Results 31 to 40 of about 247,667 (242)

Potential of Cannabinoid Receptor Ligands as Treatment for Substance Use Disorders

CNS Drugs, 2019
Substance use disorder (SUD) is a major public health crisis worldwide, and effective treatment options are limited. During the past 2 decades, researchers have investigated the impact of a variety of pharmacological approaches to treat SUD, one of which
E. Galaj, Z. Xi
semanticscholar   +1 more source

The development and therapeutic potential of classical and next-generation cannabinoid ligands

Pharmacological Research
The endogenous cannabinoid system (ECS) is a complex network that plays a crucial role in various physiological processes, and its modulation through cannabinoid ligands has garnered significant interest in pharmacological research. Cannabinoid receptors,
Verónica Muñoz-Canales, Bellinda Benhamú, Mar Martín-Fontecha, Henar Vázquez-Villa, Silvia Ortega-Gutiérrez   +4 more
doaj   +1 more source

Indomethacin Enhances Type 1 Cannabinoid Receptor Signaling

Frontiers in Molecular Neuroscience, 2019
In addition to its known actions as a non-selective cyclooxygenase (COX) 1 and 2 inhibitor, we hypothesized that indomethacin can act as an allosteric modulator of the type 1 cannabinoid receptor (CB1R) because of its shared structural features with the ...
Robert B. Laprairie, Robert B. Laprairie, Kawthar A. Mohamed, Ayat Zagzoog, Melanie E. M. Kelly, Melanie E. M. Kelly, Lesley A. Stevenson, Roger Pertwee, Eileen M. Denovan-Wright, Ganesh A. Thakur   +9 more
doaj   +1 more source

Allosteric Modulation of Cannabinoid Receptor 1—Current Challenges and Future Opportunities

International Journal of Molecular Sciences, 2019
The cannabinoid receptor type 1 (CB1R), a G protein-coupled receptor (GPCR), plays an essential role in the control of many physiological processes such as hunger, memory loss, gastrointestinal activity, catalepsy, fear, depression, and chronic pain ...
S. Hryhorowicz, M. Kaczmarek-Ryś, A. Andrzejewska, Klaudia Staszak, M. Hryhorowicz, A. Korcz, R. Słomski   +6 more
semanticscholar   +1 more source

Design, synthesis and biological evaluation of novel orthosteric-allosteric ligands of the cannabinoid receptor type 2 (CB2R)

Frontiers in Chemistry, 2022
It is well known that G protein–coupled receptors (GPCRs) assume multiple active states. Orthosteric ligands and/or allosteric modulators can preferentially stabilize specific conformations, giving rise to pathway-biased signaling.
Rebecca Ferrisi, Francesca Gado, Francesca Gado, Beatrice Polini, Caterina Ricardi, Kawthar A. Mohamed, Lesley A. Stevenson, Gabriella Ortore, Simona Rapposelli, Giuseppe Saccomanni, Roger G. Pertwee, Robert B. Laprairie, Robert B. Laprairie, Clementina Manera, Clementina Manera, Grazia Chiellini, Grazia Chiellini   +16 more
doaj   +1 more source

Cannabinoid modulation of cortical adrenergic receptors and transporters [PDF]

Journal of Neuroscience Research, 2009
AbstractWe previously reported that administration of the synthetic cannabinoid agonist WIN 55,212‐2 causes an increase in norepinephrine (NE) efflux in the frontal cortex (FC). The present study examined the expression levels of α2‐ and β1‐adrenergic receptors (ARs) as well as the norepinephrine transporter (NET) in the FC of rats following exposure ...
B A S, Reyes, J C, Rosario, P M T, Piana, E J, Van Bockstaele   +3 more
openaire   +2 more sources

The type 1 cannabinoid receptor positive allosteric modulators GAT591 and GAT593 reduce spike-and-wave discharges in Genetic Absence Epilepsy Rats from Strasbourg

IBRO Neuroscience Reports, 2022
Childhood absence epilepsy (CAE) is a non-convulsive seizure disorder primarily in children characterized by absence seizures. Absence seizures consist of 2.5–5 Hz spike-and-wave discharges (SWDs) detectable using electroencephalography (EEG).
Dan L. McElroy, Andrew J. Roebuck, Quentin Greba, Sumanta Garai, Asher L. Brandt, Orhan Yilmaz, Stuart M. Cain, Terrance P. Snutch, Ganesh A. Thakur, Robert B. Laprairie, John G. Howland   +10 more
doaj   +1 more source

An Autonomous Cannabinoid System in Islets of Langerhans

Frontiers in Endocrinology, 2021
While endocannabinoids (ECs) and cannabis were primarily studied for their nervous system effects, it is now clear that ECs are also produced in the periphery where they regulate several physiological processes, including energy storage, glucose and ...
Kanikkai Raja Aseer, Josephine M. Egan
doaj   +1 more source

Modulation of CB1 Cannabinoid Receptor by Allosteric Ligands: Pharmacology and Therapeutic Opportunities

Neuropharmacology, 2017
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 ...
Leepakshi Khurana, K. Mackie, D. Piomelli, D. Kendall   +3 more
semanticscholar   +1 more source

Distinct Binding Mechanisms for Allosteric Sodium Ion In Cannabinoid Receptors

bioRxiv, 2021
The therapeutical potential of Cannabinoid receptors is not fully explored due to psychoactive side-effects and lack of selectivity associated with the orthosteric ligands.
Soumajit Dutta, Balaji Selvam, D. Shukla
semanticscholar   +1 more source