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Buflomedil hydrochloride

CAS No.
35543-24-9
Chemical Name:
Buflomedil hydrochloride
Synonyms
BUFLOMEDIL HCL;Buflan;ll1656;Lofton;Loftyl;Provas;rrodan;Irrodan;a-48257;bufedil
CBNumber:
CB1203561
Molecular Formula:
C17H26ClNO4
Molecular Weight:
343.85
MDL Number:
MFCD00078965
MOL File:
35543-24-9.mol
MSDS File:
SDS
Last updated:2023-06-08 17:06:35

Buflomedil hydrochloride Properties

Melting point 192-193°
storage temp. Inert atmosphere,Room Temperature
solubility Freely soluble in water, soluble in ethanol (96 per cent), very slightly soluble in acetone.
color White to Off-White
InChIKey ZDPACSAHMZADFZ-UHFFFAOYSA-N
CAS DataBase Reference 35543-24-9(CAS DataBase Reference)
FDA UNII 3J944AFS8S

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P264-P270-P301+P312+P330-P501
WGK Germany  3
RTECS  EL9885000
HS Code  2933.99.8290
Toxicity LD50 in mice (mg/kg): 80 ±4.6 i.v. (Lafon)
NFPA 704
0
2 0

Buflomedil hydrochloride price More Price(40)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich B1157400 Buflomedil hydrochloride European Pharmacopoeia (EP) Reference Standard 35543-24-9 b1157400 $150 2024-03-01 Buy
Sigma-Aldrich B5899 Buflomedil hydrochloride analytical standard 35543-24-9 1g $33 2022-05-15 Buy
TCI Chemical B3647 Buflomedil Hydrochloride >98.0%(HPLC)(T) 35543-24-9 1g $29 2024-03-01 Buy
TCI Chemical B3647 Buflomedil Hydrochloride >98.0%(HPLC)(T) 35543-24-9 5g $112 2024-03-01 Buy
Sigma-Aldrich Y0001529 Buflomedil for peak identification European Pharmacopoeia (EP) Reference Standard 35543-24-9 y0001529 $223 2024-03-01 Buy
Product number Packaging Price Buy
B1157400 b1157400 $150 Buy
B5899 1g $33 Buy
B3647 1g $29 Buy
B3647 5g $112 Buy
Y0001529 y0001529 $223 Buy

Buflomedil hydrochloride Chemical Properties,Uses,Production

Description

Buflomedil hydrochloride is a vasoactive drug with a variety of actions. It is an alpha-adrenoceptor antagonist and a weak calcium channel blocker. It inhibits platelet aggregation and improves erythrocyte deformability. However, its mechanism of action in peripheral vascular disease is not known.
Buflomedil has generally been well tolerated by most patients in clinical trials. The most frequently reported adverse effects include flushing, headache, vertigo, gas-trointestinal discomfort, and dizziness. These rarely require drug withdrawal. In controlled trials, adverse effects have occurred in 20% of patients assigned to buflomedil and 18% of those assigned to placebo; only gastrointestinal discomfort occurred more frequently in buflomedil-treated patients (3.4 versus 2%)

Uses

Buflomedil hydrochloride is a vasoactive agent. Its mode of action involves increasing the peripheral and cerebral blood flow in ischaemic tissues of patients, who are mostly affected with vascular diseases.
Buflomedil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in peripheral and cerebral vascular diseases

Biological Activity

Buflomedil is a non-selective antagonist of α-adrenergic receptors (α-ARs) and vasoactive compound.It binds to rat α1A- and α1B-ARs (Kis = 4.06 and 6.84 µM, respectively) and human platelet α2-ARs (IC50 = 1 µM) in radioligand binding assays.Buflomedil (0.06-60 µM) inhibits contraction of isolated canine saphenous veins induced by phenylephrine, clonidine, sympathetic nerve stimulation, or norepinephrine.It inhibits ADP-, collagen-, or epinephrine-induced aggregation of isolated human platelets when used at a concentration of 100 µM.Buflomedil (10 mg/kg) reduces hippocampal neuronal cell death in a rat model of carotid clamping-induced ischemia-reperfusion injury.
https://www.caymanchem.com

Synthesis

The target compound of buflomedil hydrochloride was synthesized from methyl 4-chlorobutyrate by condensation with pyrrolidine,then by hydrolysis,acylation,Fridel-crafts alkylation and salt formation.The structure of the target compound was confirmed by IR,1H-NMR and MS.The synthetic procedure is suitable for industrial production for the advantage of avaible materials,shorter routes,convenient operation and lower cost,the overall yield is improved from the reported 70% to 75.7%.
https://www.semanticscholar.org

Overdosage

Buflomedil is generally considered to be innocuous at therapeutic dosages. Acute toxicity is due to accidental or intentional overdosage. Overdosage causes generalized seizures and cardiac conduction abnormalities, eventually leading to cardiac arrest (SEDA-21, 215).
Meyler's Side Effects of Cardiovascular Drugs

Chemical Properties

White Solid

Originator

Fonzylane,Lafon,France,1976

Uses

1-[3-(2,4,6-Trimethoxybenzoyl)propyl]pyrrolidinium chloride is used as an vasodilator (peripheral).

Manufacturing Process

Introduce 33.6 g (0.2 mol) of 1,3,5-trimethoxybenzene and 100 ml of chlorobenzene into a 500 ml three-neck flask with stirrer, hydrochloric acid bubbler and condenser. Stir to dissolve and add 27.7 g of 4- pyrrolidinobutyronitrile (from 4-chlorobutyronitrile and pyrrolidine). Cool to about 15°-20°C and bubble hydrochloric acid gas in for 4 hours. Cool to about 5°C and add 200 cm3 of water. Stir. Decant the aqueous layer, wash again with 150 cm3 of water. Combine the aqueous layers, drive off the traces of chlorobenzene by distilling 150 cm3 of water, and heat under reflux for one hour. Cool and render alkaline by means of 60 ml of sodium hydroxide solution of 36° Baume. Extract twice with 100 ml of ether. Wash the ether with 100 ml of water. Dry the ether over sodium sulfate and slowly run in 50 ml of 5N hydrogen chloride solution in ether, at the boil. Cool in ice. Filter, wash with ether and dry in a vacuum oven. 33.6 g of crude product are obtained. Recrystallize from 200 ml of isopropanol in the presence of 3 SA carbon black. Filter. Wash and dry in a vacuum oven.
26.9 g of a white, crystalline water-soluble powder are obtained. Yield: 39.2%. Instantaneous melting point: 192°-193°C.

Therapeutic Function

Vasodilator

Buflomedil hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 323)Suppliers
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Hangzhou FandaChem Co.,Ltd.
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View Lastest Price from Buflomedil hydrochloride manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Buflomedil Hydrochloride pictures 2024-01-20 Buflomedil Hydrochloride
35543-24-9
US $9.90-9.90 / g 5g 99.99%HPLC.USP42——Powder、Oil、Pills、Capsules、Tablets,Customiz 100kg Wuhan Biocar Pharmacy Co., Ltd.
Buflomedil Hydrochloride pictures 2023-03-06 Buflomedil Hydrochloride
35543-24-9
US $8.70 / Kg/Bag 10g 99% 10000kg Hebei Guanlang Biotechnology Co,.LTD
Buflomedil hydrochloride pictures 2023-01-31 Buflomedil hydrochloride
35543-24-9
US $0.00-0.00 / kg 1kg 99% 5000kg Hebei Mojin Biotechnology Co., Ltd
  • Buflomedil Hydrochloride pictures
  • Buflomedil Hydrochloride
    35543-24-9
  • US $9.90-9.90 / g
  • 99.99%HPLC.USP42——Powder、Oil、Pills、Capsules、Tablets,Customiz
  • Wuhan Biocar Pharmacy Co., Ltd.

Buflomedil hydrochloride Spectrum

BUFLOMEDIL HCL EP BuflomedilHclC17H25No4.Hcl BUFLOMEDIL HYDROCHLORIDE ll1656 2',4',6-Trimethoxy-4-[1-pyrrolidinyl] butyrophenone hydrochloride Buflan Durabuflo Buflocit Buflonat Irrodan Irrodan R Lofton Loftyl Provas 1-(4-oxo-4-(2,4,6-triMethoxyphenyl)butyl)pyrrolidin-1-iuM chloride 4-(1-pyrrolidinyl)-1-(2,4,6-trimethoxyphenyl)-1-butanone,hydrochloride (1:1) 4-(pyrrolidin-1-yl)-1-(2,4,6-trimethoxyphenyl)butan-1-one hydrochloride Buflomedilhydrochloride(GMP) rrodan Bulflomedil HCL Buflomedil for peak identification 4-(1-pyrrolidinyl)-1-(2,4,6-trimethoxyphenyl)-1-butanonhydrochloride 4-(1-pyrrolidyl)-1-(2,4,6-trimethoxyphenyl)-1-butanonehydrochloride a-48257 bufedil chlorhydratede(trimethoxy-2-4-6)phenyl-(pyrrolidine-3)propylacetone fonzylane 1-[3-(2,4,6-trimethoxybenzoyl)propyl]pyrrolidinium chloride 4-(1-PYRROLIDINYL)-1-(2,4,6-TRIMETHOXYPHENYL)-1-BUTANONE HYDROCHLORIDE 4-[1-PYRROLIDINYL]-[2,4,6-TRIMETHOXYPHENYL]-1-BUTANONE HYDROCHLORIDE 4-(2,3,4,5-tetrahydropyrrol-1-yl)-1-(2,4,6-trimethoxyphenyl)-1-butanone chloride Buflomedil hydrochloride / Buflomedil HCl Buflomedil hydrochloride CRS Buflomedil for peak identification CRS Buflomedil Hydrochloride > 1-[3-(2,4,6-Trimethoxybenzoyl)propyl]pyrrolidinium chloride USP/EP/BP bulflomedil hydrochloride BUFLOMEDIL HCL Buflomedil Hydrochloride, ≥ 98.0% 35543-24-9 C17H25NO4ClH C17H26ClNO4 C17H25NO4HCl C18H27ClO4 BUFEDIL APIs API Pharmaceutical intermediate