Ka. Wardle et al., PHARMACOLOGICAL CHARACTERIZATION OF THE VANILLOID RECEPTOR IN THE RATISOLATED VAS-DEFERENS, Journal of Pharmacy and Pharmacology, 48(3), 1996, pp. 285-291
The present study set out to further characterize the vanilloid recept
or in the rat isolated vas deferens. In this preparation, both capsaic
in and resiniferatoxin (RTX) evoked a concentration-dependent inhibiti
on in the amplitude of electrically-evoked contractions with pEC50 val
ues of 7.62 +/- 0.03 and 12.2 +/- 0.21 respectively. Responses to caps
aicin were fast in onset and faded rapidly over a 30-min exposure peri
od, whereas those to RTX were slow in onset and well maintained, an ob
servation believed to reflect pharmacokinetic differences in the rate
of penetration to the vanilloid receptor. Responses to both agonists s
howed mutual cross-desensitization and were antagonized by both the va
nilloid-receptor antagonist capsazepine and the ion-channel blocker ru
thenium red. The capsaicin analogue, olvanil failed to either mimic or
antagonize capsaicin-evoked responses in the rat isolated vas deferen
s, an effect at variance with previous observations in other tissues.
The reason for these differences is unclear, but the possibility of mu
ltiple classes of receptor cannot at this stage be ruled out.