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Papers of the Week


Papers: 12 Mar 2022 - 18 Mar 2022


Pharmacology/Drug Development


2022


Front Mol Biosci


9

Targeting CB2 and TRPV1: Computational Approaches for the Identification of Dual Modulators.

Authors

Morales P, Muller C, Jagerovic N, Reggio PH
Front Mol Biosci. 2022; 9:841190.
PMID: 35281260.

Abstract

Both metabotropic (CBRs) and ionotropic cannabinoid receptors (ICRs) have implications in a range of neurological disorders. The metabotropic canonical CBRs CB1 and CB2 are highly implicated in these pathological events. However, selective targeting at CB2 versus CB1 offers optimized pharmacology due to the absence of psychoactive outcomes. The ICR transient receptor potential vanilloid type 1 (TRPV1) has also been reported to play a role in CNS disorders. Thus, activation of both targets, CB2 and TRPV1, offers a promising polypharmacological strategy for the treatment of neurological events including analgesia and neuroprotection. This brief research report aims to identify chemotypes with a potential dual CB2/TRPV1 profile. For this purpose, we have rationalized key structural features for activation and performed virtual screening at both targets using curated chemical libraries.