In vitro TRPV1 activity of piperine derived amides.

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Correa EA, Hogestatt ED, Sterner O, Echeverri F, Zygmunt PM

In vitro TRPV1 activity of piperine derived amides.

Bioorg Med Chem. 2010 May 1;18(9):3299-306. doi: 10.1016/j.bmc.2010.03.013. Epub 2010 Mar 11.

PubMed ID

20381363 [ View in PubMed

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Abstract

A series of natural and synthetic piperine amides were evaluated for activity on the human TRPV1 expressed in HEK293 cells. The agonistic effect of piperine amides was mainly dependent on the length of the carbon chain. Structural changes of double bonds and stereochemistry in the aliphatic chain of these compounds did not change their potency or efficacy, indicating that increased rigidity or planarity of the piperine structure does not affect the activity. The opening of the methylenedioxy ring or changes in the heterocyclic ring of the piperine molecule reduced or abolished activity. Furthermore, inactive compounds did not display functional antagonistic activity.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Capsaicin	Transient receptor potential cation channel subfamily V member 1	EC 50 (nM)	2.51	N/A	N/A	Details