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Guanoxabenz hydrochloride
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。
Guanoxabenz hydrochloride图片
CAS NO:23256-40-8
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
Guanoxabenz (Hydroxyguanabenz) hydrochloride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。
Cas No.23256-40-8
别名Hydroxyguanabenz hydrochloride
Canonical SMILESClC1=C(/C=N/NC(NO)=N)C(Cl)=CC=C1.[H]Cl
分子式C8H9Cl3N4O
分子量283.54
溶解度DMSO : 83.33 mg/mL (293.89 mM)
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Guanoxabenz (Hydroxyguanabenz) hydrochloride 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].

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].

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].

References:
[1]. UhlÉn S, et al. Characterization of the enzymatic activity for biphasic competition by guanoxabenz (1-(2,6-dichlorobenzylidene-amino)-3-hydroxyguanidine) at alpha2-adrenoceptors. I. Description of an enzymatic activity in spleen membranes. Biochem Pharmacol. 1998 Nov 1;56(9):1111-9.
[2]. Dambrova M, et al. Characterization of the enzymatic activity for biphasic competition by guanoxabenz (1-(2,6-dichlorobenzylidene-amino)-3-hydroxyguanidine) at alpha2-adrenoceptors. II. Description of a xanthine-dependent enzymatic activity in spleen cytosol. Biochem Pharmacol. 1998 Nov 1;56(9):1121-8.
[3]. Dambrova M, et al. Characterization of Guanoxabenz reducing activity in rat brain. Pharmacol Toxicol. 1998 Oct;83(4):158-63.
[4]. P W Dettmar, et al. Neuropharmacological studies in rodents on the action of RX 781094, a new selective alpha 2-adrenoceptor antagonist. Neuropharmacology. 1983 Jun;22(6):729-37.