guanfacine

Guanfacine is a selective agonist of the α2A receptor.

Guanfacine-13C,15N3 is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine (T22824) is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values 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).2Guanfacine (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.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD).

Guanfacine hydrochloride (Intuniv) is a centrally acting antihypertensive agent with specificity towards ADRENERGIC ALPHA-2 RECEPTORS.

Etiguanfacine(SSP-1871) is a agonist of α2-adrenoreceptor.