Vanilloid receptor-1 antagonist

The first vanilloid receptor antagonist was Ruthenium Red (RR), an inorganic dye [1, 2]. Commercial RR is a mixture of compounds [65] and it remains to be understood... 

The structure-activity relationships for thiourea derivatives have been investigated as vanilloid receptor antagonist,216 220 and mast cell leukotriene release, etc.221 224... 

Scheme 5 Chemical structures of known vanilloid receptor antagonists a, capsazepine, a weak but competitive synthetic compound from Novartis, b, iodo-resiniferatoxin, a potent and competitive synthetic compound from Novo Nordisk, c, ruthenium red, a weak, non-competitive and non-selective antagonists.

Wahl, P., Foged, C., Tullin, S., Thomsen, C. lodo-resiniferatoxin, a new potent vanilloid receptor antagonist, Mol. Pharmacol. 2001, 59, 9-15. 

VANILLOID RECEPTOR ANTAGONISTS act at sites activated by sensory irritants, e.g. capsaicin see VANILLOID receptor agonists. Capsazepine, a synthetic compound developed out of vallinoids such as capsaicin, is a high-afflnity competitive vanilloid receptors antagonist. It is used as a pharmacological tool. There is some variation in affinity between different sites and species, suggesting receptor subtypes and species variants. Ruthenium Red also acts as an inhibitor at these sites in a non-competitive manner. 

Chromone derivatives, in particular 2-spiro-chroman-4(lF/)-ones, are ubiquitous in nature and possess various biological activities which include antiarrhythmic, anti-HIV, antidiabetic, acetyl-CoA carboxylase (ACC) inhibitor, vanilloid receptor antagonist, growth hormone secretagogues, histamine receptor antagonist, and... 

Vanilloid receptor agonists Vanilloid receptor antagonists Cannabinoid moduiators Growth factor moduiators... 

Szallasi A, Cortright DN, Blum CA et al (2007) The vanilloid receptor TRPV1 10 years from channel cloning to antagonist proof-of-concept. Nat Rev Drug Discov 6 357-372... 

Clinically Useful Vanilloid Receptor TRPVl Antagonists Just around the Corner (or too Early to Tell) ... 

CLINICALLY USEFUL VANILLOID RECEPTOR TRPVl ANTAGONISTS... 

Known antagonists of vanilloid receptors include capsazepine, which acts competitively but with low potency at the capsaicin binding sites (Bevan et al., 1992), iodo-RTX, which binds with high affinity (Wahl et al., 2001), the unselective antagonist ruthenium red (Amann and Maggi, 1991) and synthetic arginine-rich hexapeptides (Planells-Cases et al., 2000), which are putative channel blockers. 

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