Results 241 to 250 of about 247,999 (295)

Benzodiazepine Dependence: Clinical and Molecular Aspects, Preventive Strategies and Therapeutic Approaches. [PDF]

Int J Mol Sci
Navarrete F, Marín-Mayor M, Martínez-Hostyn L, Rubio G, Manzanares J.   +4 more
europepmc   +1 more source

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C-3 Amido-indole cannabinoid receptor modulators.

Bioorganic & Medicinal Chemistry Letters, 2002
C-3 Amido-indoles were found to selectively bind to the CB2 receptor. SAR studies led to optimized compounds with excellent in vivo potency against LPS induced TNF-alpha release in murine models of cytokine production.
J. Hynes, K. Leftheris, Hongui Wu, C. Pandit, Ping Chen, Derek J. Norris, Bang-Chi Chen, R. Zhao, P. Kiener, Xiaorong Chen, Lori A Turk, Vina Patil-Koota, Kathleen M. Gillooly, D. Shuster, K. McIntyre   +14 more
semanticscholar   +3 more sources

Enantiospecific Allosteric Modulation of Cannabinoid 1 Receptor.

ACS Chemical Neuroscience, 2017
The cannabinoid 1 receptor (CB1R) is one of the most widely expressed metabotropic G protein-coupled receptors in brain, and its participation in various (patho)physiological processes has made CB1R activation a viable therapeutic modality. Adverse psychotropic effects limit the clinical utility of CB1R orthosteric agonists and have promoted the search
R. Laprairie, P. Kulkarni, J. Deschamps, M. Kelly, D. Janero, M. Cascio, Lesley A. Stevenson, R. Pertwee, T. Kenakin, E. Denovan‐Wright, G. Thakur   +10 more
semanticscholar   +3 more sources

Molecular mechanism of allosteric modulation for the cannabinoid receptor CB1

Nature Chemical Biology, 2022
Given the promising clinical value of allosteric modulators of G protein-coupled-receptors (GPCRs), mechanistic understanding of how these modulators alter GPCR function is of significance. Here, we report the crystallographic and cryo-electron microscopy structures of the cannabinoid receptor CB1 bound to the positive allosteric modulator (PAM) ZCZ011.
Xin Yang, Xuehui Wang, Zheng Xu, Chao Wu, Yangli Zhou, Yifei Wang, Guifeng Lin, Kan Li, Ming Wu, Anjie Xia, Jingming Liu, Lin Cheng, Jun Zou, Wei Yan, Zhenhua Shao, Shengyong Yang   +15 more
semanticscholar   +3 more sources

Allosteric Modulation of the Cannabinoid CB1 Receptor

, 2017
Erin E Cawston, M. Hunter, M. Glass
semanticscholar   +2 more sources

GABAA receptors modulate cannabinoid-evoked hypothermia

Pharmacology Biochemistry and Behavior, 2004
Cannabinoids evoke hypothermia by stimulating central CB(1) receptors. GABA induces hypothermia via GABA(A) or GABA(B) receptor activation. CB(1) receptor activation increases GABA release in the hypothalamus, a central locus for thermoregulation, suggesting that cannabinoid and GABA systems may be functionally linked in body temperature regulation. We
S M, Rawls, R J, Tallarida, D A, Kon, E B, Geller, Martin W, Adler   +4 more
openaire   +2 more sources

Allosteric Modulation of the Cannabinoid CB1 Receptor

Molecular Pharmacology, 2005
We investigated the pharmacology of three novel compounds, Org 27569 (5-chloro-3-ethyl-1H-indole-2-carboxylic acid [2-(4-piperidin-1-yl-phenyl)-ethyl]-amide), Org 27759 (3-ethyl-5-fluoro-1H-indole-2-carboxylic acid [2-94-dimethylamino-phenyl)-ethyl]-amide), and Org 29647 (5-chloro-3-ethyl-1H-indole-2-carboxylic acid (1-benzyl-pyrrolidin-3-yl)-amide, 2 ...
Martin R, Price, Gemma L, Baillie, Adèle, Thomas, Lesley A, Stevenson, Morag, Easson, Richard, Goodwin, Adèle, McLean, Lorraine, McIntosh, Gillian, Goodwin, Glenn, Walker, Paul, Westwood, Julia, Marrs, Fiona, Thomson, Phillip, Cowley, Arthur, Christopoulos, Roger G, Pertwee, Ruth A, Ross   +16 more
openaire   +2 more sources

Selective cannabinoid receptor 2 modulators: a patent review 2009 – present

Expert Opinion on Therapeutic Patents, 2012
The activation of the cannabinoid receptor 2 (CB2) affects a myriad of immune responses from inflammation to neuroprotection, demonstrates analgesic effects and suppresses responses in many animal models of pain. Questions around the involvement of CB1 activation in these effects remain, but efforts have been directed toward the discovery of highly ...
Doris Riether
semanticscholar   +3 more sources