SB-616234-A

目录号: HY-19477: Data Sheet SDS 产品使用指南
FAQs
技术支持

SB-616234-A 是一种选择性的，可口服的 5-HT1B receptor 拮抗剂，具有抗焦虑和抗抑郁的功效。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

SB-616234-A Chemical Structure

CAS No. : 908601-49-0

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
1 mg	￥1288	询问价格 & 货期
5 mg	￥3213	询问价格 & 货期
10 mg	￥4588	询问价格 & 货期
25 mg	询价	询问价格 & 货期
50 mg	询价	询问价格 & 货期
100 mg	询价	询问价格 & 货期

or 大包装询价

* Please select Quantity before adding items.

Customer Review

SB-616234-A 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 5-HT Receptor 亚型特异性产品:

查看所有亚型

5-HT Receptor 5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

SB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.

IC₅₀ & Target

5-HT_1B Receptor

体外研究
(In Vitro)

SB-616234-A 对在中国仓鼠卵巢 (CHO) 细胞中稳定表达的人 5-HT1B 受体具有高亲和力 (pK_i 为 8.3 ± 0.2)，并且对除 h5-HT1D 受体 (pK_i 6.6 ± 0.1) 外的一系列分子靶点具有超过 100 倍的选择性。同样，对大鼠和豚鼠纹状体 5-HT1B 受体的亲和力 (pK_i) 为 9.2 ± 0.1。在人重组细胞系的 [³⁵S]-GTPγS 结合研究中，SB-616234-A 是一种高亲和力拮抗剂，pA₂ 值为 8.6 ± 0.2，但未提供在此系统中具有激动剂活性的证据。在大鼠纹状体膜的 [³⁵S]-GTPγS 结合研究中，SB-616234-A 作为高亲和力拮抗剂，表观 pK_B 为 8.4 ± 0.5，但同样未提供此系统中激动剂活性的证据。SB-616234-A (1 μM) 可增强豚鼠和大鼠皮质切片中电刺激的 [³H]-5-HT 释放 (S2/S1 比分别为 1.8 和 1.6)^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SB-616234-A 以剂量相关的方式逆转 5-HT1/7 受体激动剂 SKF-99101H 诱导的豚鼠体温过低，口服 ED₅₀ 为 2.4 mg/kg。SB-616234- A 在由母鼠分离引起的发声模型中均产生剂量相关的抗焦虑作用，腹腔注射 ED₅₀ 分别为 1.0 和 3.3 mg/kg^[1]。SB-616234-A (0.3-30 mg/kg, po) 剂量依赖性抑制离体 [³H]-GR125743 与大鼠纹状体 5-HT1B 受体的结合，口服 ED₅₀ 为 2.83 ± 0.39 mg/kg^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

574.11

Formula

C₃₂H₃₆ClN₅O₃

CAS 号

908601-49-0

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

纯度 & 产品资料

Data Sheet (557 KB) SDS (252 KB) 产品使用指南 (1538 KB)

参考文献

[1]. Lee A.Dawson, et al. Characterisation of the selective 5-HT1B receptor antagonist SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2′-methyl-4′-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): In vivo neurochemical and behavioural evidence of anxiolytic/antidepressant activity. Neuropharmacology Volume 50, Issue 8, June 2006, Pages 975-983

[2]. Scott C, et al. SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2'methyl-4'-(5-methyl-1,2,3-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): a novel, potent and selective 5-HT1B receptor antagonist. Neuropharmacology. 2006 Jun;50(8):984-90. Epub 2006 Mar 20. [Content Brief]

Animal Administration ^[1]	Seven days post surgery animals are placed in microdialysis cages for overnight habituation prior to microdialysis experimentation. The following morning microdialysis probes (2 mm cuprophane membrane) are implanted, via the guide cannulae, into the frontal cortex and/or dentate gyrus. Probes are perfused with artificial cerebrospinal fluid (aCSF) containing NaCl 145 mM, KCl 2.7 mM, MgCl₂ 1.0 mM, CaCl₂ 1.2 mM, Na₂HPO₄ 2.0 mM (pH 7.4) at a flow rate of 1 μL/min. A 30 min sampling regime is used throughout the microdialysis procedure. Following a 2 h equilibration period, 3 microdialysis samples are collected to establish basal extracellular levels of 5-HT. Guinea pigs are then dosed with vehicle (1% methyl cellulose, 1 mg/kg p.o.), paroxetine (3 mg/kg p.o.) or SB-616234-A (3, 10 or 30 mg/kg p.o.). Microdialysis samples are collected for a further 5 h following drug administration. 5-HT content of microdialysate samples is measured using high performance liquid chromatography (HPLC) with electrochemical detection (ECD). At the end of the experiment probes are removed and animals return to their home cage. Animals are re-used in a randomised cross-over design with 7 days between uses and a maximum of 4 uses per subject. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Lee A.Dawson, et al. Characterisation of the selective 5-HT1B receptor antagonist SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2′-methyl-4′-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): In vivo neurochemical and behavioural evidence of anxiolytic/antidepressant activity. Neuropharmacology Volume 50, Issue 8, June 2006, Pages 975-983 [2]. Scott C, et al. SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2'methyl-4'-(5-methyl-1,2,3-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): a novel, potent and selective 5-HT1B receptor antagonist. Neuropharmacology. 2006 Jun;50(8):984-90. Epub 2006 Mar 20. [Content Brief]

Animal Administration
^[1]

Seven days post surgery animals are placed in microdialysis cages for overnight habituation prior to microdialysis experimentation. The following morning microdialysis probes (2 mm cuprophane membrane) are implanted, via the guide cannulae, into the frontal cortex and/or dentate gyrus. Probes are perfused with artificial cerebrospinal fluid (aCSF) containing NaCl 145 mM, KCl 2.7 mM, MgCl₂ 1.0 mM, CaCl₂ 1.2 mM, Na₂HPO₄ 2.0 mM (pH 7.4) at a flow rate of 1 μL/min. A 30 min sampling regime is used throughout the microdialysis procedure. Following a 2 h equilibration period, 3 microdialysis samples are collected to establish basal extracellular levels of 5-HT. Guinea pigs are then dosed with vehicle (1% methyl cellulose, 1 mg/kg p.o.), paroxetine (3 mg/kg p.o.) or SB-616234-A (3, 10 or 30 mg/kg p.o.). Microdialysis samples are collected for a further 5 h following drug administration. 5-HT content of microdialysate samples is measured using high performance liquid chromatography (HPLC) with electrochemical detection (ECD). At the end of the experiment probes are removed and animals return to their home cage. Animals are re-used in a randomised cross-over design with 7 days between uses and a maximum of 4 uses per subject.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Lee A.Dawson, et al. Characterisation of the selective 5-HT1B receptor antagonist SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2′-methyl-4′-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): In vivo neurochemical and behavioural evidence of anxiolytic/antidepressant activity. Neuropharmacology Volume 50, Issue 8, June 2006, Pages 975-983

[2]. Scott C, et al. SB-616234-A (1-[6-(cis-3,5-dimethylpiperazin-1-yl)-2,3-dihydro-5-methoxyindol-1-yl]-1-[2'methyl-4'-(5-methyl-1,2,3-oxadiazol-3-yl)biphenyl-4-yl]methanone hydrochloride): a novel, potent and selective 5-HT1B receptor antagonist. Neuropharmacology. 2006 Jun;50(8):984-90. Epub 2006 Mar 20. [Content Brief]

SB-616234-A 相关分类

Neurological Disease

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量		浓度		体积		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)	×	体积 _(start)	=	浓度 _(final)	×	体积 _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB-616234-A908601-49-05-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

您最近查看的产品:

产品名称：

* 需求量：

* 客户姓名：

* Email：

* 电话：

* 公司或机构名称：

留言给我们：

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。	站点地图隐私声明
沪ICP备15051369号-4 上海工商沪公网安备31011502019417 沪(浦)应急管危经许[2021]201709(QFYS) 营业执照（三证合一）
Copyright © 2013-2025 MedChemExpress. All Rights Reserved.

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

SB-616234-A

Customer Review

SB-616234-A 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 5-HT Receptor 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

SB-616234-A 相关分类

摩尔计算器

稀释计算器

The molarity calculator equation

The dilution calculator equation

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

SB-616234-A

Customer Review

SB-616234-A 相关抗体

SB-616234-A 相关产品

•同靶点产品:

•同靶点蛋白产品:

查看 5-HT Receptor 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

SB-616234-A 相关抗体:

SB-616234-A 相关分类

摩尔计算器

稀释计算器

The molarity calculator equation

The dilution calculator equation

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z