Name: Flavoxate hydrochloride
Brand: Alomone Labs
SKU: F-140
Availability: InStock

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.

Structure

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 (K_i10 µM), and shifted the steady-state inactivation curve of Ba²⁺‏ currents to the left at a holding potential of -90 mV¹.

References-Activity

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 Ca_V1.2 currents heterologously expressed in Xenopus oocytes.
A. Time course of Ca_V1.2/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

Catterall, W.A. et al. (2003) Pharmacol. Rev. 55, 579.
Streissnig, J. et al. (1998) Trends. Pharmacol Sci. 19, 108.
Haeusler G. et al. (2002) Obstet.Gynecol 100, 1003.
Kimura, Y. et al. (1996) Int. J. Urol. 3, 218.
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 Ca_V1 (α 1S) channel genes². Ca_v1.2 (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 (Ca_V1.2) channels in human urinary bladder detrusor smooth muscle, in a concentration-dependent manner⁵.

Target L-type Ca²⁺ channels

Lyophilized Powder

Last update: 24/01/2021

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

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