Guanfacine is an a2-adrenergic receptor (a2-AR) agonist with Ki values of 93, 1,380, and 3,890 nM for a2A-, a2B-, and a2C-ARs, respectively, in a radioligand binding assay.{40326} It has EC50 values of 52, 288, and 602 nM for a2A-, a2B-, and a2C-ARs, respectively, for stimulated [35S]GTP?S 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).
Technical Information
Formal Name
2-(1',6'-dihydro-6'-oxo-1'-phenyl[2,3'-bipyridin]-5'-yl)-benzonitrile
CAS Number
380917-97-5
Molecular Formula
C23H15N3O
Formula Weight
349.4
Purity
98%
Formulation
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A crystalline solid
Solubility
(Learn about Variance in Solubility)
Acetonitrile: >1 mg/ml
Chloroform: slightly soluble
DMSO: slightly soluble
λmax
295, 347 nm
SMILES
O=C1N(C2=CC=CC=C2)C=C(C3=CC=CC=N3)C=C1C4=C(C#N)C=CC=C4
InChi Code
InChI=1S/C23H15N3O/c24-15-17-8-4-5-11-20(17)21-14-18(22-12-6-7-13-25-22)16-26(23(21)27)19-9-2-1-3-10-19/h1-14,16H
InChi Key
PRMWGUBFXWROHD-UHFFFAOYSA-N
Regulatory Information
DEA Schedule
III
Shipping & Storage Information
Storage -20°C
Shipping
Room Temperature in continental US; may vary elsewhere
Stability
Shelf life: 5 years