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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.
A cannabinoid receptor antagonist, also known simply as a cannabinoid antagonist or as an anticannabinoid, is a type of cannabinoidergic drug that binds to cannabinoid receptors (CBR) and prevents their activation by endocannabinoids. They include antagonists, inverse agonists, and antibodies of CBRs.
An agonist increases the activity of a receptor above its basal level, whereas an inverse agonist decreases the activity below the basal level. The efficacy of a full agonist is by definition 100%, a neutral antagonist has 0% efficacy, and an inverse agonist has < 0% (i.e., negative) efficacy.
Rimonabant is a selective CB 1 receptor blocker and was discovered and developed by Sanofi-Aventis. [6]On 21 June 2006, the European Commission approved the sale of rimonabant in the then-25-member European Union as a prescription drug for use in conjunction with diet and exercise for patients with a body mass index (BMI) greater than 30 kg/m 2, or patients with a BMI greater than 27 kg/m 2 ...
Cannabinoid receptor type 1 (CB 1) receptors are thought to be one of the most widely expressed G αi protein-coupled receptors in the brain. One mechanism through which they function is endocannabinoid-mediated depolarization-induced suppression of inhibition , a very common form of retrograde signaling , in which the depolarization of a ...
In 2006, it was discovered that H4CBD has a binding affinity of 145 nM at the CB1 receptor and potential anti-inflammatory effects independent of its cannabinoid receptor action. [2] In contrast, CBD has been found to bind to the CB1 receptor as an inverse agonist/antagonist with a K i ranging from 3.3 to 4.8 mM. [3] [4]
AM-251 is an inverse agonist at the CB 1 cannabinoid receptor. AM-251 is structurally very close to rimonabant; both are biarylpyrazole cannabinoid receptor antagonists.In AM-251, the p-chloro group attached to the phenyl substituent at C-5 of the pyrazole ring is replaced with a p-iodo group.
GPR55 is activated by the plant cannabinoids Δ 9-THC [12] and the endocannabinoids anandamide, 2-AG and noladin ether in the low nanomolar range. Exocannabinoids such as the synthetic cannabinoid CP-55940 are also able to activate the receptor [12] while the structurally unrelated cannabinoid mimic WIN 55,212-2 fails to activate the receptor. [10]