2208-51-7
Chemical Structure
Pelanserin
- CAS No.: 2208-51-7
- Formula:C21H24N4O2
- Molecular Weight:364.44
IUPAC Name: 3-(3-(4-phenylpiperazin-1-yl)propyl)quinazoline-2,4(1H,3H)-dione
InChIKey: WPKPLSFHHBBLRY-UHFFFAOYSA-N
SMILES: O=C1NC2=C(C(N1CCCN3CCN(CC3)C4=CC=CC=C4)=O)C=CC=C2
Biological Activity: 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].
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Pelanserin | 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. | |||||||||||||||||||||
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References
- [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 [Content Brief]
- [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. [Content Brief]
- [3]. Flores-Murrieta FJ, et al. Pharmacokinetics and antihypertensive effect of oral pelanserin in renal hypertensive dogs. Arzneimittelforschung. 1992 Sep;42(9):1105-8. [Content Brief]
