Home Neuronal Signaling AChR antagonist Flavoxate HCl

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Flavoxate HCl AChR antagonist

Cat.No.S4027

Flavoxate (NSC-114649) is a muscarinic AChR antagonist with IC50 of 12.2 μM.
Flavoxate HCl AChR antagonist Chemical Structure

Chemical Structure

Molecular Weight: 427.92

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Quality Control

Batch: S402701 Water]10 mg/mL]false]DMSO]3 mg/mL]false]Ethanol]Insoluble]false Purity: 99.98%
99.98

Chemical Information, Storage & Stability

Molecular Weight 427.92 Formula

C24H25NO4.HCl

 Storage (From the date of receipt)
CAS No. 3717-88-2 -- Storage of Stock Solutions

Synonyms NSC-114649 Smiles CC1=C(OC2=C(C1=O)C=CC=C2C(=O)OCCN3CCCCC3)C4=CC=CC=C4.Cl

Solubility

In vitro
Batch:

Water : 10 mg/mL

DMSO : 3 mg/mL ( (7.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble

Molarity Calculator

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In vivo
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Mechanism of Action

Targets/IC50/Ki
mAChR [1]
12.2 μM
In vitro
Flavoxate displaces [3H]nitrendipine on the Ca2+ channels binding sites with IC50 of 254 μM. [1] 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. [2] 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). [3] 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. [4] Flavoxate inhibits voltage-dependent nifedipine-sensitive inward Ba2+ currents in human detrusor myocytes at both 30 degrees C (Ki = 5.1 mM) and 37 degrees C (Ki = 4.6 mM). [5]
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. [2] Flavoxate (3 mg/kg, i.v.) abolishes rhythmic bladder contractions and the maximal intervals of voiding contractions is 7.20 min. [3]
References
  • https://pubmed.ncbi.nlm.nih.gov/15965499/
  • https://pubmed.ncbi.nlm.nih.gov/17909749/

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