1-氨基-2,3-二氢-1H-茚-1,5-二羧酸

1-氨基-2,3-二氢-1H-茚-1,5-二羧酸用途

UPF-523(AIDA)是一种刚性(羧基苯基)甘氨酸衍生物,是I组代谢型谷氨酸受体(mGlu1a)的相对有效和选择性拮抗剂,IC50为214μM。但UPF-523对II组(mGlu2)、III组(mGlu4)受体或离子型谷氨酸受体没有影响。UPF-523具有研究急性关节炎的潜力[1][2]。

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1-氨基-2,3-二氢-1H-茚-1,5-二羧酸名称

[ CAS 号 ]:
168560-79-0

[ 中文名 ]:
1-氨基-2,3-二氢-1H-茚-1,5-二羧酸

[ 英文名 ]:
AIDA

[英文别名 ]:

1-AMINOINDAN-1,5-DICARBOXYLIC ACID,UPF 5 23
MFCD00672638
(R,S)-1-Aminoindane-1,5
Valerenic acid

1-氨基-2,3-二氢-1H-茚-1,5-二羧酸生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 谷氨酸受体

[ 靶点 ]

mGluR1a:214 μM (IC50)

[体内研究]

UPF-523(0.18 mg/kg；i.p；0.5 ml/100 g)的最终浓度为100–150 mM,低于214 mM的IC50[1]。动物模型：幼年雄性带帽Lister大鼠(320-350 g)[1]剂量：0.18 mg/kg给药：腹腔注射。；每100克0.5毫升结果：未显示任何粗大运动异常和正常翻正反射。

[参考文献]

[1]. Nielsen KS, et al. Class I mGlu receptor antagonist 1-aminoindan-1,5-dicarboxylic acid blocks contextual but not cue conditioning in rats. Eur J Pharmacol. 1997;326(2-3):105-108.

[2]. Zhang LP, et al. The Role of Type 1 Metabotropic Glutamate Receptors in the Generation of Dorsal Root Reflexes Induced by Acute Arthritis or the Spinal Infusion of 4-Aminopyridine in the Anesthetized Rat. J Pain. 2000;1(2):151-161.

1-氨基-2,3-二氢-1H-茚-1,5-二羧酸物理化学性质

[ 密度 ]:
1.481 g/cm3

[ 沸点 ]:
470.4ºC at 760 mmHg

[ 分子式 ]:
C₁₁H₁₁NO₄

[ 分子量 ]:
221.20900

[ 闪点 ]:
238.3ºC

[ 精确质量 ]:
221.06900

[ PSA ]:
100.62000

[ LogP ]:
1.26990

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
1.19E-09mmHg at 25°C

1-氨基-2,3-二氢-1H-茚-1,5-二羧酸安全信息

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

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S37/39

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

[ 海关编码 ]:
2922499990

1-氨基-2,3-二氢-1H-茚-1,5-二羧酸海关

[ 海关编码 ]: 2922499990

[ 中文概述 ]:
2922499990 其他氨基酸及其酯及它们的盐（含有一种以上含氧基的除外）. 增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: P.进境动植物、动植物产品检疫 Q.出境动植物、动植物产品检疫 R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验

[ Summary ]:
HS:2922499990 other amino-acids, other than those containing more than one kind of oxygen function, and their esters; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%

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