Exploring determinants of agonist efficacy at the CB1 cannabinoid receptor: Analogues of the synthetic cannabinoid receptor agonist EG-018.

Cannabinoid Receptor Agonists / chemical synthesis Carbazoles / chemical synthesis Cyclic AMP / metabolism GTP-Binding Proteins / metabolism HEK293 Cells Humans Naphthalenes / chemical synthesis Receptor, Cannabinoid, CB1 / agonists Signal Transduction / drug effects Structure-Activity Relationship
CB1 receptor EG-018 cannabinoids signal transduction structure-activity relationships

Journal

Pharmacology research & perspectives
ISSN: 2052-1707
Titre abrégé: Pharmacol Res Perspect
Pays: United States
ID NLM: 101626369

Informations de publication

Date de publication:
02 2022
Historique:
received: 16 11 2021
accepted: 19 11 2021
entrez: 18 1 2022
pubmed: 19 1 2022
medline: 25 2 2022
Statut: ppublish

Résumé

Neutral antagonists of GPCRs remain relatively rare-indeed, a large majority of GPCR antagonists are actually inverse agonists. The synthetic cannabinoid receptor agonist (SCRA) EG-018 was recently reported as a low efficacy cannabinoid receptor agonist. Here we report a comparative characterization of EG-018 and 13 analogues along with extant putative neutral antagonists of CB

Identifiants

DOI: 10.1002/prp2.901 PMID: 35041297 PMC: PMC8929370
pubmed: 35041297
doi: 10.1002/prp2.901
pmc: PMC8929370
doi:

Substances chimiques

Cannabinoid Receptor Agonists 0
Carbazoles 0
Naphthalenes 0
Receptor, Cannabinoid, CB1 0
EG-018 5G2788GL5G
Cyclic AMP E0399OZS9N
GTP-Binding Proteins EC 3.6.1.-

Types de publication

Journal Article Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

e00901

Subventions

Organisme : NIDA NIH HHS
ID : R01 DA040693
Pays : United States
Organisme : NIDA NIH HHS
ID : R01 DA040460
Pays : United States
Organisme : NIDA NIH HHS
ID : K01 DA045752
Pays : United States

Informations de copyright

© 2022 The Authors. Pharmacology Research & Perspectives published by John Wiley & Sons Ltd, British Pharmacological Society and American Society for Pharmacology and Experimental Therapeutics.

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Auteurs

David B Finlay (DB)

Department of Pharmacology and Toxicology, School of Biomedical Sciences, University of Otago, Dunedin, New Zealand.
ORCID: 0000-0002-3160-2931

Thuy Nguyen (T)

RTI International, Research Triangle Park, North Carolina, USA.

Thomas F Gamage (TF)

RTI International, Research Triangle Park, North Carolina, USA.

Shuli Chen (S)

Department of Pharmacology and Toxicology, School of Biomedical Sciences, University of Otago, Dunedin, New Zealand.

Daniel G Barrus (DG)

RTI International, Research Triangle Park, North Carolina, USA.

Purvi R Patel (PR)

RTI International, Research Triangle Park, North Carolina, USA.

Brian F Thomas (BF)

RTI International, Research Triangle Park, North Carolina, USA.

Jenny L Wiley (JL)

RTI International, Research Triangle Park, North Carolina, USA.

Yanan Zhang (Y)

RTI International, Research Triangle Park, North Carolina, USA.

Michelle Glass (M)

Department of Pharmacology and Toxicology, School of Biomedical Sciences, University of Otago, Dunedin, New Zealand.

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Hormones, substituts d'hormones et antagonistes d'hormones › Hormones › Modulateurs des récepteurs de cannabinoïdes › Agonistes des récepteurs de cannabinoïdes › Exploring determinants of agonist efficacy at...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérocycliques 3 noyaux › Carbazoles › Exploring determinants of agonist efficacy at...
questionsmedicales.fr › Acides nucléiques, nucléotides et nucléosides › Nucléotides › Ribonucléotides › Nucléotides adényliques › AMP cyclique › Exploring determinants of agonist efficacy at...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines et peptides de signalisation intracellulaire › Protéines G › Exploring determinants of agonist efficacy at...
questionsmedicales.fr › Cellules › Cellules épithéliales › Cellules HEK293 › Exploring determinants of agonist efficacy at...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Exploring determinants of agonist efficacy at...
questionsmedicales.fr › Composés polycycliques › Hydrocarbures aromatiques polycycliques › Naphtalènes › Exploring determinants of agonist efficacy at...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs couplés aux protéines G › Récepteurs de cannabinoïdes › Récepteur cannabinoïde de type CB1 › Exploring determinants of agonist efficacy at...
questionsmedicales.fr › Phénomènes physiologiques cellulaires › Transduction du signal › Exploring determinants of agonist efficacy at...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Exploring determinants of agonist efficacy at...