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.
For research use only. We do not sell to patients.
- CAS No.: 2208-51-7
- Formula: C21H24N4O2
- Molecular Weight:364.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | Inhibition |
-8.83 %
Compound: PELANSERIN
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Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
10.21203/rs.3.rs-23951/v1 |
Chemical Information
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CAS No. 2208-51-7
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Molecular Weight 364.44
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Formula C21H24N4O2
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SMILES
O=C1NC2=C(C(N1CCCN3CCN(CC3)C4=CC=CC=C4)=O)C=CC=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)