Naloxone Is a Potential Binding Ligand and Activator of the Capsaicin Receptor TRPV1

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F20%3A00532415" target="_blank" >RIV/61388963:_____/20:00532415 - isvavai.cz</a>

Alternative codes found

RIV/00216208:11310/20:10415787

Result on the web

<a href="https://doi.org/10.1248/bpb.b19-00806" target="_blank" >https://doi.org/10.1248/bpb.b19-00806</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1248/bpb.b19-00806" target="_blank" >10.1248/bpb.b19-00806</a>

Result language

angličtina

Original language name

Naloxone Is a Potential Binding Ligand and Activator of the Capsaicin Receptor TRPV1

Original language description

The receptor channel transient receptor potential vanilloid 1 (TRPV1) functions as a sensor of noxious heat and various chemicals. There is increasing evidence for a crosstalk between TRPV1 and opioid receptors. Here we investigated the effect of the prototypical TRPV1 agonist capsaicin and selected opioid ligands on TRPV1 movement in the plasma membrane and intracellular calcium levels in HEK293 cells expressing TRPV1 tagged with cyan fluorescent protein (CFP). We observed that lateral mobility of TRPV1 increased after treatment of cells with capsaicin or naloxone (a nonselective opioid receptor antagonist) but not with DAMGO (a μ-opioid receptor agonist). Interestingly, both capsaicin and naloxone, unlike DAMGO, elicited intracellular calcium responses. The increased TRPV1 movement and calcium influx induced by capsaicin and naloxone were blocked by the TRPV1 antagonist capsazepine. The ability of naloxone to directly interact with TRPV1 was further corroborated by [3H]-naloxone binding. In conclusion, our data suggest that besides acting as an opioid receptor antagonist, naloxone may function as a potential TRPV1 agonist.

Czech name

—

Czech description

—

Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

10608 - Biochemistry and molecular biology

Project

—

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2020

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Biological & Pharmaceutical Bulletin

ISSN

0918-6158

e-ISSN

—

Volume of the periodical

43

Issue of the periodical within the volume

5

Country of publishing house

JP - JAPAN

Number of pages

5

Pages from-to

908-912

UT code for WoS article

000567167900020

EID of the result in the Scopus database

2-s2.0-85084328535