Flavoxate hydrochloride  (Synonyms: Rec-7-0040; DW61)

Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca²⁺ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba²⁺ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions^[1][2][3].

Flavoxate hydrochloride (100 nM-30 μM) causes concentration-dependent relaxation of K⁺-precontracted human detrusor muscle strips, with an IC₅₀ of 2 μM^[1].
Flavoxate hydrochloride (10-30 μM; 5 minutes) inhibits voltage-dependent, nifedipine-sensitive Ba²⁺ currents (L-type Ca²⁺ channel currents) in freshly isolated human detrusor myocytes in a voltage- and concentration-dependent manner, with a K_i value of 10 μM at a holding potential of -60 mV and 56 μM at a holding potential of -90 mV^[1].
Flavoxate hydrochloride (1-30 μM; 22°C, 30°C, 37°C) inhibits voltage-dependent inward Ba²⁺ currents through L-type Ca²⁺ channels in human detrusor muscle cells in a concentration-dependent and temperature-sensitive manner, with enhanced efficacy at higher temperatures (K_i=10.3 μM at 22°C, K_i=5.1 μM at 30°C, K_i=4.6 μM at 37°C), and shifts the steady-state inactivation curve leftward at 30°C^[2].
Flavoxate hydrochloride (10^-8-10^-5 M; 15 min) concentration-dependently inhibits cAMP production in membrane preparations from rat striatum and cerebral cortex via pertussis toxin-sensitive G₁-coupled receptors; its inhibitory effect at 10^-6 M is completely reversed by combined treatment with any two of adenosine A₁, dopamine D₂, or adrenergic α₂ receptor antagonists^[3].
Flavoxate hydrochloride (10^-8-10^-4 M) binds to rat adenosine A₁, adrenergic α₂, dopamine D₂, and muscarinic M₂ receptors with K_i values in the micromolar to submicromolar range, but shows negligible affinity for many other neurotransmitter receptors^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Flavoxate hydrochloride (3 mg/kg; i.v.; single dose) completely abolishes isovolumetric rhythmic bladder contractions in vehicle-pretreated female Sprague-Dawley rats, an effect that is eliminated by prior intracerebroventricular Pertussis Toxin (PTX) pretreatment^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

427.92

C₂₄H₂₆ClNO₄

3717-88-2

Solid

White to off-white

O=C(C1=C2C(C(C(C)=C(C3=CC=CC=C3)O2)=O)=CC=C1)OCCN4CCCCC4.Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Tomoda T, et al. The effects of flavoxate hydrochloride on voltage-dependent L-type Ca2+ currents in human urinary bladder. Br J Pharmacol. 2005;146(1):25-32.  [Content Brief]

  [2]. Tomoda T, et al. Effects of flavoxate hydrochloride on voltage-dependent Ba2+ currents in human detrusor myocytes at different experimental temperatures. Naunyn Schmiedebergs Arch Pharmacol. 2007;376(3):195-203.  [Content Brief]

  [3]. Oka M, et al. Brain pertussis toxin-sensitive G proteins are involved in the flavoxate hydrochloride-induced suppression of the micturition reflex in rats. Brain Res. 1996;727(1-2):91-98.  [Content Brief]