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Flavoxate hydrochloride

Flavoxate hydrochloride structure

CAS No:
3717-88-2
Formula:
C24H25NO4.ClH
Chemical Name:
Flavoxate hydrochloride
Synonyms:
4H-1-Benzopyran-8-carboxylic acid,3-methyl-4-oxo-2-phenyl-,2-(1-piperidinyl)ethyl ester,hydrochloride (1:1);4H-1-Benzopyran-8-carboxylic acid,3-methyl-4-oxo-2-phenyl-,2-piperidinoethyl ester,hydrochloride;4H-1-Benzopyran-8-carboxylic acid,3-methyl-4-oxo-2-phenyl-,2-(1-piperidinyl)ethyl ester,hydrochloride;1-Piperidineethanol,3-methyl-4-oxo-2-phenyl-4H-1-benzopyran-8-carboxylate (ester),hydrochloride;Flavoxate hydrochloride;Piperidinoethyl-3-methylflavone-8-carboxylate hydrochloride;DW 61;Peflate;Rec 7/0040;Spasmal;Urispas;Bladderon;Genurin;Patricin;Spasuret;NSC 114649;2-(Piperidin-1-yl)ethyl 3-methyl-4-oxo-2-phenyl-4H-chromene-8-carboxylate hydrochloride
Categories:
Active Pharmaceutical Ingredients > Urinary System Drugs

Description

Flavoxate Hydrochloride(DW-61 Hydrochloride) is a muscarinic AChR antagonist used in various urinary syndromes and as an antispasmodic.Target: mAChRFlavoxate 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.

Flavoxate hydrochloride is the hydrochloride salt of flavoxate. It has a role as a muscarinic antagonist, an antispasmodic drug and a parasympatholytic. It contains a flavoxate(1+).|Flavoxate Hydrochloride is the hydrochloride salt form of flavoxate, a parasympatholytic agent with antispasmodic activity. Flavoxate hydrochloride competitively binds to muscarinic receptors, thereby preventing the actions of acetylcholine. This relaxes vascular smooth muscle, mainly of the urinary tract, and prevents smooth muscle contractions.|A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist.

Flavoxate hydrochloride Basic Attributes

Molecular Weight：

427.92

Exact Mass：

427.155029

EC Number：

223-066-4

UNII：

9C05J6089W

NSC Number：

114649

DSSTox ID：

DTXSID1047784

NCI Thesaurus Code：

C47533

HScode：

2934999090

Characteristics

PSA：

55.8

XLogP3：

5.15100

Appearance：

white solid

Density：

1.203g/cm3

Melting Point：

232-234 °C

Boiling Point：

564.1ºC at 760 mmHg

Flash Point：

294.9ºC

Water Solubility：

H2O: ~6.6 mg/mL

Storage Conditions：

Refrigerator

Toxicity：

LD50 i.v. in rats: 27.4 mg/kg (Cazzulani)

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

22-36/37/38

safety instructions：

RTECS Number：

DJ2450000

Marks：

Precautionary statement(s)：

P301 + P312 + P330-P305 + P351 + P338

Hazard Statements：

H302-H315-H319-H335

GHS Classification：

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 95 companies from 7 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

MeSH：

Agents that inhibit the actions of the parasympathetic nervous system. The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS. (See all compounds classified as Parasympatholytics.)|Drugs used in the treatment of urogenital conditions and diseases such as URINARY INCONTINENCE; PROSTATIC HYPERPLASIA; and ERECTILE DYSFUNCTION. (See all compounds classified as Urological Agents.)

MeSH Entry Terms：

Bladuril

Flavoxate hydrochloride Use and Manufacturing

Uses

Smooth muscle relaxant. Used as antispasmodic; in treatment of urinary incontinence This product is suitable for symptoms such as frequent urination, urgency, dysuria, dysuria and urinary incontinence caused by the following diseases: 1. Infectious diseases of the lower urinary tract (prostatitis, cystitis, urethritis, etc.). 2. Lower urinary tract obstructive diseases (early and mid-stage prostate hyperplasia, spasticity, functional urethral stricture). 3. After lower urinary tract instrument examination or surgery (prostate enucleation, urethral dilation, intravesical surgery). 4. Urethral syndrome. 5. Urgent urinary incontinence Urinary system medication

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:427.9
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:6
Exact Mass:427.1550360
Monoisotopic Mass:427.1550360
Topological Polar Surface Area:55.8
Heavy Atom Count:30
Complexity:631
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

This product is a smooth muscle relaxant. It has the function of inhibiting adenylate cyclase and phosphodiesterase, antagonizing calcium ions, and has a weak anti-muscarinic effect. It has a selective spasmolytic effect on the smooth muscles of the urogenital system, and can directly relieve the spasm of the smooth muscles of the urogenital system, relax the muscles, and eliminate frequent urination, urgency, urinary incontinence, and lower abdominal pain caused by urethral bladder smooth muscle spasm.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

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Indication	Not yet clear.
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Registered Holders

RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.P.A.

France
Active
ISOCHEM

France
Active
Chongqing Unger Dragon Pharmaceutical Co., Ltd.

China
Active

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