水杨酸毒扁豆碱

水杨酸毒扁豆碱用途

Physostigmine salicylate (Eserine salicylate) 是一种可逆的乙酰胆碱酯酶 (AChE) 抑制剂。Physostigmine salicylate 可以透过血脑屏障并刺激中枢胆碱能神经传递。Physostigmine salicylate 能逆转阿尔茨海默病转基因小鼠的记忆缺陷。Physostigmine salicylate 也是抗胆碱能中毒的解毒剂。

水杨酸毒扁豆碱名称

[ CAS 号 ]:
57-64-7

[ 中文名 ]:
伊色林水杨酸盐

[ 英文名 ]:
Physostigmine salicylate

[中文别名 ]:

[英文别名 ]:

EINECS 200-343-8
MFCD00135659
Physostigmine Salicylate

水杨酸毒扁豆碱生物活性

[ 描述 ]:

[ 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]

水杨酸毒扁豆碱；0.03-0.3mg/kg；s、 c。；每天6周)改善Tg(+)小鼠上下文和线索记忆的缺陷[2]。水杨酸毒扁豆碱(IV；0.1,0.2mg/kg)延迟异氟醚麻醉后的苏醒时间≥雄性Sprague-Dawley大鼠0.2 mg/kg[4]。动物模型：杂合子转基因小鼠(Tg(+)小鼠)[2]剂量：0.03、0.1、0.3mg/kg给药：SC；结果：Tg(+)组动物的背景记忆缺损趋于正常化,与Tg(-)组动物更为相似。

[参考文献]

[1]. Haase U, et al. Pharmakotherapie--physostigmin post OP [Pharmacotherapy--physostigmine administered post-operatively]. Anasthesiol Intensivmed Notfallmed Schmerzther. 2007;42(3):188‐189.

[2]. Dong H, et al, Bertchume A, Vallera D, Csernansky JG. Acetylcholinesterase inhibitors ameliorate behavioral deficits in the Tg2576 mouse model of Alzheimer's disease. Psychopharmacology (Berl). 2005;181(1):145‐152.

[3]. Frascogna N. Physostigmine: is there a role for this antidote in pediatric poisonings?. Curr Opin Pediatr. 2007;19(2):201‐205.

[4]. Jonathan D Kenny, et al. Physostigmine and Methylphenidate Induce Distinct Arousal States During Isoflurane General Anesthesia in Rats. Anesth Analg. 2016 Nov;123(5):1210-1219.

水杨酸毒扁豆碱物理化学性质

[ 沸点 ]:
393.5ºC at 760 mmHg

[ 熔点 ]:
181-183 °C

[ 分子式 ]:
C₂₂H₂₇N₃O₅

[ 分子量 ]:
413.46700

[ 闪点 ]:
191.8ºC

[ 精确质量 ]:
413.19500

[ PSA ]:
102.34000

[ LogP ]:
3.25810

[ 外观性状 ]:
无色晶体,无臭

[ 储存条件 ]:
2-8°C

水杨酸毒扁豆碱MSDS

详细MSDS(安全技术说明书)

水杨酸毒扁豆碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TJ2450000

CAS REGISTRY NUMBER :: 57-64-7

LAST UPDATED :: 199706

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C15-H21-N3-O2.C7-H6-O3

MOLECULAR WEIGHT :: 413.52

WISWESSER LINE NOTATION :: T B556 EN GNTT&J B1 E1 G1 KOVM1 &QR BVO

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 14 ug/kg

TOXIC EFFECTS :: Cardiac - arrhythmias (including changes in conduction) Gastrointestinal - nausea or vomiting

REFERENCE :: JCLPDE Journal of Clinical Psychiatry. (Physicians Postgraduate Press, Inc., POB 240008, Memphis, TN 38124) V.39- 1978- Volume(issue)/page/year: 46,446,1985

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 25,569,1973

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1280 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DCTODJ Drug and Chemical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.1- 1977/78- Volume(issue)/page/year: 7,507,1984

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2500 ug/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 81,276,1950

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 640 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 28,227,1974

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 800 ug/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis

REFERENCE :: JPPMAB Journal of Pharmacy and Pharmacology. (Pharmaceutical Soc. of Great Britain, 1 Lambeth High St., London SEI 7JN, UK) V.1- 1949- Volume(issue)/page/year: 34,603,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 310 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 20,474,1971

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1200 ug/kg

TOXIC EFFECTS :: Autonomic Nervous System - other (direct) parasympathomimetic Behavioral - coma Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB158-508

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 800 ug/kg

TOXIC EFFECTS :: Autonomic Nervous System - other (direct) parasympathomimetic Behavioral - coma Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: NTIS** National Technical Information Service. (Springfield, VA 22161) Formerly U.S. Clearinghouse for Scientific & Technical Information. Volume(issue)/page/year: PB158-508

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 2 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AEXPBL Archiv fuer Experimentelle Pathologie und Pharmakologie. (Leipzig, Ger. Dem. Rep.) V.1-109, 1873-1925. For publisher information, see NSAPCC. Volume(issue)/page/year: 53,313,1905

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1570 ug/kg

TOXIC EFFECTS :: Behavioral - tremor

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 81,276,1950 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 200 ug/kg

SEX/DURATION :: male 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - mating performance (e.g. # sperm positive females per # females mated; # copulations per # estrus cycles)

REFERENCE :: PHBHA4 Physiology and Behavior. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1966- Volume(issue)/page/year: 4,677,1969 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 80481 No. of Facilities: 68 (estimated) No. of Industries: 1 No. of Occupations: 6 No. of Employees: 2770 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 80481 No. of Facilities: 54 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 1828 (estimated) No. of Female Employees: 1354 (estimated)

水杨酸毒扁豆碱安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300-H330

[ 警示性声明 ]:
P260-P264-P284-P301 + P310-P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T+: Very toxic;

[ 风险声明 (欧洲) ]:
R26/28

[ 安全声明 (欧洲) ]:
S25-S45

[ 危险品运输编码 ]:
UN 1544 6.1/PG 1

[ WGK德国 ]:
3

[ RTECS号 ]:
TJ2450000

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
2933990090

水杨酸毒扁豆碱海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

水杨酸毒扁豆碱文献

Possible interaction of cholinergic and GABAergic systems between MS and CA1 upon memory acquisition in rats.

Behav. Brain Res. 235(2) , 231-43, (2012)

The present study explored the possibility that cholinergic and GABAergic systems of medial septum (MS) might influence acquisition of memory by regulation of acetylcholine (Ach) and γ-aminobutyric ac...

The effects of physostigmine infusion on patients with panic disorder.

Biol. Psychiatry 29(7) , 658-64, (1991)

Nine patients who met both DSM-III and RDC criteria for panic disorder and nine age-matched normal controls received infusions of physostigmine. The patients and normal controls did not differ in eith...

Development and optimization of a sublingual tablet formulation for physostigmine salicylate.

Acta. Pharm. 59(3) , 301-12, (2009)

This study is aimed to design and optimize a sublingual tablet formulation of physostigmine salicylate, an effective drug in Alzheimer's disease and nerve gas poisoning, by means of the D-optimal expe...

更多文献