Results 11 to 20 of about 247,999 (295)

Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators [PDF]

Bioorganic & Medicinal Chemistry Letters, 2016
This Letter was supported by the Biotechnology and Biological Sciences Research Council (BBSRC) and the Scottish Universities Life Sciences Alliance (SULSA) in 2011Peer ...
Abdelrahman, Mostafa Hamed, Baillie, Gemma L., Greig, Iain R., Ross, Ruth A., Trembleau, Laurent   +4 more
core   +4 more sources

Metabolic disorders: Safe cannabinoid receptor modulators in sight? [PDF]

Nature Reviews Drug Discovery, 2012
Sarah Crunkhorn
semanticscholar   +4 more sources

Pharmacological Evaluation of Cannabinoid Receptor Modulators Using GRAB_eCB2.0 Sensor. [PDF]

Int J Mol Sci
Cannabinoid receptors CB1R and CB2R are G-protein coupled receptors acted upon by endocannabinoids (eCBs), namely 2-arachidonoylglycerol (2-AG) and N-arachidonoyl ethanolamine (AEA), with unique pharmacology and modulate disparate physiological processes. A genetically encoded GPCR activation-based sensor that was developed recently—GRABeCB2.0—has been
Shivshankar S, Nimely J, Puhl H, Iyer MR.   +3 more
europepmc   +3 more sources

Translational potential of allosteric modulators targeting the cannabinoid CB1 receptor [PDF]

Acta Pharmacologica Sinica, 2018
The cannabinoid type-1 (CB1) receptor, a G-protein-coupled receptor, is an attractive target for drug discovery due to its involvement in many physiological processes. Historically, drug discovery efforts targeting the CB1 receptor have focused on the development of orthosteric ligands that interact with the active site to which endogenous cannabinoids
D. Lu, Sri Sujana Immadi, Zhixing Wu, D. Kendall   +3 more
semanticscholar   +3 more sources

Microglial Cannabinoid CB2 Receptors in Pain Modulation

International Journal of Molecular Sciences, 2023
Pain, especially chronic pain, can strongly affect patients’ quality of life. Cannabinoids ponhave been reported to produce potent analgesic effects in different preclinical pain models, where they primarily function as agonists of Gi/o protein-coupled cannabinoid CB1 and CB2 receptors.
Kangtai Xu, Yifei Wu, Zhuangzhuang Tian, Yuanfan Xu, Chaoran Wu, Zilong Wang   +5 more
openaire   +2 more sources

Endogenous Cannabinoid Receptors Modulate Plasticity at Immature Synapses

Journal of Integrative Neuroscience, 2022
Background: To explore the mechanism of endocannabinoid cannabinoid receptor 1 (CB1) receptor pathway that regulates synaptic plasticity in the dorsal horn of the spinal cord of rats with neuropathic pain at different ages. Methods: Neonatal, juvenile, and adult male sprague dawley (SD) rats were divided into the spinal nerve preservation injury (SNI),
Jie Cheng, Xueling Chen, Hui Xia, Fanli Kong, Li Wang, Liang Zhong, Jiang Wu   +6 more
openaire   +3 more sources

Structural Optimization of the Diarylurea PSNCBAM-1, an Allosteric Modulator of Cannabinoid Receptor 1

Current Therapeutic Research, 2020
: Background: Structure–activity relationship studies improve the pharmacological and pharmacokinetic properties of a lead compound such as PSNCBAM-1, an allosteric modulator of the cannabinoid receptor 1.
Rachel Dopart, Sri Sujana Immadi, Dai Lu, Debra A. Kendall   +3 more
doaj   +1 more source

Pharmacological evaluation of enantiomerically separated positive allosteric modulators of cannabinoid 1 receptor, GAT591 and GAT593

Frontiers in Pharmacology, 2022
Positive allosteric modulation of the type 1 cannabinoid receptor (CB1R) has substantial potential to treat both neurological and immune disorders.
Asher L. Brandt, Sumanta Garai, Ayat Zagzoog, Dow P. Hurst, Lesley A. Stevenson, Roger G. Pertwee, Gregory H. Imler, Patricia H. Reggio, Ganesh A. Thakur, Robert B. Laprairie, Robert B. Laprairie   +10 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

Brain cannabinoid receptor 2: expression, function and modulation [PDF]

Acta Pharmacologica Sinica, 2017
Cannabis sativa (marijuana) is a fibrous flowering plant that produces an abundant variety of molecules, some with psychoactive effects. At least 4% of the world's adult population uses cannabis annually, making it one of the most frequently used illicit drugs in the world. The psychoactive effects of cannabis are mediated primarily through cannabinoid
De-Jie, Chen, Ming, Gao, Fen-Fei, Gao, Quan-Xi, Su, Jie, Wu   +4 more
openaire   +2 more sources