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Flavoxate hydrochloride

Bladderon®, piperidinoethyl-3-methylflavone-8-carboxylate, Urispas®

A Blocker of Voltage-Gated L-Type Ca2+ Channels

Cat #: F-140
Alternative Name Bladderon®, piperidinoethyl-3-methylflavone-8-carboxylate, Urispas®
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 427.9
    Purity: >96%
    Effective concentration 1-100 µM.
    Chemical name 3-Methyl-4-oxo-2-phenyl-4H-1-benzopyran-8-carboxylic acid 2-(1-piperidinyl)ethyl ester hydrochloride.
    Molecular formula C24H26NO4Cl.
    CAS No.: 3717-88-2
    Activity 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 (K10 µM), and shifted the steady-state inactivation curve of Ba2+ currents to the left at a holding potential of -90 mV1.
    1. Tomoda, T. et al. (2005) Br. J. Pharmacol. 146, 25.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Water. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Flavoxate hydrochloride inhibits voltage-gated CaV1.2 currents heterologously expressed in Xenopus oocytes.
      Alomone Labs Flavoxate hydrochloride inhibits voltage-gated CaV1.2 currents heterologously expressed in Xenopus oocytes.
      A. Time course of CaV1.2/α2-δ1/β2a (L-type) current inhibition by 100 µM Flavoxate hydrochloride (#F-140). Currents were elicited by application of voltage steps from a holding potential of -100 mV to 0 mV (100 msec). B. Superimposed example traces of current responses before and during perfusion of 100 µM Flavoxate hydrochloride as indicated.
    References - Scientific background
    1. Catterall, W.A. et al. (2003) Pharmacol. Rev. 55, 579.
    2. Streissnig, J. et al. (1998) Trends. Pharmacol Sci. 19, 108.
    3. Haeusler G. et al. (2002) Obstet.Gynecol 100, 1003.
    4. Kimura, Y. et al. (1996) Int. J. Urol. 3, 218.
    5. Tomoda, T. et al. (2005) Br. J. Pharmacol. 146, 25.
    Scientific background

    Voltage-dependent L-type Ca2+ channels play an important role Ca2+ influx. L-type calcium currents typically require a strong depolarization for activation and are long-lasting1.

    The common pharmacological profile of L-type channels is determined by the α1 subunit, which forms the Ca2+ selective pore, and is encoded by one of the CaV1 (α 1S) channel genes2. Cav1.2 (CACNA1C) in humans is widely expressed in cardiac myocytes, smooth muscle myocytes, endocrine cells, neuronal cell bodies and proximal dendrites1.

    Flavoxate hydrochloride is widely used for the treatment of urinary frequency3. Flavoxate increases urinary bladder capacity primarily by suppressing the micturition reflex through modulation of the central nervous system4. However, in addition to its activity in the CNS, it possesses direct inhibitory effects on the detrusor muscle. Flavoxate causes a detrusor relaxation through inhibition of L-type Ca+2 (CaV1.2) channels in human urinary bladder detrusor smooth muscle, in a concentration-dependent manner5.

    Target L-type Ca2+ channels
    Last update: 24/01/2021

    Flavoxate hydrochloride (#F-140) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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