Počet záznamů: 1
Naloxone Is a Potential Binding Ligand and Activator of the Capsaicin Receptor TRPV1
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SYSNO ASEP 0532415 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Naloxone Is a Potential Binding Ligand and Activator of the Capsaicin Receptor TRPV1 Tvůrce(i) Melkes, B. (CZ)
Marková, V. (CZ)
Hejnová, L. (CZ)
Marek, Aleš (UOCHB-X) RID, ORCID
Novotný, J. (CZ)Zdroj.dok. Biological & Pharmaceutical Bulletin. - : Pharmacetical Society of Japan - ISSN 0918-6158
Roč. 43, č. 5 (2020), s. 908-912Poč.str. 5 s. Jazyk dok. eng - angličtina Země vyd. JP - Japonsko Klíč. slova naloxone ; transient receptor potential vanilloid 1 ; receptor lateral mobility ; fluorescence recovery after photobleaching ; calcium Vědní obor RIV CE - Biochemie Obor OECD Biochemistry and molecular biology Způsob publikování Open access Institucionální podpora UOCHB-X - RVO:61388963 UT WOS 000567167900020 EID SCOPUS 85084328535 DOI 10.1248/bpb.b19-00806 Anotace 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. Pracoviště Ústav organické chemie a biochemie Kontakt asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Jana Procházková, Tel.: 220 183 418 Rok sběru 2021 Elektronická adresa https://doi.org/10.1248/bpb.b19-00806
Počet záznamů: 1