Uses
6-?iodonordihydrocapsaicin (6-?I-?CPS) is a weak ERα agonist. It was demonstrated to induce luciferase gene expression.
Definition
ChEBI: N-[(4-hydroxy-2-iodo-5-methoxyphenyl)methyl]nonanamide is a member of phenols and a member of methoxybenzenes.
Biological Activity
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 [1].
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 [1].
IC 50
10 nm against 100 nm capsaicin
References
[1] 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.
