The Endocannabinoid Peptide RVD-Hemopressin Is a TRPV1 Channel Blocker

Author:

Suárez-Suárez Constanza1,González-Pérez Sebastián1,Márquez-Miranda Valeria2,Araya-Duran Ingrid2,Vidal-Beltrán Isabel3,Vergara Sebastián4,Carvacho Ingrid4,Hinostroza Fernando3456

Affiliation:

1. Facultad de Ciencias Agrarias y Forestales, Universidad Católica del Maule, Talca 3460000, Chile

2. Center for Bioinformatics and Integrative Biology (CBIB), Universidad Andrés Bello, Santiago 8370146, Chile

3. Centro de Investigación de Estudios Avanzados del Maule (CIEAM), Vicerrectoría de Investigación y Postgrado, Universidad Católica del Maule, Talca 3460000, Chile

4. Departamento de Medicina Traslacional, Facultad de Medicina, Universidad Católica del Maule, Talca 3460000, Chile

5. Centro de Investigación en Neuropsicología y Neurociencias Cognitivas, Facultad de Ciencias de la Salud, Universidad Católica del Maule, Talca 3460000, Chile

6. Centro para la Investigación Traslacional en Neurofarmacología, Universidad de Valparaíso, Valparaíso 2340000, Chile

Abstract

Neurotransmission is critical for brain function, allowing neurons to communicate through neurotransmitters and neuropeptides. RVD-hemopressin (RVD-Hp), a novel peptide identified in noradrenergic neurons, modulates cannabinoid receptors CB1 and CB2. Unlike hemopressin (Hp), which induces anxiogenic behaviors via transient receptor potential vanilloid 1 (TRPV1) activation, RVD-Hp counteracts these effects, suggesting that it may block TRPV1. This study investigates RVD-Hp’s role as a TRPV1 channel blocker using HEK293 cells expressing TRPV1-GFP. Calcium imaging and patch-clamp recordings demonstrated that RVD-Hp reduces TRPV1-mediated calcium influx and TRPV1 ion currents. Molecular docking and dynamics simulations indicated that RVD-Hp interacts with TRPV1’s selectivity filter, forming stable hydrogen bonds and van der Waals contacts, thus preventing ion permeation. These findings highlight RVD-Hp’s potential as a therapeutic agent for conditions involving TRPV1 activation, such as pain and anxiety.

Funder

ANID

FONDECYT

FOVI

Publisher

MDPI AG

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