Resiniferatoxin and its analogs provide novel insights into the pharmacology of the vanilloid (capsaicin) receptor.

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Szallasi A, Blumberg PM

Resiniferatoxin and its analogs provide novel insights into the pharmacology of the vanilloid (capsaicin) receptor.

Life Sci. 1990;47(16):1399-408.

PubMed ID

2174484 [ View in PubMed

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Abstract

Capsaicin, the pungent constituent of chili peppers, represents the paradigm for the capsaicinoids or vanilloids, a family of compounds shown to stimulate and then desensitize specific subpopulations of sensory receptors, including C-polymodal nociceptors, A-delta mechanoheat nociceptors and warm receptors of the skin, as well as enteroceptors of thin afferent fibers. An exciting recent advance in the field has been the finding that resiniferatoxin (RTX), a naturally occurring diterpene containing a homovanillic acid ester, a key structural motif of capsaicin, functions as an ultrapotent capsaicin analog. For most of the responses characteristic of capsaicin, RTX is 100-10,000 fold more potent. Structure/activity analysis indicates, however, that RTX and related homovanillyl-diterpene esters display distinct spectra of activity. Specific [3H]RTX binding provides the first direct proof for the existence of vanilloid receptors. We expect that the RTX class of vanilloids will promote rapid progress in understanding of vanilloid structure/activity requirements and mechanism.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Resiniferatoxin	Transient receptor potential cation channel subfamily V member 1	Protein	Humans	Unknown	Not Available	Details