Afloqualone - CAS 56287-74-2
Catalog number: 56287-74-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C16H14FN3O
Molecular Weight:
283.3
COA:
Inquire
Targets:
GABA Receptor
Description:
Afloqualone is a agonist of GABA receptor has sedative and muscle-relaxant effects.
Purity:
≥98%
Appearance:
White to off-white solid
Synonyms:
6-amino-2-(fluoromethyl)-3-(2-methylphenyl)quinazolin-4-one;
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
A agonist of GABA receptor
Quality Standard:
Enterprise Standard/USP/EP
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Grams-Kilos
Melting Point:
195-196 °C
InChIKey:
VDOSWXIDETXFET-UHFFFAOYSA-N
InChI:
1S/C16H14FN3O/c1-10-4-2-3-5-14(10)20-15(9-17)19-13-7-6-11(18)8-12(13)16(20)21/h2-8H,9,18H2,1H3
Canonical SMILES:
CC1=CC=CC=C1N2C(=NC3=C(C2=O)C=C(C=C3)N)CF
Current Developer:
Tanabe Seiyaku
1.Determination of afloqualone in human plasma using liquid chromatography/tandem mass spectrometry: Application to pharmacokinetic studies in humans.
Yun HY1, Lee SP, Jeong HH, Yoon YR, Sohn SJ, Kim SK, Kang W, Kwon KI. Talanta. 2007 Oct 15;73(4):635-43. doi: 10.1016/j.talanta.2007.04.039. Epub 2007 May 1.
Two methods for determining the central-acting muscle relaxant afloqualone in human plasma were developed and compared using API2000 and API4000 liquid chromatography tandem mass spectrometry (LC/MS/MS) systems. In the API2000 LC/MS/MS system, afloqualone and the internal standard methaqualone were extracted from plasma using a methyl-tertiary ether. After drying the organic layer, the residue was reconstituted in a mobile phase (0.1% formic acid-acetonitrile:0.1% formic acid buffer, 80:20 v/v) and injected onto a reversed-phase C(18) column. The isocratic mobile phase was eluted at 0.2ml/min. The ion transitions monitored in multiple reaction-monitoring mode were m/z 284-->146 and 251-->117 for afloqualone and methaqualone, respectively. Sample preparation for the API4000LC/MS/MS system involved simple protein precipitation with an organic mixture (methanol:10% ZnSO(4)=8:2). The ion transitions monitored in multiple reaction-monitoring mode were m/z 284-->146 and 251-->131 for afloqualone and methaqualone, respectively.
2.Photodynamic DNA-breaking activity of serum from patients with various photosensitivity dermatoses.
Hashizume H1, Tokura Y, Oku T, Iwamoto Y, Takigawa M. Arch Dermatol Res. 1995;287(6):586-90.
Various drugs and chemicals break the DNA strand under ultraviolet irradiation. This study aimed to clarify the DNA-breaking activity (DBA) of serum from 39 patients with various photosensitivity disorders and that from eight normal subjects. A mixture of serum and circular plasmid DNA was exposed to longwave ultraviolet radiation, and the photoinduced cleavage of plasmid DNA was examined by electrophoretic analysis. DBA was found in serum from patients with erythropoietic protoporphyria (2 of 2), drug-induced photosensitivity (3 of 5), chronic actinic dermatitis (1 of 12) and hydroa vacciniforme (1 of 1). DBA was not found in serum from patients with porphyria cutanea tarda, collagen diseases with photosensitivity, papulovesicular light eruption or pellagra. The inhibition profile of DBA by active oxygen scavengers was different between afloqualone- and tetracycline-induced photosensitivity and chronic actinic dermatitis. The present method was useful for the detection of serum phototoxicity and the investigation of the pathomechanisms of photosensitivity.
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CAS 56287-74-2 Afloqualone

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