product name Flavoxate HCl
Description: Flavoxate is a muscarinic AChR antagonist with IC50 of 12.2 μM. Flavoxate (>10 μM) suppresses carbachol-induced contractions in isolated rat detrusor strips with pD value of 4.55. Flavoxate inhibits CAMP formation in a concentration-dependent manner in membranes from the rat striatum and cerebral cortex, an action which is completely abolished by pretreating the membranes with pertussis toxin (PTX).
References: Int J Urol. 1996 May;3(3):218-27; Brain Res. 1996 Jul 15;727(1-2):91-8.
427.92
Formula
C24H25NO4.HCl
CAS No.
3717-88-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 3 mg/mL (7.0 mM)
Water: 10 mg/mL (23.4 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
NSC-114649
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19392817
| In Vitro |
In vitro activity: Flavoxate displaces [3H]nitrendipine on the Ca2+ channels binding sites with IC50 of 254 μM. Flavoxate (>10 μM) suppresses carbachol-induced contractions in isolated rat detrusor strips with pD value of 4.55. Flavoxate (>10 μM) suppresses Ca2+-induced contractions in isolated rat detrusor strips with pIC50 value of 4.92. Flavoxate (0.01 μM −10 μM) inhibits CAMP formation in a concentration-dependent manner in membranes from the rat striatum and cerebral cortex, an action which is completely abolished by pretreating the membranes with pertussis toxin (PTX). Flavoxate causes a concentration-dependent reduction of the K+-induced contraction of human urinary bladder. Flavoxate inhibits the peak amplitude of voltage-dependent nifedipine-sensitive inward Ba2+ currents in a voltage- and concentration-dependent manner with Ki value of 10 μM in human detrusor myocytes. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Flavoxate (10mg/kg) suppresses both the an initial, rapidly rising phasic contraction (phase 1) and the tonic contraction (phase 2) contractions to the same extent in rats. Flavoxate (10mg/kg) abolishes the bladder contractions without causing any change in the amplitude of the contractions in rats. Flavoxate (3 mg/kg) abolishes the efferent neural activity and the associated bladder contractions for about 10 minutes without changing the baseline vesical pressure in rats. ICV-injected (50 to 200 μg/rat) or IT-injected (100 to 200 μg/rat) Flavoxate abolishes rhythmic bladder contractions during and after injection for five to 15 minutes in a dose-dependent manner in rats. Flavoxate (3 mg/kg, i.v.) abolishes rhythmic bladder contractions and the maximal intervals of voiding contractions is 7.20 min. |
| Animal model | Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in saline; 10 mg/kg; i.v. injection |
| References | Int J Urol. 1996 May;3(3):218-27; Brain Res. 1996 Jul 15;727(1-2):91-8. |
Related Posts
product name Flavoxate HCl
Description: Flavoxate is a muscarinic AChR antagonist with IC50 of 12.2 μM. Flavoxate (>10 μM) suppresses carbachol-induced contractions in isolated rat detrusor strips with pD value of 4.55. Flavoxate inhibits CAMP formation in a concentration-dependent manner in membranes from the rat striatum and cerebral cortex, an action which is completely abolished by pretreating the membranes with pertussis toxin (PTX).
References: Int J Urol. 1996 May;3(3):218-27; Brain Res. 1996 Jul 15;727(1-2):91-8.
427.92
Formula
C24H25NO4.HCl
CAS No.
3717-88-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 3 mg/mL (7.0 mM)
Water: 10 mg/mL (23.4 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
NSC-114649
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19392817
| In Vitro |
In vitro activity: Flavoxate displaces [3H]nitrendipine on the Ca2+ channels binding sites with IC50 of 254 μM. Flavoxate (>10 μM) suppresses carbachol-induced contractions in isolated rat detrusor strips with pD value of 4.55. Flavoxate (>10 μM) suppresses Ca2+-induced contractions in isolated rat detrusor strips with pIC50 value of 4.92. Flavoxate (0.01 μM −10 μM) inhibits CAMP formation in a concentration-dependent manner in membranes from the rat striatum and cerebral cortex, an action which is completely abolished by pretreating the membranes with pertussis toxin (PTX). Flavoxate causes a concentration-dependent reduction of the K+-induced contraction of human urinary bladder. Flavoxate inhibits the peak amplitude of voltage-dependent nifedipine-sensitive inward Ba2+ currents in a voltage- and concentration-dependent manner with Ki value of 10 μM in human detrusor myocytes. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Flavoxate (10mg/kg) suppresses both the an initial, rapidly rising phasic contraction (phase 1) and the tonic contraction (phase 2) contractions to the same extent in rats. Flavoxate (10mg/kg) abolishes the bladder contractions without causing any change in the amplitude of the contractions in rats. Flavoxate (3 mg/kg) abolishes the efferent neural activity and the associated bladder contractions for about 10 minutes without changing the baseline vesical pressure in rats. ICV-injected (50 to 200 μg/rat) or IT-injected (100 to 200 μg/rat) Flavoxate abolishes rhythmic bladder contractions during and after injection for five to 15 minutes in a dose-dependent manner in rats. Flavoxate (3 mg/kg, i.v.) abolishes rhythmic bladder contractions and the maximal intervals of voiding contractions is 7.20 min. |
| Animal model | Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in saline; 10 mg/kg; i.v. injection |
| References | Int J Urol. 1996 May;3(3):218-27; Brain Res. 1996 Jul 15;727(1-2):91-8. |