Diphacinone 敌鼠

敌鼠　　diphacinone；diphacin

学名2-二苯基乙酰基-1,3-茚二酮。又名敌鼠钠盐、野鼠净。一种抗凝血的高效杀鼠剂。

药剂特性
纯品为黄色针状结晶。工业品是黄色无臭针状晶体，熔点146~147℃。不溶于水，溶于丙酮、乙醇等有机溶剂。钠盐溶于热水。两者化学性质都稳定。敌鼠的钠盐为淡黄色粉末，无臭无味，可溶于热水和乙醇等有机溶剂。 敌鼠是目前应用最广泛的第一代抗凝血杀鼠品种之一。具有适口性好、效果好等特点，一般抗药后4-6天出现死鼠。

毒理
在鼠体内不易分解和排泄。有抑制维生素K的作用，阻碍血液中凝血酶原的合成，使摄食该药的老鼠内脏出血不止而死亡。中毒个体无剧烈的不适症状，不易被同类警觉。

制备
由偏二苯基丙酮在甲醇钠催化剂存在下与苯二甲酸甲酯作用而制得。

主要剂型
80％敌鼠钠盐粉剂。 市售的是1%敌鼠粉剂和1%敌鼠钠盐。

防治对象及使用方法
敌鼠一般以配毒饵防治害鼠为主。防野栖鼠类使用浓度0．05-0．1%，每亩使用毒饵量75-150克。配饵可采用小麦小米、大米等。毒饵于傍晚投放于鼠洞附近，每洞口3克。第一天全洞投放，第二天检查，如已被吃掉，应立即补放。

注意事项
（1）对人毒性大，误食后可服用维生素K解毒，并及时遵医指导抢救。
（2）药剂应贮于阴凉、干燥处。

diphacinone
Rodenticide
indandione anticoagulant

NOMENCLATURE
Common name diphacinone (BSI, E-ISO, (m) F-ISO, ANSI); diphacins (JMAF); diphenadione (BAN); diphacin (former exception, Turkey); no name (Italy)
IUPAC name 2-(diphenylacetyl)indan-1,3-dione
Chemical Abstracts name 2-(diphenylacetyl)-1H-indene-1,3(2H)-dione
CAS RN [82-66-6] EEC no. 201-434-5

PHYSICAL CHEMISTRY
Composition Tech. is 95% pure. Mol. wt. 340.4 M.f. C23H16O3 Form Yellow crystals; (tech., yellow powder). M.p. 145-147 ºC V.p. 1.37 ´ 10-5 mPa (25 ºC, tech.) KOW logP = 4.27 Henry 1.55 ´ 10-5 Pa m3 mol-1 (calc.) S.g./density 1.281 Solubility Practically insoluble in water (c. 0.3 mg/kg). In chloroform 204, toluene 73, xylene 50, acetone 29, ethanol 2.1, heptane 1.8 (all in g/kg). Soluble in alkalis with the formation of salts. Stability Stable for 14 d (pH 6-9); hydrolysed in <24 h (pH 4). Rapidly decomposed in water by sunlight. Decomposes at 338 ºC (without boiling). pKa Acidic, forming water-soluble alkali metal salts.

COMMERCIALISATION
History Rodenticide reported by J. T. Correll et al. (Proc. Soc. Exp. Biol. Med., 1952, 80, 139). Introduced by Velsicol Chemical Corp. (became Novartis Crop Protection AG) and Upjohn Co. (both companies ceased to manufacture and market it). Patents US 2672483 Manufacturers Bell

APPLICATIONS
Biochemistry Anticoagulant; inhibits the vitamin K-dependent steps in the synthesis of coagulation factors II, VII and X. Mode of action Requires multiple feedings to produce lethal effects. Duration of action much longer than that of warfarin. Uses Control of rats, mice, voles, prairie dogs (Cynomys spp.), ground squirrels, and other rodents. Formulation types CB; RB. Compatibility Chemically and physically compatible with other rodenticides. Selected products: 'Ditrac' (Bell); 'Ramik' (Kemio, HACO)

OTHER PRODUCTS
'Promar' (HACO); 'Tomcat' (Antec) Discontinued products: 'Diphacin' * (Velsicol); 'Promer' * (Velsicol); 'Tomcat Rat and Mouse' * (Antec)

ANALYSIS
Product analysis by hplc (K. Hunter, Anal. Methods Pestic. Plant Growth Regul., 1988, 16, 119, 128). Residues determined by hplc or glc (idem, ibid.).

MAMMALIAN TOXICOLOGY
Oral Acute oral LD50 for rats 2.3, mice 50-300, rabbits 35, cats 14.7, dogs 3-7.5, pigs 150 mg/kg. Skin and eye Acute percutaneous LD50 for rats <200 mg/kg. Non-irritating to skin and eyes; non-sensitising to skin (guinea pigs). Inhalation LC50 (4 h) for rats <2 mg/l air (dust). NOEL Chronic LD50 for albino rats is 0.1 mg/kg daily. Other Non-mutagenic in the Ames test. Toxicity class WHO (a.i.) Ia; EPA (formulation) I EC classification T+; R28| T; R48/23/24/25

ECOTOXICOLOGY
Birds Acute oral LD50 for mallard ducks 3158 mg/kg. A 56-day secondary poisoning trial with bait (50 mg a.i./kg) revealed no hazard to sparrow hawks under conditions likely to be encountered in nature. Fish LC50 (96 h) for rainbow trout 2.6, bluegill sunfish 7.5, channel catfish 2.1 mg/l. Daphnia LC50 (48 h) 1.8 mg/l.

ENVIRONMENTAL FATE
EHC 175 (WHO, 1995) Animals Not extensively metabolised in the rat; any metabolism mainly involves hydroxylation and conjugation.