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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.
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.
Honokiol is a weak CB2 receptor ligand but the naturally occurring derivative 4-O-methylhonokiol was shown to be a potent and selective cannabinoid CB2 receptor inverse agonist and to possess antiosteoclastic effects. [18]
S-444,823 is a drug developed by Shionogi which is a cannabinoid agonist. [1] It was developed as an antipruritic, and has moderate selectivity for the CB 2 subtype, having a CB 2 affinity of 18nM, and 32x selectivity over the CB 1 receptor.
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 ...
CID16020046 is a compound which acts as an inverse agonist at the former orphan receptor GPR55, [1] and may be the first selective inverse agonist characterised for this receptor. It was found to block a number of GPR55 mediated responses such as wound healing and activation of immune system T-cells and B-cells, as well as showing inverse ...
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 ...
Drinabant (INN; AVE-1625) is a drug that acts as a selective CB 1 receptor antagonist, which was under investigation varyingly by Sanofi-Aventis as a treatment for obesity, schizophrenia, Alzheimer's disease, Parkinson's disease, and nicotine dependence.