RESINIFERATOXIN

Description

Resiniferatoxin (57444-62-9) is an ultrapotent TRPV1 activator (Ki=43 pM).1 Resiniferatoxin is 100-10,000 fold more potent than capsaicin for most responses yet displays a spectrum of activity distinct from capsaicin.2 A potent sensory neuron excitotoxin.3 Induces a long lasting analgesia in a rodent model of burn pain.4 SEVERE IRRITANT – HANDLE WITH CARE

Chemical Properties

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Uses

Resiniferatoxin has been used as an agonist to transient receptor potential vanilloid 2 (TRPV2):

• for complex preparation for cryo-electron microscopy structural studies
• to test its effect towards immune responses toP.aeruginosa in sensory neurons associated with the cornea
• to study its effects in the denervation of the peripheral sensory nerves in psoriatic mice

Definition

ChEBI: Resiniferatoxin is a heteropentacyclic compound found in Euphorbia poissonii with molecular formula C37H40O9. It is an agonist of the transient receptor potential cation channel subfamily V member 1 (TrpV1). It has a role as a TRPV1 agonist, a plant metabolite, a neurotoxin and an analgesic. It is a diterpenoid, an ortho ester, a tertiary alpha-hydroxy ketone, a member of phenols, a monomethoxybenzene, an organic heteropentacyclic compound, a carboxylic ester and an enone.

Hazard

A poison.

Biological Activity

Ultrapotent analog of capsaicin that is an agonist at vanilloid receptors (K i = 43 pM). Like capsaicin, it acts as a selective modulator of primary afferent neurons. Also available as part of the Vanilloid TRPV1 Receptor Tocriset™ .

Biochem/physiol Actions

Resiniferatoxin (RTX) is an analog of capsaicin. It effectively ablates corneal sensory neurons by activating transient receptor potential vanilloid 1 (TRPV1) channels. RTX facilitates corneal bacterial clearance. It also elicits protective functionality towards cardiac function in a rat model with congestive heart failure (CHF).

References

[1] J SZOLCSANYI. Resiniferatoxin: an ultrapotent selective modulator of capsaicin-sensitive primary afferent neurons.[J]. Journal of Pharmacology and Experimental Therapeutics, 1990, 255 2: 923-928.
[2] ARPAD SZALLASI  Peter M B. Resiniferatoxin and its analogs provide novel insights into the pharmacology of the vanilloid (capsaicin) receptor[J]. Life sciences, 1990, 47 16: Pages 1399-1408. DOI:10.1016/0024-3205(90)90518-v
[3] JANET WINTER. Cellular mechanism of action of resiniferatoxin: a potent sensory neuron excitotoxin[J]. Brain Research, 1990, 520 1: Pages 131-140. DOI:10.1016/0006-8993(90)91698-g
[4] SALAS M M, CLIFFORD J, HAYDEN J, et al. Local Resiniferatoxin Induces Long-Lasting Analgesia in a Rat Model of Full Thickness Thermal Injury[C]//12 1. 2016: 0. DOI:10.1093/pm/pnw260