Guanfacine-13C,15N3

Description: Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an alpha2-adrenergic receptor (alpha2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for alpha2A-, alpha2B-, and alpha2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for alpha2A-, alpha2B-, and alpha2C-ARs, respectively, for stimulated [35S]GTPgammaS 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). Smiles: [15NH2][13C](=[15NH])[15NH]C(=O)Cc1c(Cl)cccc1Cl. References: Jasper, J.R., Lesnick, J.D., Chang, L.K., et al.Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: Agonist-mediated [35S]GTPgammaS bindingBiochem. Pharmacol.55(7)1035-1043(1998)