Allosteric Modulators of Serotonin Receptors: A Medicinal Chemistry Survey
Abstract Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter regulating numerous physiological functions, and its dysregulation is a crucial component of the…
GPCR
Saturated Cannabinoids: Update on Synthesis Strategies and Biological Studies of These Emerging Cannabinoid Analogs
Abstract Natural and non-natural hexahydrocannabinols (HHC) were first described in 1940 by Adam and in late 2021 arose on the…
Molecular insights into GPCR mechanisms for drugs of abuse
Abstract Substance abuse is on the rise, and while many people may use illicit drugs mainly due to their rewarding…
Role of the Endocannabinoid System in the Regulation of Intestinal Homeostasis
Abstract The maintenance of intestinal homeostasis is fundamentally important to health. Intestinal barrier function and immune regulation are key determinants…
Nanoscale Sub-Compartmentalization of the Dendritic Spine Compartment
Abstract Compartmentalization of the membrane is essential for cells to perform highly specific tasks and spatially constrained biochemical functions in…
Alternative Pre-mRNA Splicing of the Mu Opioid Receptor Gene, OPRM1: Insight into Complex Mu Opioid Actions
Abstract Most opioid analgesics used clinically, including morphine and fentanyl, as well as the recreational drug heroin, act primarily through…
The GPR18 Agonist PSB-KD-107 Exerts Endothelium-Dependent Vasorelaxant Effects
Abstract GPR18 is an orphan GPCR that is activated by the cannabinoid tetrahydrocannabinol (THC). Emerging evidence indicates its involvement in…
CT Findings and Patterns of e-Cigarette or Vaping Product Use-Associated Lung Injury
Abstract Background: e-Cigarette or vaping-induced lung injury (EVALI) causes a spectrum of CT lung injury patterns. Relative frequencies and associations…
Allosteric Modulation of Cannabinoid Receptor 1—Current Challenges and Future Opportunities
Abstract The cannabinoid receptor type 1 (CB1R), a G protein-coupled receptor (GPCR), plays an essential role in the control of…
Targeting Cannabinoid CB2 Receptors in the Central Nervous System. Medicinal Chemistry Approaches with Focus on Neurodegenerative Disorders
Abstract Endocannabinoids activate two types of specific G-protein-coupled receptors (GPCRs), namely cannabinoid CB1 and CB2. Contrary to the psychotropic actions…