Bioactivity | Guanfacine-d2 (hydrochloride) is the deuterium labeled Guanfacine hydrochloride. Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors[1][2]. |
Invitro | Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1]. |
Name | Guanfacine-d2 (hydrochloride) |
CAS | 1398065-88-7 |
Formula | C9H8D2Cl3N3O |
Molar Mass | 284.57 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Intengan HD, Smyth DD. Alpha-2a/d adrenoceptor subtype stimulation by guanfacine increases osmolar clearance. J Pharmacol Exp Ther. 1997 Apr;281(1):48-53. [3]. Uhlén S, Wikberg JE. Delineation of rat kidney alpha 2A- and alpha 2B-adrenoceptors with [3H]RX821002 radioligand binding: computer modelling reveals that guanfacine is an alpha 2A-selective compound. Eur J Pharmacol. 1991 Sep 17;202(2):235-43. [4]. Board AW, Perry VP, Shepperson BE, A postmarketing evaluation of guanfacine hydrochloride in mild to moderate hypertension. Clin Ther. 1988;10(6):761-75. [5]. Guanfacine |