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GENTAUR
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Fax: + 32 16 50 90 45
info@genprice.com
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• B-1040 BRUSSELS • BELGIUM
GENTAUR FRANCE
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I-6400 5'-Iodoresiniferatoxin, >99%
[5'-IRTX]
This compound is currently out of stock and is anticipated
to be
ready for shipment on the following date: indefinite.
Storage: Store at or below -20 ºC. Solubility:
Soluble in DMSO or ethanol. Disposal: A LIGHT-SENSITIVE!
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IRTX is an important new compound that appears to be a
very potent vanilloid receptor antagonist. IRTX binds to the VR1 receptor
with high affinity (Kd = 4.3 nM) but does not induce
RTX- or capsaicin-like effects in Xenopus laevis oocytes expressing
VR1. IRTX completely blocked capsaicin-induced currents in these cells,
with an IC50 of 3.9 nM. In vivo, intrathecal
IRTX was 3.5-fold more potent that morphine in blocking a pain response
induced in the mouse paw by injected capsaicin. In this assay capsazepine
was inactive at 3 µg/mouse, a 113-fold higher dose than the ITX ED50.
IRTX's potency as a vanilloid antagonist is some 40-fold higher than that of
capsazepine, a weak vanilloid antagonist having other, unrelated biological
activities. Wahl, P. et al. "Iodo-resiniferatoxin, a new potent
vanilloid receptor antagonist." Mol. Pharm. 59: 9-15 (2001). |
| NOTE: The structure shown in FIg. 1 of Wahl et al. is
incorrect; the iodine atom should be next to the free OH-group on the
homovanillic acid moiety, as depicted below. |
| 5'-IRTX has also been shown to be a pure antagonist in HEK cells
expressing the human VR1, with an IC50 of 27 nM.
McDonnell, M. E., et al. "Synthesis and in vitro evaluation of a
novel iodinated resiniferatoxin derivative that is an agonist at the human
vanilloid VR1 receptor." Bioorg. Med. Chem. Lett. 12: 1189-1192
(2002). |
| NOTE: IRTX is sensitive to UV light, and prolonged
exposure to daylight or fluorescent room light may cause slow degradation.
Thus, although IRTX can be handled in normal room light, it is recommended
that such exposure be kept to a minimum. |
| Please inquire for bulk quantities of 5'-IRTX at substantial discounts.
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| Anti-inflammatoryuses and pharmaceutical formulations containing this
compound are covered by U. S. patent 5,643,948, and such formulations and
their use in medicine are covered by European patent EP 0455271, DE
P375210808, FR 0455271, GB 0455271 and SW 0455271, all assigned to PKC
Pharmaceuticals, Inc., the parent company of LC Laboratories. |
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