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New Derivatives of Natural Acyclic Guanidine Alkaloids with TRPV Receptor-Regulating Properties

Authors :
Valentin A. Stonik
Yeon Ju Lee
Tatyana N. Makarieva
Vladimir A. Denisenko
Yuliya V. Korolkova
Irina V. Mosharova
Ekaterina K. Ogurtsova
Yaroslav A. Andreev
Pavel S. Dmitrenok
Eugene V. Grishin
Source :
Natural Product Communications. 10:1934578X1501000
Publication Year :
2015
Publisher :
SAGE Publications, 2015.

Abstract

The guanidine alkaloids, dihydropulchranin A (2), prepared from pulchranin A from the sponge Monanchora pulchra, and hexadecylguanidine (3), a synthetic analog of pulchranins, were studied for their TRPV channel-regulating activities. Compound 2 was active as an inhibitor of rTRPV1 and hTRPV3 receptors with EC50 values of 24.3 and 59.1 μM, respectively. Hexadecylguanidine (3) was not active against these receptors.

Details

ISSN :
15559475 and 1934578X
Volume :
10
Database :
OpenAIRE
Journal :
Natural Product Communications
Accession number :
edsair.doi...........bffd7f8983e933d081ea7f2a5021aa85
Full Text :
https://doi.org/10.1177/1934578x1501000708