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CAS No.: 1049747-87-6

SB 242084 2HCl Catalog No. CSN13111

Synonyms: SB-242084 (hydrochloride);SB 242084 HCl;SB-242084

SB-242084 2HCl is a selective and brain-penetrant antagonist for the 5HT2C receptor.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 5-HT Receptor 2C

pKi:9
描述SB-242084 Dihydrochloride is an antagonist of the serotonin type 2C receptor (5-HT2CR), as potential pharmacotherapeutics for various affective disorders. In vivo, pretreatment with SB 242084 (0.1 mg/kg) modulated cocaine-induced dopamine increases within the nucleus accumbens, but not the caudate nucleus, of awake subjects. The mean response rate (± S.E.M.) maintained by a fixed-interval 300-s schedule of stimulus termination after vehicle pretreatments of both SB 242084 and cocaine was 0.39 ± 0.07 responses/s. When administered alone, one-way ANOVA with post hoc analyses indicated that 0.03 and 0.1 mg/kg SB 242084 significantly increased response rates up to 137 and 154% baseline, respectively^[3].
参考文献

[1] Bromidge SM, Duckworth M, et al. 6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy] -5-pyridyl] carbamoyl] - indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist. J Med Chem. 1997 Oct 24;40(22):3494-6.
[2] Kennett GA, Wood MD, et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
[3] Manvich DF, Kimmel HL, Cooper DA, Howell LL. The serotonin 2C receptor antagonist SB 242084 exhibits abuse-related effects typical of stimulants in squirrel monkeys. J Pharmacol Exp Ther. 2012 Sep;342(3):761-9.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1378 mL
- 10.6889 mL
- 21.3778 mL
- 5 mM
- 0.4276 mL
- 2.1378 mL
- 4.2756 mL
- 10 mM
- 0.2138 mL
- 1.0689 mL
- 2.1378 mL

技术信息

CAS号

1049747-87-6

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H21Cl3N4O2

运输

蓝冰

分子量

467.78

别名

SB-242084 (hydrochloride);SB 242084 HCl;SB-242084

溶解度

DMSO	125.5 mg/mL (268.3 mM)

动物实验配方

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SB 242084 2HCl Catalog No. CSN13111

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