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- Title
The effects of flavoxate hydrochloride on voltage-dependent L-type Ca<sup>2+</sup> currents in human urinary bladder.
- Authors
Tomoda, Toshihisa; Aishima, Manami; Takano, Naruaki; Nakano, Toshiaki; Seki, Narihito; Yonemitsu, Yoshikazu; Sueishi, Katsuo; Naito, Seiji; Ito, Yushi; Teramoto, Noriyoshi
- Abstract
The effects of flavoxate hydrochloride (Bladderon®, piperidinoethyl-3-methylflavone-8-carboxylate; hereafter referred as flavoxate) on voltage-dependent nifedipine-sensitive inward Ba2+ currents in human detrusor myocytes were investigated using a conventional whole-cell patch-clamp. Tension measurement was also performed to study the effects of flavoxate on K+-induced contraction in human urinary bladder.Flavoxate caused a concentration-dependent reduction of the K+-induced contraction of human urinary bladder.In human detrusor myocytes, flavoxate inhibited the peak amplitude of voltage-dependent nifedipine-sensitive inward Ba2+ currents in a voltage- and concentration-dependent manner (Ki=10 μM), and shifted the steady-state inactivation curve of Ba2+ currents to the left at a holding potential of −90 mV.Immunohistochemical studies indicated the presence of the α1C subunit protein, which is a constituent of human L-type Ca2+ channels (CaV1.2), in the bundles of human detrusor smooth muscle.These results suggest that flavoxate caused muscle relaxation through the inhibition of L-type Ca2+ channels in human detrusor.British Journal of Pharmacology (2005) 146, 25–32. doi:10.1038/sj.bjp.0706284; published online 20 June 2005
- Subjects
BLADDER; URINARY organs; GENITOURINARY organs; NIFEDIPINE; CALCIUM antagonists; MEDICAL sciences
- Publication
British Journal of Pharmacology, 2005, Vol 146, Issue 1, p25
- ISSN
0007-1188
- Publication type
Article
- DOI
10.1038/sj.bjp.0706284