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S()-雷氯必利 (+)-酒石酸盐

S()-雷氯必利 (+)-酒石酸盐用途

酒石酸拉克洛普利是一种选择性多巴胺D2/D3受体拮抗剂,具有潜在的抗精神病作用。酒石酸拉氯普利特分别以1.8nm和3.5nm的Kis与D2和D3受体结合[1][2]。

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S()-雷氯必利 (+)-酒石酸盐名称

[ CAS 号 ]:
98185-20-7

[ 中文名 ]:
S(-)-雷氯必利(+)-酒石酸盐

[ 英文名 ]:
Raclopride tartrate

[英文别名 ]:

raclopride tartarate
raclopride tartrate
S(-)-RACLOPRIDE (+)-TARTRATE SALT

S()-雷氯必利 (+)-酒石酸盐生物活性

[ 描述 ]:

酒石酸拉克洛普利是一种选择性多巴胺D2/D3受体拮抗剂,具有潜在的抗精神病作用。酒石酸拉氯普利特分别以1.8nm和3.5nm的Kis与D2和D3受体结合[1][2]。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

[ 靶点 ]

D2 Receptor:1.8 nM (Ki)

D3 Receptor:3.5 nM (Ki)

D4 Receptor:2400 nM (Ki)

D1 Receptor:18000 nM (Ki)

[体内研究]

酒石酸Raclopride(0.1、0.3或0.6 mg/kg；IP；30分钟；O1系白化雄性小鼠)显著减少分配给攻击行为的时间[2]。

[参考文献]

[1]. Seeman P, et al. Dopamine receptor pharmacology. Trends Pharmacol Sci. 1994;15(7):264-270.

[2]. Aguilar MA, et al. Behavioral profile of raclopride in agonistic encounters between male mice. Pharmacol Biochem Behav. 1994;47(3):753-756.

S()-雷氯必利 (+)-酒石酸盐物理化学性质

[ 分子式 ]:
C₁₉H₂₆Cl₂N₂O₉

[ 分子量 ]:
497.32400

[ 精确质量 ]:
496.10200

[ PSA ]:
176.86000

[ LogP ]:
1.12790

[ 外观性状 ]:
固体

[ 储存条件 ]:
室温

S()-雷氯必利 (+)-酒石酸盐安全信息

[ 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

[ RTECS号 ]:
CV3465000

S()-雷氯必利 (+)-酒石酸盐文献

Effect of raclopride on dopamine D2 receptor mRNA expression in rat brain.

Neuroscience 47 , 771-779, (1992)

Prolonged treatment with dopamine D2 receptor antagonists is known to elevate the density of dopamine D2 receptor binding sites in caudate-putamen and nucleus accumbens in rat and human brain. In this...

Chronic treatment with the D1 receptor antagonist, SCH 23390, and the D2 receptor antagonist, raclopride, in cebus monkeys withdrawn from previous haloperidol treatment. Extrapyramidal syndromes and dopaminergic supersensitivity.

Psychopharmacology 112 , 389-397, (1993)

The effects of chronic treatment with dopamine (DA) D1 and D2 receptor antagonists were evaluated in eight cebus apella monkeys with mild oral dyskinesia after previous haloperidol treatment. SCH 2339...

Dopamine receptor antagonist properties of S 14506, 8-OH-DPAT, raclopride and clozapine in rodents.

Eur. J. Pharmacol. 271 , 167, (1994)

S 14506 (1-[-(4-fluorobenzoylamino)ethyl]-4-(7-methoxynaphthyl)piper azine hydrochloride), 8-OH-DPAT ((+/-)-8-hydroxydipropylaminotetralin hydrobromide), clozapine and raclopride were compared in some...

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