SB 242084 2HCl

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Chemical Structure| 1049747-87-6 同义名 : SB-242084 (hydrochloride);SB 242084 dihydrochloride
CAS号 : 1049747-87-6
货号 : A253004
分子式 : C21H21Cl3N4O2
纯度 : 98%+
分子量 : 467.776
MDL号 : MFCD02684417
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(224.47 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.69mL

2.14mL

1.07mL

21.38mL

4.28mL

2.14mL
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.