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GENTAUR
Tel: +32 16 58 90 45
Fax: + 32 16 50 90 45
info@genprice.com
Av. de l'Armée 68
• B-1040 BRUSSELS • BELGIUM
GENTAUR FRANCE
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• 75005 PARIS • FRANCE
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P-6388 PPAHV, >99%
[Phorbol 12-Phenylacetate 13-Acetate 20-Homovanillate]
WARNING: May be irritant to skin and mucous membranes. SPECIAL
HAZARD: possible tumor promoter. Gloves and mask should be worn when
using this compound. Care must be taken to prevent contact through all
routes of exposure.
Storage: Store at or below -20 ºC. Solubility:
Soluble in DMSO or ethanol. Disposal: A
 | Novel vanilloid (capsaicin) receptor ligand with dramatically different
pharmacological properties relative to previously known vanilloids. Like
capsaicin and resiniferatoxin, PPAHV binds to the vanilloid receptor (with
slightly higher affinity than capsaicin), downregulates rat spinal cord
vanilloid receptor number and desensitizes against neurogenic inflammation.
However, this compound is inactive in inducing hypothermia (no effect seen
at doses 200-fold higher than an active capsaicin dose) and ear edema in
mice and is at least 100-fold weaker than capsaicin in terms of pungency in
the eye-wiping assay. PPAHV also reduced or abolished the positive
cooperativity of resiniferatoxin binding to rat spinal cord membranes.
These unprecedented properties establish PPAHV as a useful new tool for
investigating vanilloid receptor function in vitro and in vivo.
Appendino, G., Cravotto, G., Palmisano, G., Annunziata, R. and Szallasi, A.
"Synthesis and evaluation of phorboid 20-homovanillates: discovery of a
class of ligands binding to the vanilloid (capsaicin) receptor with
different degrees of cooperativity." J. Med. Chem. 39:
3123-3131 (1996). Szallasi, A., Acs, G., Cravotto, G., Blumberg, P.M.,
Lundberg, J.M. and Appendino, G. "A novel agonist, phorbol 12-phenylacetate
13-acetate 20-homovanillate, abolishes positive cooperativity of binding by
the vanilloid receptor." Eur. J. Pharm. 299: 221-228 (1996).
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| Please inquire for bulk quantities of PPAHV at substantial discounts.
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| Anti-inflammatory uses 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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