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Guanfacine, a selective agonist of α2A receptor, is a sympatholytic drug to treat attention deficit hyperactivity disorder (ADHD) and hypertension. It lowers both systolic and diastolic blood pressure.

Guanfacine is an alpha2-adrenergic receptor (alpha2-AR) agonist with Ki values of 93, 1,380, and 3,890 nM for alpha2A-, alpha2B-, and alpha2C-ARs, respectively, in a radioligand binding assay. It has EC50 values 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).

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. It also improves spatial working memory deficits induced by hypobaric hypoxia in rats. Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD). Formal Name: N-(aminoiminomethyl)-2,6-dichloro-benzeneacetamide, monohydrochloride. CAS Number: 29110-48-3. Molecular Formula: C9H9Cl2N3O . HCl. Formula Weight: 282.6. Purity: >98%. Formulation: A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 25 mg/ml, PBS (pH 7.2): 10 mg/ml. SMILES: ClC1=C(CC(NC(N)=N)=O)C(Cl)=CC=C1.Cl. InChi Code: InChI=1S/C9H9Cl2N3O.ClH/c10-6-2-1-3-7(11)5(6)4-8(15)14-9(12)13,/h1-3H,4H2,(H4,12,13,14,15),1H. InChi Key: DGFYECXYGUIODH-UHFFFAOYSA-N.