N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺

N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺用途

FG 7142 (ZK 39106; LSU-65) 是一种非选择性的苯二氮杂卓反向激动剂,对含 α1 亚基的 GABAA receptor 具有高亲和力 (Ki= 91 nM)。FG 7142 (ZK 39106; LSU-65) 还调节表达 α1 亚基的 GABAA 受体上 GABA 诱导的氯通量 (EC50= 137 nM)。FG 7142 (ZK 39106; LSU-65) 可以增加酪氨酸羟化并导致小鼠大脑皮层中 β-肾上腺素受体的上调。

N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺名称

[ CAS 号 ]:
78538-74-6

[ 中文名 ]:
N-甲基-beta-咔啉-3-羧酰胺

[ 英文名 ]:
FG 7142

[英文别名 ]:

B-carboline-3-carboxylic acid N-*methylamide
FG 7142

N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

[体外研究]

FG-7142对α亚基的表达具有亲和力,α1、α2、α3和α5亚基的Ki值分别为91nm、330nm、492nm和2.150μM[1]。FG-7142在表达α1亚基(EC50=137nm)的GABA a受体处调节GABA诱导的氯离子通量方面比其他α亚基(EC50:α2=507nm,α3=1.021μM,α5=1.439μM)有更高的效率[1]。

[体内研究]

FG-7142(腹腔注射；15-30mg/kg)激活大鼠大脑中边缘皮质多巴胺能投射,导致前额叶皮质和伏隔核多巴胺增加[1]。FG-7142(腹腔注射；15mg/kg)增加了体内前额叶内侧皮质和腹侧被盖的酪氨酸羟化酶活性和多巴胺周转率,但在中边缘或黑质纹状体区域没有发现影响[1]。

[参考文献]

[1]. Cottone P, et al. FG 7142 specifically reduces meal size and the rate and regularity of sustained feeding in female rats: evidence that benzodiazepine inverse agonists reduce food palatability.Neuropsychopharmacology. 2007 May;32(5):1069-81. Epub 2006 Nov 1.

N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺物理化学性质

[ 密度 ]:
1.328g/cm3

[ 沸点 ]:
576.3ºC at 760 mmHg

[ 分子式 ]:
C₁₃H₁₁N₃O

[ 分子量 ]:
225.24600

[ 闪点 ]:
302.3ºC

[ 精确质量 ]:
225.09000

[ PSA ]:
57.78000

[ LogP ]:
2.46660

[ 折射率 ]:
1.735

[ 储存条件 ]:
2-8°C

N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UU9780100

CHEMICAL NAME :: 9H-Pyrido(3,4-b)indole-3-carboxamide, N-methyl-

CAS REGISTRY NUMBER :: 78538-74-6

LAST UPDATED :: 199212

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C13-H11-N3-O

MOLECULAR WEIGHT :: 225.27

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 150 mg/kg

SEX/DURATION :: female 12-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: GEPHDP General Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.6- 1975- Volume(issue)/page/year: 22,53,1991

N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ WGK德国 ]:
3

[ RTECS号 ]:
UU9780100

[ 海关编码 ]:
2933990090

N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺合成路线

详细合成路线

N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺上下游产品

N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺上游产品

N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺下游产品

N-甲基-9H-吡啶[3,4-b]吲哚-3-甲酰胺海关

[ 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%

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