Tìm theo
Malathion
Các tên gọi khác (12 ) :
  • [(Dimethoxyphosphinothioyl)thio]butanedioic acid diethyl ester
  • Carbophos
  • Diethyl (dimethoxyphosphinothioylthio)succinate
  • Karbofos
  • Malathion
  • Maldison
  • Mercaptothion
  • O,O-Dimethyl S-(1,2-bis(ethoxycarbonyl)ethyl)
  • O,O-Dimethyl S-(1,2-dicarbethoxyethyl) dithiophosphate
  • O,O-Dimethyl S-(1,2-dicarbethoxyethyl)phosphorodithioate
  • O,O-Dimethyl S-1,2-di(ethoxycarbamyl)ethyl
  • O,O-Dimethyldithiophosphate diethylmercaptosuccinate
cholinesterase inhibitors, insecticides
Thuốc Gốc
Small Molecule
CAS: 121-75-5
ATC: P03AX03
ĐG : DPT Laboratories Ltd. , http://www.dptlabs.com
CTHH: C10H19O6PS2
PTK: 330.358
Malathion is a parasympathomimetic organophosphate compound that is used as an insecticide for the treatment of head lice. Malathion is an irreversible cholinesterase inhibitor and has low human toxicity.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H19O6PS2
Phân tử khối
330.358
Monoisotopic mass
330.036066232
InChI
InChI=1S/C10H19O6PS2/c1-5-15-9(11)7-8(10(12)16-6-2)19-17(18,13-3)14-4/h8H,5-7H2,1-4H3
InChI Key
InChIKey=JXSJBGJIGXNWCI-UHFFFAOYSA-N
IUPAC Name
1,4-diethyl 2-{[dimethoxy(sulfanylidene)-$l^{5}-phosphanyl]sulfanyl}butanedioate
Traditional IUPAC Name
malathion
SMILES
CCOC(=O)CC(SP(=S)(OC)OC)C(=O)OCC
Độ tan chảy
2.8 °C
Độ sôi
156-157 °C at 7.00E-01 mm Hg
Độ hòa tan
143 mg/L (at 20 °C)
logP
2.36
logS
-3.3
pKa (Strongest Basic)
-6.8
PSA
71.06 Å2
Refractivity
78.18 m3·mol-1
Polarizability
31.66 Å3
Rotatable Bond Count
11
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
0
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Malathion is an organophosphate insecticide commonly used to control mosquitos and other flying insects. Pharmaceutically, malathion is used to eliminate head lice. The principal toxicological effect of malathion is cholinesterase inhibition, due primarily to malaoxon and to phosphorus thionate impurities.
Cơ Chế Tác Dụng : Malathion is a parasympathomimetic organophosphate compound that is used as an insecticide for the treatment of head lice. Malathion is an irreversible cholinesterase inhibitor and has low human toxicity. Malathion is a nonsystemic, wide-spectrum organophosphate insecticide. It inhibits acetylcholinesterase activity of most eukaryotes. Malathion is toxic to aquatic organisms, but has a relatively low toxicity for birds and mammals. The major metabolites of malathion are mono- and di-carboxylic acid derivatives, and malaoxon is a minor metabolite. However, it is malaoxon that is the strongest cholinesterase inhibitor. Cholinesterases catalyze the hydrolysis of the neurotransmitter acetylcholine into choline and acetic acid, a reaction necessary to allow a cholinergic neuron to return to its resting state after activation. Because of its essential function, chemicals that interfere with the action of cholinesterase are potent neurotoxins, causing muscle spasms and ultimately death.
Dược Động Học :
▧ Absorption :
Malathion in an acetone vehicle has been reported to be absorbed through normal human skin only to the extent of 8% of the applied dose. Absorption may be increased when malathion is applied to damaged skin. Malathion is rapidly and effectively absorbed by practically all routes including the gastrointestinal tract, skin, mucous membranes, and lungs. However, it is readily excreted in the urine, and does not accumulate in organs or tissues.
▧ Metabolism :
The major metabolites of malathion are the diacid and monoacid metabolites, namely, malathion dicarboxylic acid (DCA) and malathion monocarboxylic acid (MCA). Malaoxon, the active cholinesterase-inhibiting metabolite of malathion, is a minor metabolite. Both malathion and malaoxon are detoxified by carboxyesterases leading to polar, water-soluble compounds that are excreted.
▧ Half Life :
8-24 hours
Độc Tính : Malathion is slightly toxic via the oral route, with reported oral LD50 values of 1000 mg/kg to greater than 10,000 mg/kg in the rat. It is also slightly toxic via the dermal route, with reported dermal LD50 values of greater than 4000 mg/kg in rats. Moderate poisoning can result in chest tightness, difficulty breathing, bradycardia, tachycardia, tremor/ataxia, blurred vision, and confusion. Severe, life-threatening signs include coma, seizures, respiratory arrest, and paralysis. Malathion may also be irritating to the skin and eyes.
Chỉ Định : For patients infected with Pediculus humanus capitis (head lice and their ova) of the scalp hair.
Liều Lượng & Cách Dùng : Lotion - Topical
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : SSL
    Sản phẩm biệt dược : Derbac-M
  • Công ty : Alfaco
    Sản phẩm biệt dược : Noury
  • Công ty : Taro
    Sản phẩm biệt dược : Ovide
  • Công ty : Norpharma
    Sản phẩm biệt dược : Prioderm
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00772
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4004
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505287
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07497
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00534
ChemSpider
http://www.chemspider.com/Chemical-Structure.3864.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50240924
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/68882-014-60
PharmGKB
http://www.pharmgkb.org/drug/PA164748092
Wikipedia
http://en.wikipedia.org/wiki/Malathion
RxList
http://www.rxlist.com/cgi/generic3/ovide.htm
Drugs.com
http://www.drugs.com/cdi/malathion.html
... loading
... loading