1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Guanoxabenz

Guanoxabenz  (Synonyms: Hydroxyguanabenz)

目录号: HY-U00123
产品使用指南

Guanoxabenz是α2肾上腺素能 (α2 adrenergic receptor) 受体激动剂,Ki 值为 4000 nM,对 α2A 的 Ki 值为 40 nM。

该游离形式化合物不稳定,推荐具有相同生物学活性的稳定盐形式 Guanoxabenz hydrochloride

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Guanoxabenz Chemical Structure

Guanoxabenz Chemical Structure

CAS No. : 24047-25-4

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Guanoxabenz 的其他形式现货产品:

Other Forms of Guanoxabenz:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Guanoxabenz is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor[1][2][3].

IC50 & Target

Adrenergic receptor[1]

体外研究
(In Vitro)

The formation of high-affinity Guanoxabenz binding seems to be inhibited by a series of N-hydroxyguanidine analogs to Guanoxabenz, as well as by a series of metabolic inhibitors that included allopurinol, 1-chloro-2,4-dinitrobenzene, 5,59-dithiobis-(2-nitrobenzoic acid), cibacron blue, phenyl-p-benzoquinone, didox, and trimidox. The formation of Guanoxabenz high-affinity binding is also inhibited in a time- and concentration-dependent fashion by preincubating the membranes with the LW03 N-hydroxyguanidine analogue of Guanoxabenz[1]. The spleen cytosolic fraction mediates the reduction of Guanoxabenz to guanabenz, the latter having an almost 100-fold higher affinity for rat alpha2A-adrenoceptors than Guanoxabenz itself[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Guanoxabenz and guanabenz are both known as centrally active antihypertensive drugs. High affinity Guanoxabenz binding is induced in rat brain membranes after addition of NADH or NADPH cofactors. The rat cerebral cortex contains an enzymatic activity that may activate Guanoxabenz leading to formation of a metabolite showing high affinity for alpha 2-adrenoceptors[3].
Guanoxabenz (0.1-3 mg/kg, i.p.) causes a dose-related reduction in locomotor activity; a dose of 1 mg/kg is selected since this induces a pronounced and sustained behavioural hypoactivity[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rats[4].
Dosage: 0.5 mg/kg (RX 781094 or saline vehicle was injected intravenously (tail vein) at the time of peak effect of the agonist (20min for clonidine and 30 min for Guanoxabenz).
Administration: IP.
Result: RX 781094 (0.1-1.0 mg/kg, i.v.) produces a rapid (< 5 set) and complete antagonism of the EEG and behavioural effects induced by clonidine and Guanoxabenz.
分子量

247.08

Formula

C8H8Cl2N4O

CAS 号
中文名称

胍诺沙苄;

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Guanoxabenz
目录号:
HY-U00123
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