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dc.contributor.authorManning, Jamie J
dc.contributor.authorGreen, Hayley M
dc.contributor.authorGlass, Michelle
dc.contributor.authorFinlay, David B
dc.date.available2021-09-13T01:26:42Z
dc.date.copyright2021-05-13
dc.identifier.citationThis journal article has been publisheden_NZ
dc.identifier.issn1873-7064
dc.identifier.urihttp://hdl.handle.net/10523/12257
dc.description.abstractThe type-1 cannabinoid receptor (CB1) is a promising drug target for a wide range of diseases. However, many existing and novel candidate ligands for CB1 have shown limited therapeutic potential. Indeed, no ligands are currently approved for the clinic except formulations of the phytocannabinoids Δ9-THC and CBD and a small number of analogues. A key limitation of many promising CB1 ligands are their on-target adverse effects, notably including psychoactivity (agonists) and depression/suicidal ideation (inverse agonists). Recent drug development attempts have therefore focussed on altering CB1 signalling profiles in two ways. Firstly, with compounds that enhance or reduce the signalling of endogenous (endo-) cannabinoids, namely allosteric modulators. Secondly, with compounds that probe the capability of selectively targeting specific cellular signalling pathways that may mediate therapeutic effects using biased ligands. This review will summarise the current paradigm of CB1 signalling in terms of the intracellular transduction pathways acted on by the receptor, their endpoints, and the development of compounds to selectively activate these pathways, whether allosterically or via orthosteric bias.en_NZ
dc.language.isoenen_NZ
dc.publisherElsevieren_NZ
dc.relation.ispartofNeuropharmacologyen_NZ
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 International*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/*
dc.subjectCannabinoid Receptoren_NZ
dc.subjectAllosteric Modulationen_NZ
dc.subjectBiasen_NZ
dc.subjectSignal Transductionen_NZ
dc.subjectFunctional Selectivityen_NZ
dc.subjectG protein coupled receptoren_NZ
dc.titlePharmacological Selection of Cannabinoid Receptor Effectors; Signalling, Allosteric Modulation and Biasen_NZ
dc.typeJournal Articleen_NZ
dc.date.updated2021-09-13T01:23:38Z
otago.schoolDepartment of Pharmacology & Toxicologyen_NZ
otago.relation.volume193en_NZ
dc.identifier.doi10.1016/j.neuropharm.2021.108611en_NZ
otago.bitstream.startpage108611en_NZ
otago.openaccessAbstract Only
dc.rights.statementThis version in OUR Archive is the author’s manuscript accepted for publication after peer-review. The published version is: Manning, J. J., Green, H. M., Glass, M., & Finlay, D. B. (2021). Pharmacological selection of cannabinoid receptor effectors: Signalling, allosteric modulation and bias. Neuropharmacology, 193, 108611. https://doi.org/10.1016/j.neuropharm.2021.108611 This OUR Archive version is licensed under Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International https://creativecommons.org/licenses/by-nc-nd/4.0/en_NZ
dc.description.refereedPeer Revieweden_NZ
otago.abstractonly.term242d*
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Attribution-NonCommercial-NoDerivatives 4.0 International
Except where otherwise noted, this item's licence is described as Attribution-NonCommercial-NoDerivatives 4.0 International