Results 201 to 210 of about 6,065 (241)

Safe cannabinoid receptor modulators in sight? [PDF]

Nature Reviews Drug Discovery, 2012
Sarah Crunkhorn
exaly   +2 more sources

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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
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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
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Modulation of cannabinoid receptor signaling by endocannabinoids

2022
Abstract Endocannabinoids (eCBs) are endogenous lipid molecules that activate the cannabinoid receptor 1 (CB1), a G protein coupled receptor (GPCR) that signals primarily through the G i/o family of G proteins to regulate neurotransmitter release.
Kaavya Krishna Kumar, Michael J. Robertson, Elina Thadhani, Haoqing Wang, Carl-Mikael Suomivuori, Alexander S. Powers, Lipin Ji, Spyros P. Nikas, Maria Gerasi, Kiran Vemuri, Ron O. Dror, Asuka Inoue, Alexandros Makriyannis, Georgios Skiniotis, Brian Kobilka   +14 more
openaire   +1 more source

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
Robert B. Laprairie, Pushkar M. Kulkarni, Jeffrey R. Deschamps, Melanie E. M. Kelly, David R. Janero, Maria G. Cascio, Lesley A. Stevenson, Roger G. Pertwee, Terrence P. Kenakin, Eileen M. Denovan-Wright, Ganesh A. Thakur   +10 more
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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
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CB1 Cannabinoid Receptor Activity Is Modulated by the Cannabinoid Receptor Interacting Protein CRIP 1a

Molecular Pharmacology, 2007
The CB1 cannabinoid receptor is a G-protein coupled receptor that has important physiological roles in synaptic plasticity, analgesia, appetite, and neuroprotection. We report the discovery of two structurally related CB1 cannabinoid receptor interacting proteins (CRIP1a and CRIP1b) that bind to the distal C-terminal tail of CB1.
Jason L, Niehaus, Yunguang, Liu, Kathleen T, Wallis, Michaela, Egertová, Sheela G, Bhartur, Somnath, Mukhopadhyay, Shanping, Shi, Hengjun, He, Dana E, Selley, Allyn C, Howlett, Maurice R, Elphick, Deborah L, Lewis   +11 more
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Modulating the affinity and signaling bias of cannabinoid receptor 1 antagonists

Bioorganic Chemistry, 2023
Cannabinoid receptor 1 (CB1) is a G protein-coupled receptor and a therapeutic target for metabolic disorders. Numerous CB1 antagonists have been developed, but their functional selectivities and bias towards G protein or β-arrestin signaling have not been systemically characterized.
Wen-Chi, Hsiao, Kun-Yi, Hsin, Zhong-Wei, Wu, Jen-Shin, Song, Yen-Nan, Yeh, Yan-Fu, Chen, Chia-Hua, Tsai, Pei-Hsuan, Chen, Kak-Shan, Shia, Chun-Ping, Chang, Ming-Shiu, Hung   +10 more
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Roles of cannabinoid CB1 and CB2 receptors in the modulation of psychostimulant responses

Acta Neuropsychiatrica, 2022
AbstractAddiction to psychostimulant drugs, such as cocaine, D-amphetamine, and methamphetamine, is a public health issue that substantially contributes to the global burden of disease. Psychostimulant drugs promote an increase in dopamine levels within the mesocorticolimbic system, which is central to the rewarding properties of such drugs ...
P.H. Gobira, S.R. Joca, F.A. Moreira
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