Showing 1-6 of 6 resultados for "sml2710"
Bogna M Ignatowska-Jankowska et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 40(13), 2948-2959 (2015-06-09)
The CB1 receptor represents a promising target for the treatment of several disorders including pain-related disease states. However, therapeutic applications of Δ(9)-tetrahydrocannabinol and other CB1 orthosteric receptor agonists remain limited because of psychoactive side effects. Positive allosteric modulators (PAMs) offer...
Jose Mitjavila et al.
Pharmacological research, 129, 475-481 (2017-11-22)
The cannabinoid signaling system is found throughout the CNS and its involvement in several pathological processes makes it an attractive therapeutic target. Because orthosteric CB1 cannabinoid receptor ligands have undesirable adverse effects there has been great interest in the development...
Kaavya Krishna Kumar et al.
Cell, 176(3), 448-458 (2019-01-15)
Cannabis elicits its mood-enhancing and analgesic effects through the cannabinoid receptor 1 (CB1), a G protein-coupled receptor (GPCR) that signals primarily through the adenylyl cyclase-inhibiting heterotrimeric G protein Gi. Activation of CB1-Gi signaling pathways holds potential for treating a number of...
Noureldin Saleh et al.
Angewandte Chemie (International ed. in English), 57(10), 2580-2585 (2018-01-10)
The cannabinoid CB1 receptor (CB1R) is an abundant metabotropic G-protein-coupled receptor that has been difficult to address therapeutically because of CNS side effects exerted by orthosteric drug candidates. Recent efforts have focused on developing allosteric modulators that target CB1R. Compounds...
Chih-Chung Tseng et al.
Journal of medicinal chemistry, 62(10), 5049-5062 (2019-05-06)
The first generation of CB1 positive allosteric modulators (e.g., ZCZ011) featured a 3-nitroalkyl-2-phenyl-indole structure. Although a small number of drugs include the nitro group, it is generally not regarded as being "drug-like", and this is particularly true for aliphatic nitro...
K R Trexler et al.
Pharmacology, biochemistry, and behavior, 177, 27-33 (2019-01-01)
Recently, multiple compounds have been synthesized that target the allosteric binding site(s) of CB1. These CB1 positive allosteric modulators may capture the benefits of cannabinoid receptor activation without unwanted psychoactive effects, such as sedation. For example, ZCZ011 blocks neuropathic pain...

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