Resiniferatoxin

CHF 270.00
In stock
AG-CN2-0534-MC050.5 mgCHF 270.00
More Information
Product Details
Synonyms RTX; MCP-101
Product Type Chemical
Properties
Formula

C37H40O9

MW 628.72
CAS 57444-62-9
RTECS CY1633700
Source/Host Chemicals Isolated from Euphorbia resinifera.
Purity Chemicals ≥98% (HPLC)
Appearance White to off-white solid.
Solubility Soluble in DMSO (50mg/ml) or ethanol (25mg/ml).
InChi Key DSDNAKHZNJAGHN-MSBCBURGSA-N
Smiles CC(C1=O)=CC2[C@]1(O)CC(COC(CC3=CC(OC)=C(O)C=C3)=O)=CC4[C@]25[C@H](C)C [C@@]6(C(C)=C)[C@@H]4O[C@@](O6)(CC7=CC=CC=C7)O5
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • Highly potent TRPV1 agonist.
  • Resiniferatoxin (RTX) is a phorbol-related diterpene ester analog of capsaicin. RTX is a highly potent transient receptor potential vanilloid 1 (TRPV1) agonist (Ki=43pM) and acts as a selective modulator of primary afferent neurons. TRPV1 or vanilloid receptor 1 is a non-selective cation channel that is involved in the detection and transduction of nociceptive stimuli. TRPV1 is expressed in the plasma membrane of sensory neurons and stimulation by RTX causes this ion channel to become permeable to cations, especially calcium. The influx of cations causes the neuron to depolarize, transmitting signals similar to those that would be transmitted if the innervated tissue were being burned or damaged. This stimulation is followed by desensitization and analgesia, in part because the nerve endings die from calcium overload. Inflammation and nerve damage result in the up-regulation of TRPV1 transcription and therefore, modulators of TRPV1 channels are potentially useful in the treatment of inflammatory and neuropathic pain.

  • The primary action of RTX is to activate sensory neurons responsible for the perception of pain. RTX has been developed as an analgesic (painkiller) as a mean to provide pain relief for forms of advanced cancer. RTX has been investigated for treatment of urinary bladder hyper-reflexia, interstitial cystitis, rhinitis, lifelong premature ejaculation and chronic pain conditions. RTX has also been shown anti-inflammatory activity in T. spiralis infection, by inhibiting the Th1 immune response through the inhibition of Th1 cytokines in the intestinal phase.

Product References
  1. Resiniferatoxin, a phorbol-related diterpene, acts as an ultrapotent analog of capsaicin, the irritant constituent in red pepper: A. Szallasi & P.M. Blumberg; Neuroscience 30, 515 (1989)
  2. Resiniferatoxin and its analogs provide novel insights into the pharmacology of the vanilloid (capsaicin) receptor: A. Szallasi & P.M. Blumberg; Life Sci. 47, 1399 (1990) (Review)
  3. Resiniferatoxin: an ultrapotent selective modulator of capsaicin-sensitive primary afferent neurons: J. Szolcsanyi, et al.; J. Pharmacol. Exp. Ther. 255, 923 (1990)
  4. Characterization of resiniferatoxin binding sites on sensory neurons: co-regulation of resiniferatoxin binding and capsaicin sensitivity in adult rat dorsal root ganglia: J. Winter, et al.; Neuroscience 57, 747 (1993)
  5. Euphorbium: modern research on its active principle, resiniferatoxin, revives an ancient medicine: G. Appendino & A. Szallasi; Life Sci. 60, 681 (1997) (Review)
  6. Differential activation and desensitization of sensory neurons by resiniferatoxin: G. Acs, et al.; J. Neurosci. 17, 5622 (1997)
  7. Selective and long-lasting neural blockade with resiniferatoxin prevents inflammatory pain hypersensitivity: I. Kissin, et al.; Anesth. Analg. 94, 1253 (2002)
  8. The effect of intravesical capsaicin and resiniferatoxin in neurogenic bladder dysfunction: A.S. el-Mahrouky, et al.; Adv. Exp. Med. Biol. 539, 359 (2003) (Review)
  9. Sensory nerve inactivation by resiniferatoxin improves insulin sensitivity in male obese Zucker rats: S.G. Moesgaard, et al.; Am. J. Physiol. Endocrinol. Metab. 288, E1137 (2005)
  10. Activation of transient receptor potential vanilloid 1 (TRPV1) by resiniferatoxin: M. Raisinghani, et al.; J. Physiol. 567, 771 (2005)
  11. Analgesic effects of capsazepine and resiniferatoxin on bone cancer pain in mice: L. Menendez, et al.; Neurosci. Lett. 393, 70 (2006)
  12. The vanilloid agonist resiniferatoxin for interventional-based pain control: M.J. Iadarola & A.J. Mannes; Curr. Top Med. Chem. 11, 2171 (2011) (Review)
  13. Therapeutic targeting of TRPV1 by resiniferatoxin, from preclinical studies to clinical trials: I. Kissin & A. Szallasi; Curr. Top Med. Chem. 11, 2159 (2011) (Review)
  14. Resiniferatoxin for treatment of lifelong premature ejaculation: a preliminary study: B. Shi, et al.; Int. J. Urol. 21, 923 (2014)
  15. Resiniferatoxin modulates the Th1 immune response and protects the host during intestinal nematode infection: J.L. Munoz-Carrillo, et al.; Parasite Immunol. 39, e12448 (2017)
© 2017 Adipogen Life Sciences. Pictures: © 2012 Martin Oeggerli. All Rights Reserved.