(90)90090-s.
8
[3H]zacopride binding to 5-hydroxytryptamine3 sites on partially purified rabbit enteric neuronal membranes.[3H]扎考必利与部分纯化的兔肠神经元膜上的5-羟色胺3位点的结合。
J Pharmacol Exp Ther. 1989 Dec;251(3):962-8.
9
Quantitative autoradiographic mapping of 5-HT3 receptors in the rat CNS using [125I]iodo-zacopride and [3H]zacopride as radioligands.使用[125I]碘扎考必利和[3H]扎考必利作为放射性配体对大鼠中枢神经系统中5-HT3受体进行定量放射自显影定位。
Synapse. 1992 Apr;10(4):271-81. doi: 10.1002/syn.890100402.
10
The differential activities of R (+)- and S(-)-zacopride as 5-HT3 receptor antagonists.
Pharmacol Biochem Behav. 1990 Dec;37(4):717-27. doi: 10.1016/0091-3057(90)90554-u.

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Increased 5-HT release mediates the anxiogenic response during benzodiazepine withdrawal: a review of supporting neurochemical and behavioural evidence.
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Psychopharmacology (Berl). 1993;112(1):1-12. doi: 10.1007/BF02247357.
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The pharmacology of VA21B7: an atypical 5-HT3 receptor antagonist with anxiolytic-like properties in animal models.VA21B7的药理学：一种在动物模型中具有抗焦虑样特性的非典型5-羟色胺3受体拮抗剂。
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Br J Pharmacol. 1993 Nov;110(3):1079-84. doi: 10.1111/j.1476-5381.1993.tb13924.x.
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Psychopharmacology (Berl). 1992;108(3):333-7. doi: 10.1007/BF02245120.
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Differential modulation of extracellular levels of 5-hydroxytryptamine in the rat frontal cortex by (R)- and (S)-zacopride.（R）-和（S）-扎考必利对大鼠额叶皮质细胞外5-羟色胺水平的差异调节
Br J Pharmacol. 1992 Sep;107(1):233-9. doi: 10.1111/j.1476-5381.1992.tb14492.x.