IC50: 10 nm against 100 nm capsaicin
The vanilloid TRPV1 receptor, also known as VR1 receptor, belongs to the large family of ‘transient receptor potential’ (TRP). TRPV1 functions as a molecular integrator of nociceptive stimuli, including heat, protons and plant toxins, and is most abundant in peripheral sensory fibers of the C and Ad type. 6-iodo-nordihydrocapsaicin is a potent TRPV1 antagonist.
In vitro: Using human recombinant TRPV1, 6-Iodonordihydrocapsaicin (IC50=10 nm against 100 nm capsaicin) was about four times more potent than the prototypical TRPV1 antagonist, capsazepine .
In vivo: 6-Iodonordihydrocapsaicin was tested against capsaicin also on native TRPV1 in: (i) rat dorsal root ganglion neurons in culture; (ii) guinea-pig urinary bladder; and (iii) guinea-pig bronchi. In all cases, except for the guineapig bronchi, the compound was significantly more potent than capsazepine as a TRPV1 antagonist .
Clinical trial: Up to now, 6-Iodonordihydrocapsaicin is still in the preclinical development stage.
 Appendino G, Harrison S, De Petrocellis L, Daddario N, Bianchi F, Schiano Moriello A, Trevisani M, Benvenuti F, Geppetti P, Di Marzo V. Halogenation of a capsaicin analogue leads to novel vanilloid TRPV1 receptor antagonists. Br J Pharmacol. 2003 Aug;139(8):1417-24.
|Physical Appearance||White solid|
|Storage||Store at RT|
|Solubility||<20.96mg/ml in ethanol; <41.93mg/ml in DMSO|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|