8-OH-DPAT (Synonyms: 8-Hydroxy-DPAT)

目录号: HY-112061 纯度: 99.26%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

8-OH-DPAT 是一种有效的，选择性的 5-HT 激动剂，对 5-HT1A 的 pIC₅₀ 值为 8.19，对 5-HT7 的 K_i 值为 466 nM，对 5-HT1B (pIC₅₀, 5.42) 和 5-HT (pIC₅₀ <5) 的作用很弱。

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8-OH-DPAT Chemical Structure

CAS No. : 78950-78-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥517	In-stock
1 mg	￥190	In-stock
5 mg	￥500	In-stock
10 mg	￥800	In-stock
25 mg	￥1600	In-stock
50 mg	￥2500	In-stock
100 mg	￥3800	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of 8-OH-DPAT:

8-OH-DPAT hydrobromide In-stock
R(+)-8-OH-DPAT hydrobromide 询价

MCE 顾客使用本产品发表的 2 篇科研文献

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

8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC₅₀ of 8.19 for 5-HT1A and a K_i of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC₅₀, 5.42), 5-HT (pIC₅₀ <5).

IC₅₀ & Target

5-HT_1A Receptor

8.19 (pIC₅₀)

5-HT₇ Receptor

466 nM (Ki)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	EC₅₀	260 nM Compound: 5	The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line	[PMID: 9871775]
CHO	IC₅₀	5.2 nM Compound: 8-OH-DPAT	Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand Binding affinity to rat Dopamine receptor D2 expressed in CHO cells was determined using [125 I ] iodosulpride as radioligand	[PMID: 8759642]
HEK293	IC₅₀	5.3 x 10^-10 M Compound: 8-OH-DPAT	Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method	[PMID: 27876250]
HEK293	EC₅₀	6 nM Compound: 8-OH-DPAT	Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay Agonist activity at human 5 HT1A receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by TR-FRET assay	[PMID: 31547945]
HeLa	EC₅₀	8 nM Compound: 8-OH-DPAT	Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA Agonist activity at human 5-HT1A receptor expressed in human HeLa cells assessed as inhibition of forskolin-stimulated cAMP formation after 10 mins by RIA	[PMID: 24050112]

体外研究
(In Vitro)

8-OH-DPAT 是一种有效的选择性 5-HT 激动剂，对 5-HT1A 的 pIC₅₀ 为 8.19；与 5-HT1B (pIC₅₀，5.42)、5-HT (pIC₅₀ <5)弱结合^[1]。
8-OH-DPAT 对 5-HT7 具有高亲和力，K_i 为 466 nM，并且不与 5-HT6 或 5-HT4结合^[2]。

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

体内研究
(In Vivo)

8-OH-DPAT (1 mg/kg) 使运动减退正常化，显著增加觉醒并减少 REM 睡眠的持续时间，而不影响食欲素敲除 (KO) 小鼠在黑暗时期的非 REM 睡眠持续时间。8-OH-DPAT 对 WT 小鼠的觉醒或 REM 睡眠或非 REM 睡眠的持续时间没有明显影响。8-OH-DPAT (1 mg/kg，皮下注射) 激活食欲素敲除小鼠的 5-HT1A 受体^[3]。

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

分子量

247.38

Formula

C₁₆H₂₅NO

CAS 号

78950-78-4

性状

固体

颜色

White to gray

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (404.24 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.0424 mL	20.2118 mL	40.4236 mL
5 mM	0.8085 mL	4.0424 mL	8.0847 mL
10 mM	0.4042 mL	2.0212 mL	4.0424 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

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)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (10.11 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.11 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (10.11 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.26%

选择批次：

Data Sheet (639 KB) SDS (251 KB)

COA (194 KB) HNMR (140 KB) RP-HPLC (141 KB)

产品使用指南 (1538 KB)

参考文献

[1]. DEREK N. MIDDLEMISS, et al. 8-HYDROXY-2-(DI-n-PROPYLAMINO)-TETRALIN DISCRIMINATES BETWEEN SUBTYPES OF

[2]. Bard JA, et al. Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. J Biol Chem. 1993 Nov 5;268(31):23422-6. [Content Brief]

[3]. Mori T, et al. Narcolepsy-like sleep disturbance in orexin knockout mice are normalized by the 5-HT1A receptor agonist 8-OH-DPAT. Psychopharmacology (Berl). 2016 Jun;233(12):2343-53. [Content Brief]

Animal Administration ^[3]	Mice^[3] The locomotor activity of mice is measured by an infrared sensor placed in individual home cages. To compare the locomotor activity in the light and dark periods, locomotor activity is monitored at 30-min intervals starting at 8:00 a.m. and 8:00 p.m., respectively. To measure the effects of psychostimulants (8-OH-DPAT, 1, 3 mg/kg, s.c; etc.) on locomotor activity in the dark period, all drugs are administered at 8:00 p.m., and locomotor activity is then measured through 3 h^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. DEREK N. MIDDLEMISS, et al. 8-HYDROXY-2-(DI-n-PROPYLAMINO)-TETRALIN DISCRIMINATES BETWEEN SUBTYPES OF [2]. Bard JA, et al. Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. J Biol Chem. 1993 Nov 5;268(31):23422-6. [Content Brief] [3]. Mori T, et al. Narcolepsy-like sleep disturbance in orexin knockout mice are normalized by the 5-HT1A receptor agonist 8-OH-DPAT. Psychopharmacology (Berl). 2016 Jun;233(12):2343-53. [Content Brief]

Animal Administration
^[3]

Mice^[3]
The locomotor activity of mice is measured by an infrared sensor placed in individual home cages. To compare the locomotor activity in the light and dark periods, locomotor activity is monitored at 30-min intervals starting at 8:00 a.m. and 8:00 p.m., respectively. To measure the effects of psychostimulants (8-OH-DPAT, 1, 3 mg/kg, s.c; etc.) on locomotor activity in the dark period, all drugs are administered at 8:00 p.m., and locomotor activity is then measured through 3 h^[3].

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

参考文献

[1]. DEREK N. MIDDLEMISS, et al. 8-HYDROXY-2-(DI-n-PROPYLAMINO)-TETRALIN DISCRIMINATES BETWEEN SUBTYPES OF

[2]. Bard JA, et al. Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. J Biol Chem. 1993 Nov 5;268(31):23422-6. [Content Brief]

[3]. Mori T, et al. Narcolepsy-like sleep disturbance in orexin knockout mice are normalized by the 5-HT1A receptor agonist 8-OH-DPAT. Psychopharmacology (Berl). 2016 Jun;233(12):2343-53. [Content Brief]

8-OH-DPAT 相关分类

Neurological Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.0424 mL	20.2118 mL	40.4236 mL	101.0591 mL
	5 mM	0.8085 mL	4.0424 mL	8.0847 mL	20.2118 mL
	10 mM	0.4042 mL	2.0212 mL	4.0424 mL	10.1059 mL
	15 mM	0.2695 mL	1.3475 mL	2.6949 mL	6.7373 mL
	20 mM	0.2021 mL	1.0106 mL	2.0212 mL	5.0530 mL
	25 mM	0.1617 mL	0.8085 mL	1.6169 mL	4.0424 mL
	30 mM	0.1347 mL	0.6737 mL	1.3475 mL	3.3686 mL
	40 mM	0.1011 mL	0.5053 mL	1.0106 mL	2.5265 mL
	50 mM	0.0808 mL	0.4042 mL	0.8085 mL	2.0212 mL
	60 mM	0.0674 mL	0.3369 mL	0.6737 mL	1.6843 mL
	80 mM	0.0505 mL	0.2526 mL	0.5053 mL	1.2632 mL
	100 mM	0.0404 mL	0.2021 mL	0.4042 mL	1.0106 mL

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:

8-OH-DPAT78950-78-48-Hydroxy-DPAT5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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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）

8-OH-DPAT (Synonyms: 8-Hydroxy-DPAT)

Customer Review

Other Forms of 8-OH-DPAT:

MCE 顾客使用本产品发表的 2 篇科研文献