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Blockade of Nicotine and Cannabinoid Reinforcement and Relapse by a Cannabinoid CB1-Receptor Neutral Antagonist AM4113 and Inverse Agonist Rimonabant in Squirrel Monkeys

Charles W Schindler
Godfrey H Redhi
Zuzana Justinova
Research18 Feb 2016
Neuropsychopharmacology

Volume: 41, P: 2283-2293
Retraction Note: Crystal structures of agonist-bound human cannabinoid receptor CB₁

Tian Hua
Kiran Vemuri
Zhi-Jie Liu
Amendments and Corrections27 Aug 2025
Nature

Volume: 645, P: 544
Crystal structures of agonist-bound human cannabinoid receptor CB₁

Crystal structures of human CB₁ bound to two cannabinoid agonists reveal key features, including a twin toggle switch and binding pocket reduction, advancing understanding of receptor dynamics and guiding cannabinoid drug design.

Tian Hua
Kiran Vemuri
Zhi-Jie Liu
Research27 Aug 2025
Nature

Volume: 646, P: 754-758
Virtual library docking for cannabinoid-1 receptor agonists with reduced side effects

Tummino et al. dock 74 million molecules against the human cannabinoid-1 receptor to find uM ligands. Optimization led to a nM agonist conferring analgesia with reduced side effects in mice, highlighting its potential as a pain therapeutic and the promise of a structure-based approach.

Tia A. Tummino
Christos Iliopoulos-Tsoutsouvas
Brian K. Shoichet
ResearchOpen Access06 Mar 2025
Nature Communications

Volume: 16, P: 1-19
Structural basis for activation of CB1 by an endocannabinoid analog

This manuscript describes the structure of an endocannabinoid analog-bound CB1 complex and reveals the structural determinants of ligand efficacy. The activation mechanism, unique to CB1, that is exploited by allosteric modulators is also outlined.

Kaavya Krishna Kumar
Michael J. Robertson
Brian Kobilka
ResearchOpen Access09 May 2023
Nature Communications

Volume: 14, P: 1-11
Synthon-based ligand discovery in virtual libraries of over 11 billion compounds

V-SYNTHES, a scalable and computationally cost-effective synthon-based approach to compound screening, identified compounds with a high affinity for CB2 and CB1 in a hierarchical structure-based screen of more than 11 billion compounds.

Arman A. Sadybekov
Anastasiia V. Sadybekov
Vsevolod Katritch
Research15 Dec 2021
Nature

Volume: 601, P: 452-459
A new antibiotic selectively kills Gram-negative pathogens

Bacterial symbionts of animals may contain antibiotics that are particularly suitable for development into therapeutics; one such compound, darobactin, is active against important Gram-negative pathogens both in vitro and in animal models of infection.

Yu Imai
Kirsten J. Meyer
Kim Lewis
Research20 Nov 2019
Nature

Volume: 576, P: 459-464
Structural basis of THC analog activity at the Cannabinoid 1 receptor

Tetrahydrocannabinol (THC) analogs target the cannabinoid receptor CB1 for therapeutic and psychoactive effects. Here, the authors determine spatiotemporal ligand interactions critical for potency, efficacy, off-rates and drug design.

Thor S. Thorsen
Yashraj Kulkarni
David E. Gloriam
ResearchOpen Access08 Jan 2025
Nature Communications

Volume: 16, P: 1-13
Complex 33-beam simulated galactic cosmic radiation exposure impacts cognitive function and prefrontal cortex neurotransmitter networks in male mice

Here the authors show in male mice that acute and chronic complex simulated galactic cosmic radiation exposure differentially reorganized prefrontal cortex neurotransmitter networks in vivo, which was associated with cognitive deficits.

Rajeev I. Desai
Brian D. Kangas
Charles L. Limoli
ResearchOpen Access27 Nov 2023
Nature Communications

Volume: 14, P: 1-18
Author Correction: A new antibiotic selectively kills Gram-negative pathogens

Yu Imai
Kirsten J. Meyer
Kim Lewis
Amendments and Corrections25 Mar 2020
Nature

Volume: 580, P: E3
Endocannabinoids acting at vascular CB₁ receptors mediate the vasodilated state in advanced liver cirrhosis

Sándor Bátkai
Zoltán Járai
George Kunos
Research01 Jul 2001
Nature Medicine

Volume: 7, P: 827-832
RETRACTED ARTICLE: Crystal structures of agonist-bound human cannabinoid receptor CB₁

Crystal structures of the human cannabinoid receptor 1 (CB₁) bound to the agonists AM11542 and AM841 reveal notable structural rearrangements upon receptor activation, and this flexibility may be a common feature among other G-protein-coupled receptors.

Tian Hua
Kiran Vemuri
Zhi-Jie Liu
Research05 Jul 2017
Nature

Volume: 547, P: 468-471
Conformational gating, dynamics and allostery in human monoacylglycerol lipase

Sergiy Tyukhtenko
Xiaoyu Ma
Alexandros Makriyannis
ResearchOpen Access28 Oct 2020
Scientific Reports

Volume: 10, P: 1-16
Effects of Distal Mutations on the Structure, Dynamics and Catalysis of Human Monoacylglycerol Lipase

Sergiy Tyukhtenko
Girija Rajarshi
Alexandros Makriyannis
ResearchOpen Access29 Jan 2018
Scientific Reports

Volume: 8, P: 1-17
Expression, Purification and Characterization of the Human Cannabinoid 1 Receptor

Srikrishnan Mallipeddi
Nikolai Zvonok
Alexandros Makriyannis
ResearchOpen Access13 Feb 2018
Scientific Reports

Volume: 8, P: 1-11
AM6527, a neutral CB1 receptor antagonist, suppresses opioid taking and seeking, as well as cocaine seeking in rodents without aversive effects

Omar Soler-Cedeño
Hannah Alton
Zheng-Xiong Xi
ResearchOpen Access10 Apr 2024
Neuropsychopharmacology

Volume: 49, P: 1678-1688
Inhibition of triple negative breast cancer-associated inflammation and progression by N- acylethanolamine acid amide hydrolase (NAAA)

Othman Benchama
Michael S. Malamas
Hava Karsenty Avraham
ResearchOpen Access23 Dec 2022
Scientific Reports

Volume: 12, P: 1-16
Inhibition of triple negative breast cancer-associated inflammation, tumor growth and brain colonization by targeting monoacylglycerol lipase

Othman Benchama
Sergiy Tyukhtenko
Hava Karsenty Avraham
ResearchOpen Access29 Mar 2022
Scientific Reports

Volume: 12, P: 1-14
Biochemical and Proteomic Characterization of Recombinant Human α/β Hydrolase Domain 6

Christina Miyabe Shields
Nikolai Zvonok
Alexandros Makriyannis
ResearchOpen Access29 Jan 2019
Scientific Reports

Volume: 9, P: 1-12
Cannabinoid CB₁ receptor neutral antagonist AM4113 inhibits heroin self-administration without depressive side effects in rats

Xiang-hu He
Chloe J. Jordan
Zheng-xiong Xi
Research02 Jul 2018
Acta Pharmacologica Sinica

Volume: 40, P: 365-373
Cannabinoid Agonists but not Inhibitors of Endogenous Cannabinoid Transport or Metabolism Enhance the Reinforcing Efficacy of Heroin in Rats

Marcello Solinas
Leigh V Panlilio
Steven R Goldberg
Research04 May 2005
Neuropsychopharmacology

Volume: 30, P: 2046-2057

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