R(+)-3-氨基-1-羟基-2-吡咯烷酮

R(+)-3-氨基-1-羟基-2-吡咯烷酮用途

(R)-(+)-HA-966 ((+)-HA-966) 是 N-甲基-D-天冬氨酸 (NMDA) 受体复合物的甘氨酸位点的部分激动剂/拮抗剂。(R)-(+)-HA-966 通过苯丙胺选择性阻断中脑边缘多巴胺系统的活化。(R)-(+)-HA-966 可透过血脑屏障,有用于神经性和急性疼痛的潜力。

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R(+)-3-氨基-1-羟基-2-吡咯烷酮名称

[ CAS 号 ]:
123931-04-4

[ 中文名 ]:
R(+)-3-氨基-1-羟基-2-吡咯烷酮

[ 英文名 ]:
(R)-(+)-HA-966

[英文别名 ]:

MFCD00078583
R(+)-3-Amino-1-hydroxy-2-pyrrolidinone

R(+)-3-氨基-1-羟基-2-吡咯烷酮生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> iGluR

研究领域 >> 神经疾病

信号通路 >> 跨膜转运 >> iGluR

[ 靶点 ]

glycine site of the NMDA receptor[1][2]

[体内研究]

(R) -(+)-HA-966(+)-HA-966；10 mg/kg；i v)显著减弱全身NMDA(125、250、500和1000 mg/kg；i.v.)引起的剂量依赖性升压反应和相关的心动过速反应[3]。(+)-HA-966(30100 mg/kg；IP)剂量依赖性地阻断安非他明对伏隔核多巴胺合成的增强作用,但对雄性BKTO小鼠纹状体多巴胺合成的增加没有影响(20-30g)[1]。动物模型：Sprague-Dawley大鼠(11～12周龄)[3]剂量：10mg/kg给药：IV结果：明显减弱全身NMDA引起的剂量依赖性升压反应及相关心动过速反应。

[参考文献]

[1]. Hutson PH, et al. R-(+)-HA-966, a glycine/NMDA receptor antagonist, selectively blocks the activation of the mesolimbic dopamine system by amphetamine. Br J Pharmacol. 1991 Aug;103(4):2037-44.

[2]. Witkin JM, et al. Discriminative stimulus effects of R-(+)-3-amino-1-hydroxypyrrolid-2-one, [(+)-HA-966], a partial agonist of the strychnine-insensitive modulatory site of the N-methyl-D-aspartate receptor. J Pharmacol Exp Ther. 1995 Dec;275(3):1267-73.

[3]. Christensen D, et al. The antinociceptive effect of combined systemic administration of morphine and the glycine/NMDA receptor antagonist, (+)-HA966 in a rat model of peripheral neuropathy. Br J Pharmacol. 1998 Dec;125(8):1641-50.

R(+)-3-氨基-1-羟基-2-吡咯烷酮物理化学性质

[ 密度 ]:
1.436g/cm3

[ 沸点 ]:
258.6ºC at 760mmHg

[ 分子式 ]:
C₄H₈N₂O₂

[ 分子量 ]:
116.11900

[ 闪点 ]:
110.2ºC

[ 精确质量 ]:
116.05900

[ PSA ]:
66.56000

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.002mmHg at 25°C

[ 折射率 ]:
1.59

R(+)-3-氨基-1-羟基-2-吡咯烷酮MSDS

详细MSDS(安全技术说明书)

R(+)-3-氨基-1-羟基-2-吡咯烷酮安全信息

[ 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

R(+)-3-氨基-1-羟基-2-吡咯烷酮文献

Enantiomers of HA-966 (3-amino-1-hydroxypyrrolid-2-one) exhibit distinct central nervous system effects: (+)-HA-966 is a selective glycine/N-methyl-D-aspartate receptor antagonist, but (-)-HA-966 is a potent gamma-butyrolactone-like sedative.

Proc. Natl. Acad. Sci. U. S. A. 87 , 347, (1990)

The antagonist effect of (+/-)-3-amino-1-hydroxypyrrolid-2-one (HA-966) at the N-methyl-D-aspartate (NMDA) receptor occurs through a selective interaction with the glycine modulatory site within the r...

The discriminative stimulus properties of (+)-HA-966, an antagonist at the glycine/N-methyl-D-aspartate receptor.

Eur. J. Pharmacol. 186 , 129, (1990)

Using a two-lever operant drug discrimination paradigm, rats have been trained to discriminate between the administration of saline and R-(+)-HA-966 (R-(+)-3-amino-1-hydroxypyrrolid-2-one, 30 mg/kg i....

Stereoselectivity for the (R)-enantiomer of HA-966 (1-hydroxy-3-aminopyrrolidone-2) at the glycine site of the N-methyl-D-aspartate receptor complex.

J. Neurochem. 55 , 1346, (1990)

HA-966 (1-hydroxy-3-aminopyrrolidone-2) is an antagonist at the glycine allosteric site of the N-methyl-D-aspartate receptor ionophore complex. Unlike presently known glycine antagonists, HA-966 is ch...

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