An α2-AR agonist (Kis = 93

Guanfacine (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
29110-48-3
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Ki values of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.{40326} It has EC50 values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki = 19 nM in a radioligand binding assay).{40341} Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.{40342} It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.{40340} Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD).  

 

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Description

An α2-AR agonist (Kis = 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively); EC50s = 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively for stimulated [35S]GTPγS binding; Ki = 19 nM for imidazoline receptor 1; lowers blood pressure in hypertensive rats in a dose-dependent manner when administered at a dose of 0.3-5 mg/kg; improves spatial working memory deficits induced by hypobaric hypoxia in rats

Formal name: N-(aminoiminomethyl)-2,6-dichloro-benzeneacetamide, monohydrochloride

Synonyms: 

Molecular weight: 282.6

CAS: 29110-48-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory

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