Literature DB >> 28527758

Modulation of CB1 cannabinoid receptor by allosteric ligands: Pharmacology and therapeutic opportunities.

Leepakshi Khurana1, Ken Mackie2, Daniele Piomelli3, Debra A Kendall4.   

Abstract

Cannabinoid pharmacology has been intensely studied because of cannabis' pervasive medicinal and non-medicinal uses as well as for the therapeutic potential of cannabinoid-based drugs for the treatment of pain, anxiety, substance abuse, obesity, cancer and neurodegenerative disorders. The identification of allosteric modulators of the cannabinoid receptor 1 (CB1) has given a new direction to the development of cannabinoid-based therapeutics due to the many advantages offered by targeting allosteric site(s). Allosteric receptor modulators hold potential to develop subtype-specific and pathway-specific therapeutics. Here we briefly discuss the first-generation of allosteric modulators of CB1 receptor, their structure-activity relationships, signaling pathways and the allosteric binding site(s) on the CB1 receptor. This article is part of the Special Issue entitled "A New Dawn in Cannabinoid Neurobiology".
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Allosteric modulator; Biased signaling; CB(1); Therapeutic potential

Mesh：

Substances：

Year:  2017        PMID： 28527758      PMCID： PMC5540789          DOI： 10.1016/j.neuropharm.2017.05.018

Source DB:  PubMed          Journal:  Neuropharmacology        ISSN： 0028-3908            Impact factor:   5.250


  83 in total

1.  Effects of the allosteric antagonist 1-(4-chlorophenyl)-3-[3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl]urea (PSNCBAM-1) on CB1 receptor modulation in the cerebellum.

Authors:  Xiaowei Wang; James G Horswill; Benjamin J Whalley; Gary J Stephens
Journal:  Mol Pharmacol       Date:  2010-12-28       Impact factor: 4.436

Review 2.  Allosterism and cannabinoid CB(1) receptors: the shape of things to come.

Authors:  Ruth A Ross
Journal:  Trends Pharmacol Sci       Date:  2007-11       Impact factor: 14.819

3.  A key agonist-induced conformational change in the cannabinoid receptor CB1 is blocked by the allosteric ligand Org 27569.

Authors:  Jonathan F Fay; David L Farrens
Journal:  J Biol Chem       Date:  2012-07-30       Impact factor: 5.157

Review 4.  Functional and structural perspectives on allosteric modulation of GPCRs.

Authors:  Christopher J Langmead; Arthur Christopoulos
Journal:  Curr Opin Cell Biol       Date:  2013-12-22       Impact factor: 8.382

5.  Small-molecule agonists for the glucagon-like peptide 1 receptor.

Authors:  Lotte Bjerre Knudsen; Dan Kiel; Min Teng; Carsten Behrens; Dilip Bhumralkar; János T Kodra; Jens J Holst; Claus B Jeppesen; Michael D Johnson; Johannes Cornelis de Jong; Anker Steen Jorgensen; Tim Kercher; Jarek Kostrowicki; Peter Madsen; Preben H Olesen; Jacob S Petersen; Fritz Poulsen; Ulla G Sidelmann; Jeppe Sturis; Larry Truesdale; John May; Jesper Lau
Journal:  Proc Natl Acad Sci U S A       Date:  2007-01-09       Impact factor: 11.205

Review 6.  Cannabidiol and epilepsy: Rationale and therapeutic potential.

Authors:  Antonio Leo; Emilio Russo; Maurizio Elia
Journal:  Pharmacol Res       Date:  2016-03-11       Impact factor: 7.658

Review 7.  The Utility of Cannabidiol in the Treatment of Refractory Epilepsy.

Authors:  D S Reddy
Journal:  Clin Pharmacol Ther       Date:  2016-09-29       Impact factor: 6.875

8.  PSNCBAM-1, a novel allosteric antagonist at cannabinoid CB1 receptors with hypophagic effects in rats.

Authors:  J G Horswill; U Bali; S Shaaban; J F Keily; P Jeevaratnam; A J Babbs; C Reynet; P Wong Kai In
Journal:  Br J Pharmacol       Date:  2007-06-25       Impact factor: 8.739

9.  Endogenous vs Exogenous Allosteric Modulators in GPCRs: A dispute for shuttling CB1 among different membrane microenvironments.

Authors:  Mariano Stornaiuolo; Agostino Bruno; Lorenzo Botta; Giuseppe La Regina; Sandro Cosconati; Romano Silvestri; Luciana Marinelli; Ettore Novellino
Journal:  Sci Rep       Date:  2015-10-20       Impact factor: 4.379

10.  Anti-inflammatory lipoxin A4 is an endogenous allosteric enhancer of CB1 cannabinoid receptor.

Authors:  Fabricio A Pamplona; Juliano Ferreira; Octávio Menezes de Lima; Filipe Silveira Duarte; Allisson Freire Bento; Stefânia Forner; Jardel G Villarinho; Luigi Bellocchio; Luigi Bellochio; Carsten T Wotjak; Raissa Lerner; Krisztina Monory; Beat Lutz; Claudio Canetti; Isabelle Matias; João Batista Calixto; Giovanni Marsicano; Marilia Z P Guimarães; Reinaldo N Takahashi
Journal:  Proc Natl Acad Sci U S A       Date:  2012-11-12       Impact factor: 11.205
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  27 in total

Review 1.  The cannabinoid system and pain.

Authors:  Stephen G Woodhams; Victoria Chapman; David P Finn; Andrea G Hohmann; Volker Neugebauer
Journal:  Neuropharmacology       Date:  2017-06-15       Impact factor: 5.250

2.  Pyrimidinyl Biphenylureas Act as Allosteric Modulators to Activate Cannabinoid Receptor 1 and Initiate β-Arrestin-Dependent Responses.

Authors:  Caitlin A D Jagla; Caitlin E Scott; Yaliang Tang; Changjiang Qiao; Gabriel E Mateo-Semidey; Guillermo A Yudowski; Dai Lu; Debra A Kendall
Journal:  Mol Pharmacol       Date:  2018-10-15       Impact factor: 4.436

3.  Prediction of Orthosteric and Allosteric Regulations on Cannabinoid Receptors Using Supervised Machine Learning Classifiers.

Authors:  Yuemin Bian; Yankang Jing; Lirong Wang; Shifan Ma; Jaden Jungho Jun; Xiang-Qun Xie
Journal:  Mol Pharm       Date:  2019-05-03       Impact factor: 4.939

4.  Development of 3-(4-Chlorophenyl)-1-(phenethyl)urea Analogues as Allosteric Modulators of the Cannabinoid Type-1 Receptor: RTICBM-189 is Brain Penetrant and Attenuates Reinstatement of Cocaine-Seeking Behavior.

Authors:  Thuy Nguyen; Thomas F Gamage; David B Finlay; Ann M Decker; Tiffany L Langston; Daniel Barrus; Michelle Glass; Jun-Xu Li; Terry P Kenakin; Yanan Zhang
Journal:  J Med Chem       Date:  2021-12-20       Impact factor: 7.446

5.  Positive allosteric modulation of the cannabinoid type-1 receptor (CB1R) in periaqueductal gray (PAG) antagonizes anti-nociceptive and cellular effects of a mu-opioid receptor agonist in morphine-withdrawn rats.

Authors:  Udita Datta; Leslie K Kelley; Jason W Middleton; Nicholas W Gilpin
Journal:  Psychopharmacology (Berl)       Date:  2020-08-28       Impact factor: 4.530

6.  CB1 positive allosteric modulation attenuates Δ9-THC withdrawal and NSAID-induced gastric inflammation.

Authors:  K R Trexler; M L Eckard; S G Kinsey
Journal:  Pharmacol Biochem Behav       Date:  2018-12-28       Impact factor: 3.533

7.  Cannabinoids and Pain: Weeding Out Undesired Effects With a Novel Approach to Analgesia.

Authors:  Joao P De Aquino; David A Ross
Journal:  Biol Psychiatry       Date:  2018-11-15       Impact factor: 13.382

8.  Structure of an allosteric modulator bound to the CB1 cannabinoid receptor.

Authors:  Zhenhua Shao; Wei Yan; Karen Chapman; Karthik Ramesh; Aaron J Ferrell; Jie Yin; Xuehui Wang; Qingping Xu; Daniel M Rosenbaum
Journal:  Nat Chem Biol       Date:  2019-10-28       Impact factor: 15.040

Review 9.  Positron Emission Tomography Imaging of the Endocannabinoid System: Opportunities and Challenges in Radiotracer Development.

Authors:  Lu Hou; Jian Rong; Ahmed Haider; Daisuke Ogasawara; Cassis Varlow; Michael A Schafroth; Linjing Mu; Jiefeng Gan; Hao Xu; Christopher J Fowler; Ming-Rong Zhang; Neil Vasdev; Simon Ametamey; Benjamin F Cravatt; Lu Wang; Steven H Liang
Journal:  J Med Chem       Date:  2020-12-30       Impact factor: 7.446

10.  Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids.

Authors:  Thuy Nguyen; Thomas F Gamage; Ann M Decker; David B Finlay; Tiffany L Langston; Daniel Barrus; Michelle Glass; Danni L Harris; Yanan Zhang
Journal:  Bioorg Med Chem       Date:  2021-05-12       Impact factor: 3.461
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