In vitro TRPV1 activity of piperine derived amides
Andres Correa, Edwin ; Högestätt, Edward LU ; Sterner, Olov LU ; Echeverri, Fernando and Zygmunt, Peter LU
(2010)
In Bioorganic & Medicinal Chemistry
18(9).
p.3299-3306
- 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. (C) 2010 Elsevier Ltd. All rights reserved.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/1619532
- author
- Andres Correa, Edwin
; Högestätt, Edward
LU
; Sterner, Olov
LU
; Echeverri, Fernando
and Zygmunt, Peter
LU
- organization
- publishing date
- 2010
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- Fluorometric assays, vanilloid 1, Transient receptor potential, Piperine, Piperine-derived amides, Pain, Analgesic activity
- in
- Bioorganic & Medicinal Chemistry
- volume
- 18
- issue
- 9
- pages
- 3299 - 3306
- publisher
- Elsevier
- external identifiers
-
- wos:000277083400032
- scopus:77951295220
- pmid:20381363
- ISSN
- 0968-0896
- DOI
- 10.1016/j.bmc.2010.03.013
- language
- English
- LU publication?
- yes
- additional info
- The information about affiliations in this record was updated in December 2015. The record was previously connected to the following departments: Division of Clinical Chemistry and Pharmacology (013250300), Organic chemistry (S/LTH) (011001240)
- id
- 1646da8c-75df-49cf-ad84-ed71151fd48f (old id 1619532)
- date added to LUP
- 2016-04-01 10:56:40
- date last changed
- 2022-04-28 03:03:13
@article{1646da8c-75df-49cf-ad84-ed71151fd48f,
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. (C) 2010 Elsevier Ltd. All rights reserved.}},
author = {{Andres Correa, Edwin and Högestätt, Edward and Sterner, Olov and Echeverri, Fernando and Zygmunt, Peter}},
issn = {{0968-0896}},
keywords = {{Fluorometric assays; vanilloid 1; Transient receptor potential; Piperine; Piperine-derived amides; Pain; Analgesic activity}},
language = {{eng}},
number = {{9}},
pages = {{3299--3306}},
publisher = {{Elsevier}},
series = {{Bioorganic & Medicinal Chemistry}},
title = {{In vitro TRPV1 activity of piperine derived amides}},
url = {{http://dx.doi.org/10.1016/j.bmc.2010.03.013}},
doi = {{10.1016/j.bmc.2010.03.013}},
volume = {{18}},
year = {{2010}},
}