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6-(4-Methoxyphenyl)-3-pyridazinamine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
6-(4-Methoxyphenyl)-3-pyridazinamine图片
CAS NO:4776-87-8
规格:98%
分子量:201.2
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
GABAA receptor antagonist
CAS:4776-87-8
分子式:C11H11N3O
分子量:201.2
纯度:98%
存储:Store at -20°C

Background:

6-(4-Methoxyphenyl)-3-pyridazinamine is a GABAA receptor antagonist.


Ionotropic GABAA receptors are ligand-gated ion channels that facilitate the passing of chloride ions across the cell membrane and promote an inhibitory influence on target neurons. These receptors are the major targets for benzodiazepines and related anxiolytic drugs.


In vitro: 6-(4-Methoxyphenyl)-3-pyridazinamine is an intermediate in the synthesis of SR 95103 [2-(3-carboxypropyl)-3-amino-4-methyl-6-phenylpyridazinium chloride]. SR 95103 was identified as a selective and competitive GABA-A receptor antagonist. Moreover, SR 95103 was shown to be able to displace [3H]GABA from rat brain membranes with an apparent Ki of 2.2 μM. In addition, SR 95103 was found, on the basis of biochemical, electrophysiological, and pharmacological results, to be a selective and competitive antagonist of GABA at the GABA-A receptor site [1].


In vivo: The behavioral effects of unilateral microinjections of SR 95103 into periventricular structures were studied. Results showed that when injected into the medial hypothalamus (MH) or into the dorsal part of the mesencephalic central gray (CG), SR 95103 produced a dose-dependent behavioral activation together with jumps. The behavioral activation was found to be attenuated by pretreatment with THIP, a GABA receptor agonist [2].


Clinical trial: So far, no clinical study has been conducted.


参考文献:
[1] Wermuth, C. G.,Bourguignon, J.J.,Schlewer, G., et al. Synthesis and structure-activity relationships of a series of aminopyridazine derivatives of γ-aminobutyric acid acting as selective GABA-A antagonists. Journal of Medicinal Chemistry 30(2), 239-249 (1987).
[2] Schmitt P, Di Scala G, Brandao ML, Karli P.  Behavioral effects of microinjections of SR 95103, a new GABA-A antagonist, into the medial hypothalamus or the mesencephalic central gray. Eur J Pharmacol. 1985 Nov 5;117(2):149-58.