Characterization of a peripheral vanilloid (capsaicin) receptor in the urinary bladder of the rat

Capsazepine Is a Novel Activator of the δ Subunit of the Human Epithelial Na+ Channel

“…Capsazepine has been developed as a synthetic competitive antagonist at TRPV1 (21,22,24). In a variety of bioassays in vitro and in vivo, capsazepine is effective against both capsaicin-and resiniferatoxin-evoked responses (21)(22)(23)(24).…”

“…In a variety of bioassays in vitro and in vivo, capsazepine is effective against both capsaicin-and resiniferatoxin-evoked responses (21)(22)(23)(24). Capsazepine at micromolar concentrations, which are necessary to inhibit capsaicin-evoked responses in most tissues, also blocks voltage-dependent calcium channels (29,30) and voltage-dependent potassium channels (30) as well as nicotinic acetylcholine receptors (31).…”

“…The effects of capsazepine, a well known competitive antagonist for TRPV1 (21)(22)(23)(24), on the hENaC␦␤␥ current were examined using a two-electrode voltage clamp technique in the Xenopus oocyte expression system. When hENaC␦␤␥ heteromultimer was expressed in Xenopus oocytes, an inward current was induced at a holding potential of Ϫ60 mV, and the current was mostly inhibited by 100 M amiloride (Fig.…”

“…Capsazepine, which possesses a vanilloid moiety, has been developed as a synthetic competitive antagonist for the transient receptor potential vanilloid subfamily 1 (TRPV1) (21)(22)(23)(24). Here we show that capsazepine activates hENaC␦␤␥ in a concentrationdependent manner, although other vanilloids (capsaicin, resiniferatoxin, and olvanil) were not affected on the hENaC␦␤␥ current.…”

Chillies: from antiquity to urology

“…The scientific rationale for this treatment was based on de Groat's experiments in cats. like capsaicin) is thought to represent the site of this receptor [31]. In the human bladder presumptive sensory…”