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CBD may optimize our ability to fight pain by interacting with receptors involved in the pain response, including serotonin receptors and opioid receptors, Dr. Friedman notes. CBD, which stands ...
Olorinab (APD371) is a drug being developed by Arena Pharmaceuticals for the treatment of gastrointestinal pain associated with Crohn's disease and irritable bowel syndrome. [1] It acts as a potent and selective cannabinoid CB 2 receptor agonist and is claimed to be orally active and peripherally selective.
This fact led to the logical extension that blocking of the cannabinoid receptors might be useful in decreasing appetite and food intake. [11] It was then discovered that the blockage of the CB 1 receptor represented a new pharmacological target. The first specific CB 1 receptor antagonist / inverse agonist was rimonabant, discovered in 1994 ...
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Tedalinab (GRC-10693) is a drug developed by Glenmark Pharmaceuticals for the treatment of osteoarthritis and neuropathic pain, which acts as a potent and selective cannabinoid CB 2 receptor agonist.
Zevaquenabant was described as a third generation cannabinoid receptor 1 (CB1R) antagonist due to its peripheral selectivity and polypharmacology. [1] It acts as a peripherally selective inverse agonist of the cannabinoid receptor 1 and an inducible nitric oxide synthase (iNOS) inhibitor.
It acts as an antagonist of the CB 1 receptor and agonist of the CB 2 receptor. Concentrations of virodhamine in the human hippocampus are similar to those of anandamide, but they are 2- to 9-fold higher in peripheral tissues that express CB 2. Virodhamine lowers body temperature in mice, demonstrating cannabinoid activity in vivo. [1]
Endogenous cannabinoids are believed to exhibit an analgesic effect on these receptors by limiting both GABA and glutamate of PAG cells that relate to nociceptive input processing, a hypothesis consistent with the finding that anandamide release in the PAG is increased in response to pain-triggering stimuli. [20]
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