Results 141 to 150 of about 10,682 (172)

Oximes short-acting CB1 receptor agonists

Bioorganic & Medicinal Chemistry, 2018
New oximes short-acting CB1 agonists were explored by the introduction of an internal oxime and polar groups at the C3 alkyl tail of Δ8-THC. The scope of the research was to drastically alter two important physicochemical properties hydrophobicity (log P) and topological surface area (tPSA) of the compound, which play a critical role in tissue ...
Michael S. Malamas, Jimit Girish Raghav, Xiaoyu Ma, Chandrashekhar Honrao, JodiAnne T. Wood, Othman Benchama, Han Zhou, Srikrishnan Mallipeddi, Alexandros Makriyannis   +8 more
openaire   +4 more sources

Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists

Bioorganic & Medicinal Chemistry Letters, 2005
Structure-activity relationship studies directed toward the optimization of 4,5-diarylimidazole-2-carboxamide analogs as human CB1 receptor inverse agonists resulted in the discovery of the two amide derivatives 24a and b (hCB1 IC50 = 6.1 and 4.0 nM) which also demonstrated efficacy in overnight feeding studies in the rat for reduction in both food ...
Christopher W, Plummer, Paul E, Finke, Sander G, Mills, Junying, Wang, Xinchun, Tong, George A, Doss, Tung M, Fong, Julie Z, Lao, Marie-Therese, Schaeffer, Jing, Chen, Chun-Pyn, Shen, D Sloan, Stribling, Lauren P, Shearman, Alison M, Strack, Lex H T, Van der Ploeg   +14 more
openaire   +4 more sources

Tetrahydroindazole derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists

Bioorganic & Medicinal Chemistry Letters, 2016
A series of potent and receptor-selective cannabinoid-1 (CB1) receptor inverse agonists has been discovered. Peripheral selectivity of the compounds was assessed by a mouse tissue distribution study, in which the concentrations of a test compound in both plasma and brain were measured.
Jay M, Matthews, James J, McNally, Peter J, Connolly, Mingde, Xia, Bin, Zhu, Shawn, Black, Cailin, Chen, Cuifen, Hou, Yin, Liang, Yuting, Tang, Mark J, Macielag   +10 more
openaire   +4 more sources

Aminopyrazine CB1 receptor inverse agonists

Bioorganic & Medicinal Chemistry Letters, 2008
A series of 5,6-diaryl-2-amino-pyrazines were prepared and found to have antagonist-like properties at the CB1 receptor. Subsequent SAR studies optimized both receptor potency and drug-like properties including solubility and Cytochrome-P450 inhibition potential.
David J, Wustrow, George D, Maynard, Jun, Yuan, He, Zhao, Jianmin, Mao, Qin, Guo, Mark, Kershaw, Jack, Hammer, Robbin M, Brodbeck, Kristen E, Near, Dan, Zhou, David S, Beers, Bertrand L, Chenard, James E, Krause, Alan J, Hutchison   +14 more
openaire   +2 more sources

Cannabinoid 1 (CB1) Receptor - Pharmacology, Role in Pain and Recent Developments in Emerging CB1 Agonists

CNS & Neurological Disorders - Drug Targets, 2011
Cannabinoids are antinociceptive in animal models of acute pain, tissue injury and nerve injury induced nociception and act via their cognate receptors, cannabinoid receptor 1 and 2. This review examines the underlying biology of the endocannabinoids and behavioural, neurophysiological, neuroanatomical evidence supporting the notion of pain modulation ...
Rashmi, Talwar, Vijay Kumar, Potluri
openaire   +2 more sources

Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists

Bioorganic & Medicinal Chemistry Letters, 2005
Structure-activity relationship studies for two series of 2-benzyloxy-5-(4-chlorophenyl)-6-(2,4-dichlorophenyl)pyridines having either a 3-cyano or 3-carboxamide moiety resulted in the preparation of the 2-(3,4-difluorobenzyloxy)-3-nitrile analog 10d and the 2-(3,4-difluorobenzyloxy)-3-(N-propylcarboxamide) analog 16c, (hCB1 IC(50)=1.3 and 1.7 nM ...
Laura C, Meurer, Paul E, Finke, Sander G, Mills, Thomas F, Walsh, Richard B, Toupence, John S, Debenham, Mark T, Goulet, Junying, Wang, Xinchun, Tong, Tung M, Fong, Julie, Lao, Marie-Therese, Schaeffer, Jing, Chen, Chun-Pyn, Shen, D, Sloan Stribling, Lauren P, Shearman, Alison M, Strack, Lex H T, Van der Ploeg   +17 more
openaire   +3 more sources

CB1 receptor inverse agonist pharmacotherapy for metabolic disorders

Drug Development Research, 2009
AbstractThe cannabinoid‐1 receptor (CB1R) has been implicated in the control of energy balance based on its anatomical localization, the interaction among the endocannabinoid system and other transmitter systems, and the appetite‐enhancing effect of tetrahydrocannabinol.
Tung M. Fong, Carol Addy, Ngozi Erondu, Steven B. Heymsfield   +3 more
openaire   +1 more source

Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists

Bioorganic & Medicinal Chemistry Letters, 2011
Novel 3-(1H-indol-3-yl)-1,2,4-oxadiazoles and -thiadiazoles were synthesized and found to be potent CB1 cannabinoid receptor agonists. The oral bioavailability of these compounds could be dramatically improved by optimization studies of the side chains attached to the indole and oxadiazole cores, leading to identification of a CB1 receptor agonist with
Kiyoi, Takao, Adam, Julia M, Clark, John K, Davies, Keneth, Easson, Anna-Marie, Edwards, Darren, Feilden, Helen, Fields, Ruth, Francis, Stuart, Jeremiah, Fiona, McArthur, Duncan, Morrison, Angus J, Prosser, Alan, Ratcliffe, Paul D, Schulz, Jurgen, Wishart, Grant, Baker, James, Campbell, Robert, Cottney, Jean E, Deehan, Maureen, Epemolu, Ola, Evans, Louise   +21 more
openaire   +3 more sources