[HTML][HTML] Activation and signaling mechanism revealed by cannabinoid receptor-Gi complex structures

T Hua, X Li, L Wu, C Iliopoulos-Tsoutsouvas, Y Wang… - Cell, 2020 - cell.com
Human endocannabinoid systems modulate multiple physiological processes mainly
through the activation of cannabinoid receptors CB1 and CB2. Their high sequence …

[HTML][HTML] Structural basis for activation of CB1 by an endocannabinoid analog

K Krishna Kumar, MJ Robertson, E Thadhani… - Nature …, 2023 - nature.com
Endocannabinoids (eCBs) are endogenous ligands of the cannabinoid receptor 1 (CB1), a
G protein-coupled receptor that regulates a number of therapeutically relevant physiological …

Homologation: a versatile molecular modification strategy to drug discovery

LM Lima, MA Alves… - Current Topics in Medicinal …, 2019 - ingentaconnect.com
Homologation is a concept introduced by Gerhard in 1853 to describe a homologous series
in organic chemistry. Since then, the concept has been adapted and used in medicinal …

A systematic review of novel cannabinoids and their targets: insights into the significance of structure in activity

MRA Hamzekalayi, MH Ardakani, Z Moeini… - European Journal of …, 2024 - Elsevier
To provide a comprehensive framework of the current information on the potency and
efficacy of interaction between phyto-and synthetic cannabinoids and their respective …

Cannabinoid-2 agonism with AM2301 mitigates morphine-induced respiratory depression

BM Wiese, E Liktor-Busa, A Levine… - Cannabis and …, 2021 - liebertpub.com
Introduction: An escalating number of fatalities resulting from accidental opioid overdoses
typically attributed to respiratory depression continue to define the opioid epidemic. Opioid …

1-, 2-and 3-AG as substrates of the endocannabinoid enzymes and endogenous ligands of the cannabinoid receptor 1

SI Farah, S Hilston, N Tran, N Zvonok… - Biochemical and …, 2022 - Elsevier
Arachidonoylglycerol (2-AG) is the most potent and abundant endocannabinoid that acts as
a full agonist at the cannabinoid 1 (CB1) and 2 (CB2) receptors. It serves as a substrate for …

Fenton-Inspired C–H Functionalization: Peroxide-Directed C–H Thioetherification

BJ Groendyke, A Modak, SP Cook - The Journal of organic …, 2019 - ACS Publications
Substoichiometric iron mediates the thioetherification of unactivated aliphatic C–H bonds
directed by resident silylperoxides. Upon exposure to a catalytic amount of iron (II) triflate …

Brain penetrant, but not peripherally restricted, synthetic cannabinoid 1 receptor agonists promote morphine-mediated respiratory depression

BM Wiese, E Liktor-Busa, SA Couture… - Cannabis and …, 2022 - liebertpub.com
Introduction: Cannabis acceptance and use continues to rise despite the gaps in knowledge
regarding the mechanisms of cannabinoids and the endocannabinoid system in many …

Chiral Me-2-arachidonoyl Glycerols: The First Potent Endocannabinoid Glyceride Templates with Stability to COX-2

SP Nikas, L Ji, Y Liu, MO Georgiadis… - ACS Medicinal …, 2024 - ACS Publications
2-Arachidonoyl glycerol (2-AG) is the principal endogenously produced ligand for the
cannabinoid CB1 and CB2 receptors (CBRs). The lack of potent and efficacious 2-AG …

Improved cyclobutyl nabilone analogs as potent CB1 receptor agonists

IP Papanastasiou, MO Georgiadis… - European Journal of …, 2022 - Elsevier
In earlier work, we explored the SAR for the C3 side chain pharmacophore in the
hexahydrocannabinol template represented by the drug nabilone, which resulted in the …