The effects of flavoxate hydrochloride on voltage-dependent L-type Ca 2+ currents in human urinary bladder

Toshihisa Tomoda, Manami Aishima, Naruaki Takano, Toshiaki Nakano, Narihito Seki, Yoshikazu Yonemitsu, Katsuo Sueishi, Seiji Naito, Yushi Ito, Noriyoshi Teramoto

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

The effects of flavoxate hydrochloride (Bladderon®, piperidinoethyl-3-methylflavone-8-carboxylate; hereafter referred as flavoxate) on voltage-dependent nifedipine-sensitive inward Ba 2+ 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 Ba 2+ currents in a voltage- and concentration-dependent manner (K i = 10 μM), and shifted the steady-state inactivation curve of Ba 2+ currents to the left at a holding potential of -90mV. Immunohistochemical studies indicated the presence of the α 1c subunit protein, which is a constituent of human L-type Ca 2+ channels (Ca v1-2), in the bundles of human detrusor smooth muscle. These results suggest that flavoxate caused muscle relaxation through the inhibition of L-type Ca 2+ channels in human detrusor.

Original languageEnglish
Pages (from-to)25-32
Number of pages8
JournalBritish Journal of Pharmacology
Volume146
Issue number1
DOIs
Publication statusPublished - Dec 1 2005

Fingerprint

Flavoxate
Urinary Bladder
Nifedipine
Muscle Cells
Muscle Relaxation
Protein Subunits
Smooth Muscle

All Science Journal Classification (ASJC) codes

  • Pharmacology

Cite this

The effects of flavoxate hydrochloride on voltage-dependent L-type Ca 2+ currents in human urinary bladder. / Tomoda, Toshihisa; Aishima, Manami; Takano, Naruaki; Nakano, Toshiaki; Seki, Narihito; Yonemitsu, Yoshikazu; Sueishi, Katsuo; Naito, Seiji; Ito, Yushi; Teramoto, Noriyoshi.

In: British Journal of Pharmacology, Vol. 146, No. 1, 01.12.2005, p. 25-32.

Research output: Contribution to journalArticle

Tomoda, Toshihisa ; Aishima, Manami ; Takano, Naruaki ; Nakano, Toshiaki ; Seki, Narihito ; Yonemitsu, Yoshikazu ; Sueishi, Katsuo ; Naito, Seiji ; Ito, Yushi ; Teramoto, Noriyoshi. / The effects of flavoxate hydrochloride on voltage-dependent L-type Ca 2+ currents in human urinary bladder. In: British Journal of Pharmacology. 2005 ; Vol. 146, No. 1. pp. 25-32.
@article{c1543242c3374b2ca403ffed2f9751c2,
title = "The effects of flavoxate hydrochloride on voltage-dependent L-type Ca 2+ currents in human urinary bladder",
abstract = "The effects of flavoxate hydrochloride (Bladderon{\circledR}, piperidinoethyl-3-methylflavone-8-carboxylate; hereafter referred as flavoxate) on voltage-dependent nifedipine-sensitive inward Ba 2+ 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 Ba 2+ currents in a voltage- and concentration-dependent manner (K i = 10 μM), and shifted the steady-state inactivation curve of Ba 2+ currents to the left at a holding potential of -90mV. Immunohistochemical studies indicated the presence of the α 1c subunit protein, which is a constituent of human L-type Ca 2+ channels (Ca v1-2), in the bundles of human detrusor smooth muscle. These results suggest that flavoxate caused muscle relaxation through the inhibition of L-type Ca 2+ channels in human detrusor.",
author = "Toshihisa Tomoda and Manami Aishima and Naruaki Takano and Toshiaki Nakano and Narihito Seki and Yoshikazu Yonemitsu and Katsuo Sueishi and Seiji Naito and Yushi Ito and Noriyoshi Teramoto",
year = "2005",
month = "12",
day = "1",
doi = "10.1038/sj.bjp.0706284",
language = "English",
volume = "146",
pages = "25--32",
journal = "British Journal of Pharmacology",
issn = "0007-1188",
publisher = "Wiley-Blackwell",
number = "1",

}

TY - JOUR

T1 - The effects of flavoxate hydrochloride on voltage-dependent L-type Ca 2+ currents in human urinary bladder

AU - Tomoda, Toshihisa

AU - Aishima, Manami

AU - Takano, Naruaki

AU - Nakano, Toshiaki

AU - Seki, Narihito

AU - Yonemitsu, Yoshikazu

AU - Sueishi, Katsuo

AU - Naito, Seiji

AU - Ito, Yushi

AU - Teramoto, Noriyoshi

PY - 2005/12/1

Y1 - 2005/12/1

N2 - The effects of flavoxate hydrochloride (Bladderon®, piperidinoethyl-3-methylflavone-8-carboxylate; hereafter referred as flavoxate) on voltage-dependent nifedipine-sensitive inward Ba 2+ 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 Ba 2+ currents in a voltage- and concentration-dependent manner (K i = 10 μM), and shifted the steady-state inactivation curve of Ba 2+ currents to the left at a holding potential of -90mV. Immunohistochemical studies indicated the presence of the α 1c subunit protein, which is a constituent of human L-type Ca 2+ channels (Ca v1-2), in the bundles of human detrusor smooth muscle. These results suggest that flavoxate caused muscle relaxation through the inhibition of L-type Ca 2+ channels in human detrusor.

AB - The effects of flavoxate hydrochloride (Bladderon®, piperidinoethyl-3-methylflavone-8-carboxylate; hereafter referred as flavoxate) on voltage-dependent nifedipine-sensitive inward Ba 2+ 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 Ba 2+ currents in a voltage- and concentration-dependent manner (K i = 10 μM), and shifted the steady-state inactivation curve of Ba 2+ currents to the left at a holding potential of -90mV. Immunohistochemical studies indicated the presence of the α 1c subunit protein, which is a constituent of human L-type Ca 2+ channels (Ca v1-2), in the bundles of human detrusor smooth muscle. These results suggest that flavoxate caused muscle relaxation through the inhibition of L-type Ca 2+ channels in human detrusor.

UR - http://www.scopus.com/inward/record.url?scp=30644460756&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=30644460756&partnerID=8YFLogxK

U2 - 10.1038/sj.bjp.0706284

DO - 10.1038/sj.bjp.0706284

M3 - Article

C2 - 15965499

AN - SCOPUS:30644460756

VL - 146

SP - 25

EP - 32

JO - British Journal of Pharmacology

JF - British Journal of Pharmacology

SN - 0007-1188

IS - 1

ER -