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碘解磷定

碘解磷定用途

Pralidoxime iodide 是乙酰胆碱酯酶 (AChE) 的活化剂。Pralidoxime iodide 能激活神经毒剂,抑制乙酰胆碱酯酶的活性,其途径是通过结合神经毒剂磷中心的肟部分直接亲核攻击。Pralidoxime iodide 是有机磷中毒的解毒剂。
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碘解磷定名称

[ CAS 号 ]:
94-63-3

[ 中文名 ]:
碘解磷啶

[ 英文名 ]:
Pralidoxime Iodide

[中文别名 ]:

[英文别名 ]:

碘解磷定生物活性

[ 描述 ]:

Pralidoxime iodide 是乙酰胆碱酯酶 (AChE) 的活化剂。Pralidoxime iodide 能激活神经毒剂,抑制乙酰胆碱酯酶的活性,其途径是通过结合神经毒剂磷中心的肟部分直接亲核攻击。Pralidoxime iodide 是有机磷中毒的解毒剂。

[ 相关类别 ]:

研究领域 >> 神经疾病
信号通路 >> 神经信号通路 >> 疼痛

[体内研究]

碘解磷定(10-150 mg/kg；i.m.)逆转对氧磷诱导的小鼠呼吸毒性[3]。动物模型：雄性F1B6D2小鼠(清醒、无束缚小鼠的二乙基对氧磷中毒但非致死模型)[3]剂量：10、50、100和150 mg/kg给药：肌肉结果：150 mg/kg时二乙基对氧磷诱导的呼吸毒性逆转。

[参考文献]

[1]. Cadieux CL, et al. Probing the activity of a non-oxime reactivator for acetylcholinesterase inhibited by organophosphorus nerve agents. Chem Biol Interact. 2016;259(Pt B):133‐141.

[2]. Eyer P, Buckley N. Pralidoxime for organophosphate poisoning. Lancet. 2006;368(9553):2110‐2111.

[3]. Houzé P, et al. High Dose of Pralidoxime Reverses Paraoxon-Induced Respiratory Toxicity in Mice. Turk J Anaesthesiol Reanim. 2018;46(2):131‐138.

碘解磷定物理化学性质

[ 密度 ]:
1.7439 g/ml

[ 熔点 ]:
220 °C (dec.)(lit.)

[ 分子式 ]:
C7H9IN2O

[ 分子量 ]:
264.064

[ 精确质量 ]:
263.975952

[ PSA ]:
36.47000

[ 外观性状 ]:
淡黄色针状结晶性粉末

[ 储存条件 ]:
2-8°C

碘解磷定MSDS

详细MSDS(安全技术说明书)

碘解磷定毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UU4375000
CHEMICAL NAME :
Pyridinium, 2-formyl-1-methyl-, iodide, oxime
CAS REGISTRY NUMBER :
94-63-3
LAST UPDATED :
199710
DATA ITEMS CITED :
12
MOLECULAR FORMULA :
C7-H9-N2-O.I
MOLECULAR WEIGHT :
264.08
WISWESSER LINE NOTATION :
T6KJ A1 B1UNQ &Q &I

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
305 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
BJPCAL British Journal of Pharmacology and Chemotherapy. (London, UK) V.1-33, 1946-68. For publisher information, see BJPCBM. Volume(issue)/page/year: 13,202,1958
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
178 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 129,31,1960
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
249 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 129,31,1960
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1500 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JPMSAE Journal of Pharmaceutical Sciences. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.50- 1961- Volume(issue)/page/year: 53,1143,1964
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
136 mg/kg
TOXIC EFFECTS :
Lungs, Thorax, or Respiration - other changes
REFERENCE :
ABBIA4 Archives of Biochemistry and Biophysics. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.31- 1951- Volume(issue)/page/year: 60,261,1956
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
140 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
AEHLAU Archives of Environmental Health. (Heldref Pub., 4000 Albemarle St., NW, Washington, DC 20016) V.1- 1960- Volume(issue)/page/year: 5,21,1962
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
145 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 132,50,1961
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
240 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 14,5,1964 *** REVIEWS *** TOXICOLOGY REVIEW JPMSAE Journal of Pharmaceutical Sciences. (American Pharmaceutical Assoc., 2215 Constitution Ave., NW, Washington, DC 20037) V.50- 1961- Volume(issue)/page/year: 53,1143,1964 TOXICOLOGY REVIEW JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 166,1834,1958 TOXICOLOGY REVIEW AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New York, NY 10022) V.1- 1946- Volume(issue)/page/year: 50,475,1971
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碘解磷定安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
UU4375000

碘解磷定合成路线

详细合成路线

碘解磷定上下游产品

碘解磷定上游产品

碘解磷定下游产品

碘解磷定制备

氯解磷定置换得到。将氯解磷定加等量水，加热溶解，搅拌下滴加碘化钾饱和溶液，析出结晶，过滤，甩干。再用蒸馏水重结晶，活性炭脱色得碘解磷定。

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碘解磷定文献

A trivalent approach for determining in vitro toxicology: Examination of oxime K027.

J. Appl. Toxicol. 35(2) , 219-27, (2014)

Unforeseen toxic effects contribute to compound attrition during preclinical evaluation and clinical trials. Consequently, there is a need to correlate in vitro toxicity to in vivo and clinical outcom...

Reactions of methylphosphonic difluoride with human acetylcholinesterase and oximes--Possible therapeutic implications.

Toxicol. Lett. 231(1) , 92-8, (2014)

Highly toxic organophosphorus (OP) nerve agents are well characterized regarding chemical, biological and toxicological properties and the effectiveness of standard atropine and oxime therapy. Open li...

An in vivo zebrafish screen identifies organophosphate antidotes with diverse mechanisms of action.

J. Biomol. Screen. 18(1) , 108-15, (2013)

Organophosphates are a class of highly toxic chemicals that includes many pesticides and chemical weapons. Exposure to organophosphates, either through accidents or acts of terrorism, poses a signific...


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