2,3,4,5-四氢-2,8-二甲基-5-[2-(6-甲基吡啶-3-基)乙基]-1H-吡啶并[4,3-b]吲哚

用途

Latrepirdine is an orally-available drug, approved in Russia for use as a non-selective antihistamine, that has shown promise in the treatment of neurodegenerative diseases, including Alzheimer’s and Huntington’s disease. In addition to reported activity in preventing the onset and progression of disease by being neuroprotective, dimebolin appears to promote clinical improvement by increasing cognitive function. At the cellular level, dimebolin appears to have diverse effects, inhibiting the neurotoxic action of β-amyloid and blocking L-type calcium channels,5 inhibiting NMDA-type glutamate receptors, and preventing mitochondrial leakage.

名称

[ CAS 号 ]:
3613-73-8

[ 中文名 ]:
2,3,4,5-四氢-2,8-二甲基-5-[2-(6-甲基吡啶-3-基)乙基]-1H-吡啶并[4,3-b]吲哚

[ 英文名 ]:
Latrepirdine

[中文别名 ]:

丹吡芙蓉

[英文别名 ]:

Dimebolin
Dimebon
aka latrepiridine
Dimebone
Latrepirdine
Dimeboline
Preparation 84

物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
505.7±50.0 °C at 760 mmHg

[ 熔点 ]:
115-116 °C

[ 分子式 ]:
C₂₁H₂₅N₃

[ 分子量 ]:
319.443

[ 闪点 ]:
259.7±30.1 °C

[ 精确质量 ]:
319.204834

[ PSA ]:
21.06000

[ LogP ]:
3.96

[ 外观性状 ]:
棕褐色固体

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.629

[ 储存条件 ]:
室温

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UV0625000

CHEMICAL NAME :: 1H-Pyrido(4,3-b)indole, 2,3,4,5-tetrahydro-2,8-dimethyl-5-(2-(6-methyl-3-pyri dyl)ethyl)-

CAS REGISTRY NUMBER :: 3613-73-8

BEILSTEIN REFERENCE NO. :: 0622478

LAST UPDATED :: 199612

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C21-H25-N3

MOLECULAR WEIGHT :: 319.49

WISWESSER LINE NOTATION :: T B656 DN HNTT&J D1 L1 H2- ET6NJ B1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 356 mg/kg

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

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 46(5),90,1983

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 178 mg/kg

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

REFERENCE :: RPTOAN Russian Pharmacology and Toxicology (English Translation). Translation of FATOAO. (Euromed Pub., 33, Woodlands Rd., Surbiton, Surrey, UK) V.30- 1967- Volume(issue)/page/year: 31,105,1968 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1500 mg/kg

SEX/DURATION :: female 8-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - other developmental abnormalities

REFERENCE :: FATOAO Farmakologiya i Toksikologiya (Moscow). For English translation, see PHTXA6 and RPTOAN. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.2- 1939- Volume(issue)/page/year: 48(6),89,1985

安全信息

[ 危害码 (欧洲) ]:
Xi