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SCH 23390盐酸盐

SCH 23390盐酸盐用途

SCH 23390 hydrochloride是有效的多巴胺受体D1拮抗剂,对D1和D5的Ki值分别为0.2和0.3 nM。

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SCH 23390盐酸盐名称

[ CAS 号 ]:
125941-87-9

[ 中文名 ]:
SCH 23390盐酸盐

[ 英文名 ]:
SCH 23390 hydrochloride

[英文别名 ]:

R(+)-SCH-23390 hydrochloride
SCH 23390（HCI)
SCH 23390 hydrochloride

SCH 23390盐酸盐生物活性

[ 描述 ]:

SCH 23390 hydrochloride是有效的多巴胺受体D1拮抗剂,对D1和D5的Ki值分别为0.2和0.3 nM。

[ 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 ]

Ki: 0.2 nM (D1), 0.3 nM (D5)[1]

[体外研究]

市售的盐酸盐的分子量为324.25,是可溶于水(8mg/mL),DMSO(3mg/mL)或乙醇(2mg/mL)的白色固体[1]。 SCH 23390还在h5-HT2C位点显示出高亲和力(Ki = 9.3nM)[2]。 SCH23390阻断AtT-20细胞中生长抑素或D3多巴胺受体诱导的内源性GIRK电流(IC50 = 268 nM)[3]。

[体内研究]

SCH 23390是更好地了解多巴胺系统作用的主要工具。 SCH 23390是一种非常短效的化合物,在大鼠腹腔注射0.3 mg/kg后,其消除半衰期约为25 min [1]。重复施用SCH 23390(0.05mg/kg sc,每天三次,持续21天)增强纹状体(+ 30％)和黑质(+ 24％)中多巴胺D1受体的稳态密度。这种治疗还增加了纹状体(+ 44％)和黑质(+ 54％)中多巴胺D1受体的产生率[4]。系统性SCH 23390通过显着降低主动杠杆响应和使用10μg/ kg SCH 23390进行预处理后音调+光线提示的主动杠杆-偶然分娩数量的显着减少来证明糖精寻求减少[5]。

[动物实验]

大鼠：所有大鼠在其测试日之前的两个下午1天接受适应性盐水注射。在训练阶段结束时，将大鼠（n = 15或16只大鼠/组）分配到三种条件中的一种（0,1或10μg/ kg SCH 23390的IP注射）。在训练阶段后的第二天，在操作6个调节室中测试大鼠的糖精提示反应性（糖精寻找）[5]。

[参考文献]

[1]. Bourne JA, et al . SCH 23390: the first selective dopamine D1-like receptor antagonist. CNS Drug Rev. 2001 Winter;7(4):399-414.

[2]. Millan MJ, et al. The "selective" dopamine D1 receptor antagonist, SCH23390, is a potent and high efficacy agonist at cloned human serotonin2C receptors. Psychopharmacology (Berl). 2001 Jun;156(1):58-62.

[3]. Kuzhikandathil EV, et al. Classic D1 dopamine receptor antagonist R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (SCH23390) directly inhibits G protein-coupledinwardly rectifying potassium channels. Mol Pharmacol. 2002 Jul;62(1):119-26.

[4]. Giorgi O, et al. Chronic treatment with SCH 23390 increases the production rate of dopamine D1 receptors in the nigro-striatal system of the rat. Eur J Pharmacol. 1993 Apr 15;245(2):139-45.

[5]. Aoyama K, et al. Systemic injection of the DAD1 antagonist SCH 23390 reduces saccharin seeking in rats. Appetite. 2016 Oct 1;105:8-13.

[相关活性小分子]

SCH 23390盐酸盐物理化学性质

[ 沸点 ]:
414.7ºC at 760 mmHg

[ 分子式 ]:
C₁₇H₁₉Cl₂NO

[ 分子量 ]:
324.245

[ 闪点 ]:
204.6ºC

[ 精确质量 ]:
323.084381

[ PSA ]:
23.47000

[ LogP ]:
4.40530

[ 蒸汽压 ]:
1.81E-07mmHg at 25°C

[ 储存条件 ]:
室温，保存在惰性气体中

SCH 23390盐酸盐MSDS

详细MSDS(安全技术说明书)

SCH 23390盐酸盐安全信息

[ 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

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