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Guanoxabenz hydrochloride Sale

(Synonyms: Hydroxyguanabenz hydrochloride) 目录号 : GC61882

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。

Guanoxabenz hydrochloride Chemical Structure

Cas No.:23256-40-8

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10mM (in 1mL DMSO)
¥3,960.00
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5 mg
¥3,600.00
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10 mg
¥6,120.00
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25 mg
¥12,150.00
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50 mg
¥19,800.00
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100 mg
¥30,600.00
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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.

Chemical Properties

Cas No. 23256-40-8 SDF
别名 Hydroxyguanabenz hydrochloride
Canonical SMILES ClC1=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°C
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1 mg 5 mg 10 mg
1 mM 3.5268 mL 17.6342 mL 35.2684 mL
5 mM 0.7054 mL 3.5268 mL 7.0537 mL
10 mM 0.3527 mL 1.7634 mL 3.5268 mL
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Research Update

[Estimation of guanoxabenz in biological fluids (author's transl)]

Ann Biol Clin (Paris) 1980;38(6):351-4.PMID:7212391doi

A molecule sensitive to light, to variations in temperature and pH, Guanoxabenz hydrochloride cannot be estimated in biological fluids according to classical technics. The authors propose an analytical method based, during the extraction phase, on the formation of a copper complex extractable in organic medium and in the true phase of measurement, on the transformation, by hydrochloric acid hydrolysis in dichloro-2-6-benzaldehyde, estimated by gas phase chromatography with detection by capture of electrons. The sensitivity and the specificity of the technic authorise its use in pharmacokinetic studies in man.