Guanoxabenz
Guanoxabenz is an α2 adrenergic receptor agonist, with a Ki of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor.
The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Guanoxabenz hydrochloride) that retains the same biological activity.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 24047-25-4
- 화학식: C8H8Cl2N4O
- 분자량:247.08
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Other In-stock Forms of Guanoxabenz
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Adrenergic Receptor Isoforms
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Biological Activity
제품 설명
IC50 & Target
Adrenergic receptor[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[4].
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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).
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Administration:IP.
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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.
Chemical Information
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CAS No. 24047-25-4
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분자량 247.08
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화학식 C8H8Cl2N4O
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SMILES
ClC1=C(/C=N/NC(NO)=N)C(Cl)=CC=C1
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Synonyms
Hydroxyguanabenz
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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 Pharmac [Content Brief]
[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 cyto [Content Brief]
[3]. Dambrova M, et al. Characterization of Guanoxabenz reducing activity in rat brain. Pharmacol Toxicol. 1998 Oct;83(4):158-63. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Guanoxabenz Related Classifications
HY-U00123 Related Classifications
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