Results 1 to 10 of about 10,682 (172)

Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists

Bioorganic & Medicinal Chemistry Letters, 2007
Optimization of the biological activity for 5,6-diarylpyridines as CB1 receptor inverse agonists is described. Food intake and pharmacokinetic evaluation of 3f and 15c indicate that these compounds are effective orally active modulators of CB1.
Christina B, Madsen-Duggan, John S, Debenham, Thomas F, Walsh, Richard B, Toupence, Song X, Huang, Junying, Wang, Xinchun, Tong, Julie, Lao, Tung M, Fong, Marie-Therese, Schaeffer, Jing Chen, Xiao, Cathy R-R C, Huang, Chun-Pyn, Shen, D Sloan, Stribling, Lauren P, Shearman, Alison M, Strack, D Euan, MacIntyre, Lex H T, Van der Ploeg, Mark T, Goulet   +18 more
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Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain

Bioorganic & Medicinal Chemistry Letters, 2012
Novel, low brain penetrant, orally bioavailable CB1 receptor agonists were designed starting from a mature lead series of potent brain penetrant CB1 receptor agonists. Increasing the calculated polar surface area was found to be a good strategy for reducing brain penetration whilst retaining drug-like properties.
Julia M, Adam, John K, Clark, Keneth, Davies, Kathryn, Everett, Ruth, Fields, Stuart, Francis, Fiona, Jeremiah, Takao, Kiyoi, Maurice, Maidment, Angus, Morrison, Paul, Ratcliffe, Alan, Prosser, Jurgen, Schulz, Grant, Wishart, James, Baker, Susan, Boyce, Robert, Campbell, Jean E, Cottney, Maureen, Deehan, Iain, Martin   +19 more
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AM630 is an inverse agonist at the human cannabinoid CB1 receptor

Life Sciences, 1998
The present investigation examines WIN 55,212-2 and AM630 at the cloned human cannabinoid CB1 receptor stably expressed in Chinese hamster ovary (CHO) cells. The effect of various concentrations of WIN 55,212-2 and AM630 on basal [35S]GTPgammaS binding to cell membranes was determined.
R S, Landsman, A, Makriyannis, H, Deng, P, Consroe, W R, Roeske, H I, Yamamura   +5 more
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SR141716A is an inverse agonist at the human cannabinoid CB1 receptor

European Journal of Pharmacology, 1997
The effects of R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4- benzoxazin-yl]-(1-napthalenyl)methanone mesylate (WIN 55,212-2) and N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-3-pyrazo le-carboxamide (SR141716A) on guanosine-5'-O-(3-[35S]thio)triphosphate ([35S]GTPgammaS) binding to membranes isolated from ...
R S, Landsman, T H, Burkey, P, Consroe, W R, Roeske, H I, Yamamura   +4 more
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Relative efficacies of cannabinoid CB1 receptor agonists in the mouse brain

European Journal of Pharmacology, 1997
We measured (-)-5-(1,1-dimethylheptyl)-2-[5-hydroxy-2-(3-hydroxypropyl)cyclohe xyl]-phenol (CP 55,940)-, (-)11-OH-delta8-tetrahydrocannabinol-dimethylheptyl (HU-210)-, anandamide- and delta9-tetrahydrocannabinol-stimulated G protein activation in mouse brain using the [35S]GTPgammaS functional assay.
T H, Burkey, R M, Quock, P, Consroe, F J, Ehlert, Y, Hosohata, W R, Roeske, H I, Yamamura   +6 more
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Discovery of a novel class of selective human CB1 inverse agonists

Bioorganic & Medicinal Chemistry Letters, 2008
Ligand-based virtual screening led to the discovery of a new class of potent inverse agonists of the human cannabinoid receptor 1, hCB(1), which are selective versus hCB(2). These CB(1) ligands present intriguing departures from a classical CB(1) antagonist pharmacophore. Elements of SAR are discussed in this context.
Nicolas, Foloppe, Nicola H, Allen, Carol H, Bentley, Teresa D, Brooks, Guy, Kennett, Antony R, Knight, Stefania, Leonardi, Anil, Misra, Nathaniel J T, Monck, Daniel M, Sellwood   +9 more
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Alterations in behavioral flexibility by cannabinoid CB1 receptor agonists and antagonists

Psychopharmacology, 2006
Cannabinoid CB1 receptors are expressed in the prefrontal cortex, but their role in mediating executive functions such as behavioral flexibility is unclear.The present study examined the effect of pharmacological activation or blockade of the cannabinoid CB1 receptors on behavioral flexibility using a strategy set-shifting task conducted on a cross ...
Matthew N, Hill, Larissa M, Froese, Anna C, Morrish, Jane C, Sun, Stan B, Floresco   +4 more
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Induction of CB1 cannabinoid receptor by inflammation in primary afferent neurons facilitates antihyperalgesic effect of peripheral CB1 agonist

Pain, 2006
Cannabinoids act on various regions in the nervous system to modulate neuronal activity including nociception. Here, we investigated CB1 receptor expression in primary afferent neurons in the dorsal root ganglion (DRG) and the efficacy of a local (intraplantar) application of the selective CB1 agonist, 2-arachidonyl-2-chloroethylamide (ACEA), on ...
Fumimasa, Amaya, Goshun, Shimosato, Yasuhiko, Kawasaki, Satoru, Hashimoto, Yoshifumi, Tanaka, Ru-Rong, Ji, Masaki, Tanaka   +6 more
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The synthetic CB1 cannabinoid receptor selective agonists: Putative medical uses and their legalization

Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2021
More than 500 molecules have been identified as components of Cannabis sativa (C. sativa), of which the most studied is Δ9-tetrahydrocannabinol (Δ9-THC). Several studies have suggested that Δ9-THC exerts diverse biological effects, ranging from fragmentation of DNA to behavioral disruptions.
Astrid, Coronado-Álvarez, Karen, Romero-Cordero, Lorena, Macías-Triana, Agnes, Tatum-Kuri, Alba, Vera-Barrón, Henning, Budde, Sérgio, Machado, Tetsuya, Yamamoto, Claudio, Imperatori, Eric, Murillo-Rodríguez   +9 more
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Recent CB1 cannabinoid receptor antagonists and inverse agonists

Drug Development Research, 2009
AbstractAntagonists or inverse agonists of the cannabinoid CB1 receptor (CB1R) reported from the 2006–2007 period are reviewed. The compounds are either variations of the archetypical cannabinoid CB1 inverse agonist rimonabant (SR141716) or are other structures less obviously related to the archetype.
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