SB 242084 2HCl | SB-242084 (hydrochloride) | 5-HT2C Receptor Antagonist

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SB 242084 2HCl 99%+

货号：A253004 同义名： SB-242084 (hydrochloride);SB 242084 dihydrochloride

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

SB 242084 2HCl 化学结构
CAS号：1049747-87-6

SB 242084 2HCl 3D分子结构
CAS号：1049747-87-6

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SB 242084 2HCl 纯度/质量文件产品仅供科研

货号：A253004 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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5-羟色胺受体亚型比较

产品名称	5-HT ↓ ↑	5-HT1 ↓ ↑	5-HT2 ↓ ↑	5-HT3 ↓ ↑	5-HT5 ↓ ↑	5-HT6 ↓ ↑	5-HT7 ↓ ↑	其他靶点	纯度
Desvenlafaxine	++ 5-HT, Ki: 40.2 nM								98%
Lamotrigine	+ 5-HT (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 μM								99%+
Venlafaxine	✔								99%+
Fluvoxamine maleate	✔								99%
Iloperidone	✔								99%+
Ziprasidone HCl	✔								98+%
Atomoxetine HCI	+ 5-HT, Ki: 77 nM								98%
Dapoxetine HCl	✔								99%+
Trazodone	✔								98+%
Clomipramine HCl	✔								99%+
Mirtazapine	✔								99+%
Escitalopram oxalate	+++ 5-HT, Ki: 0.89 nM								99%+
Duloxetine	✔								98+%
Sertraline HCl	++ 5-HT, Ki: 13 nM								99%+
Citalopram HBr	+++ serotonin reuptake, IC50: 1.8 nM								99%+
Latrepirdine 2HCl	✔							GluR	99%+
Fluoxetine hydrochloride	✔								98%
Paroxetine hydrochloride	✔							AChR	99%+
BMY 7378		++ 5-HT1D, pIC50: 5.9 5-HT1A, pIC50: 6.4	+ 5-HT2, pIC50: 5.5						97%
Flibanserin		+++ 5-HT1A, Ki: 1 nM	+ 5-HT2A, Ki: 49 nM						98%
LY310762		+ 5-HT1D, Ki: 249 nM							99%+
Cyclobenzaprine HCI			✔						99%
Blonanserin			+++ 5-HT2, Ki: 3.98 nM						99%+
Cyproheptadine HCl			++++ 5-HT2, IC50: 0.6 nM						99+%
Olanzapine			✔						99+%
Pimavanserin hemitartrate			+++ 5-HT2A, pIC50: 8.7						99%
Ketanserin			+++ 5-HT2C (Human), Ki: 2.5 nM 5-HT2C (Rat), Ki: 50 nM						99%+
Loxapine succinate			++ 5-HT2 (bovine), Ki: 6.6 nM 5-HT2 (human), Ki: 6.8 nM						99%
Agomelatine			✔						99%+
Clozapine			✔						99%+
Amitriptyline			+ 5-HT2, Ki: 235 nM					SERT	98%
PRX-08066 maleate			+++ 5-HT2B, IC50: 3.4 nM						98+%
RS-127445			++++ 5-HT2B, pKi: 9.5 5-HT2B, pIC50: 10.4						99%+
Sarpogrelate HCl			++++ 5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM						98%
Tropisetron				✔					99%
Palonosetron				✔					98+%
Ramosetron HCl				++++ 5-HT3 receptor, Ki: 0.091 nM					99%+
Ondansetron				✔					99%
Granisetron				✔					98%
Alosetron HCl				✔					98%
Ondansetron hydrochloride dihydrate				✔					99%+
VUF10166				++++ 5-HT3AB, Ki: 22 nM 5-HT3A, Ki: 0.04 nM					99%+
Azasetron hydrochloride				++++ 5-HT3, IC50: 0.33 nM					98%
Asenapine maleate		+++ 5-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6	++++ 5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46		+++ 5-HT5A, pKi: 8.84	++++ 5-HT6, pKi: 9.6	++++ 5-HT7, pKi: 9.94		99%+
Risperidone		++ 5-HT1B, Ki: 14.9 nM 5-HT1D, Ki: 84.6 nM	++++ 5-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 nM		+ 5-HT5A, Ki: 206 nM		++ 5-HT7, Ki: 6.6 nM		99%+
SB 271046 HCl						+++ 5-HT6, pKi: 8.92			99%+
Intepirdine						++++ 5-HT6, pKi: 9.63			99%+
SB-269970 HCl							++ 5-HT7, pKi: 8.3		98+%
BRL 15572		++ 5-HT1B, pKi: 6.1 5-HT1D, pKi: 6	++ 5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2			+ 5-HT6, pKi: 5.9	+ 5-HT7, pKi: 6.3		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

SB 242084 2HCl 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].

SB 242084 2HCl 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.

SB 242084 2HCl 实验方案

计算器

存储液制备

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

SB 242084 2HCl 技术信息

CAS号	1049747-87-6
分子式	C₂₁H₂₁Cl₃N₄O₂
分子量	467.776

别名	SB-242084 (hydrochloride);SB 242084 dihydrochloride
运输	蓝冰

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

SB 242084 2HCl 99%+

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