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RESEARCH ARTICLE
Contents Vol 74(6)

Development of Chromenopyrazole-Based Selective Cannabinoid 2 Receptor Agonists

Sameek Singh A , Ian Liddle B , Christa Macdonald C , Joel D. A. Tyndall A , Michelle Glass D and Andrea J. Vernall https://orcid.org/0000-0001-8056-0726 B E
+ Author Affiliations
- Author Affiliations

A School of Pharmacy, University of Otago, Dunedin 9054, New Zealand.

B Department of Chemistry, University of Otago, Dunedin 9054, New Zealand.

C Department of Pharmacology and Clinical Pharmacology, University of Auckland, Auckland 1142, New Zealand.

D Department of Pharmacology and Toxicology, University of Otago, Dunedin 9054, New Zealand.

E Corresponding author. Email: andrea.vernall@otago.ac.nz

Australian Journal of Chemistry 74(6) 433-442 https://doi.org/10.1071/CH20263
Submitted: 31 August 2020  Accepted: 1 November 2020   Published: 18 November 2020

Abstract

The cannabinoid type 2 receptor (CB2R) is an important therapeutic target for pain and inflammatory disorders. G protein-coupled receptors (GPCRs) are conventionally thought to signal exclusively at the plasma membrane; however, recently this has been challenged by the notion of intracellular signalling receptors. Better understanding of GPCR location requires tools that can differentiate cell surface versus subcellular receptors as well as accessing different parts of the body. Herein, we report the synthesis and pharmacological evaluation of polar chromenopyrazole-based CB2R-selective agonists that contain short peptides that could be useful tools for interrogating CB2R.


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