Pelanserine

Pelanserin (Compound 1) is an orally active antihypertensive agent. Pelanserin is a potent 5-HT2 receptor antagonist. Pelanserin has the ability to block the activity of α-adrenergic receptor, with its ED50 being 0.03 μg/mL. Pelanserin has vasodilatory activity, with its ED100 being 5 μg. Pelanserin exhibits antihypertensive activity in hypertensive rats and renal hypertensive dog breeds. Pelanserin can be used for research on hypertension[1][2][3].

2208-51-7

12352005

5-HT Receptor; Adrenergic Receptor

GPCR/G Protein; Neuronal Signaling

Cardiovascular Disease

O=C1NC2=C(C(N1CCCN3CCN(CC3)C4=CC=CC=C4)=O)C=CC=C2

C21H24N4O2

364.44

[1]Havera HJ, Vidrio H. Derivatives of 1,3-disubstituted 2,4 (1H,3H) -quinazolinediones as possible peripheral vasodilators or antihypertensive agents. J Med Chem. 1979 Dec;22 (12) :1548-50|[2]Villalobos-Molina R, et al. The 5-HT2 receptor antagonist, pelanserin, inhibits alpha 1-adrenoceptor-mediated vasoconstriction in vitro. Eur J Pharmacol. 1995 Apr 24;277 (2-3) :181-5.|[3]Flores-Murrieta FJ, et al. Pharmacokinetics and antihypertensive effect of oral pelanserin in renal hypertensive dogs. Arzneimittelforschung. 1992 Sep;42 (9) :1105-8.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-180379/

Reference compound1

No Development Reported