Diphenhydramine (Synonyms: 苯海拉明)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物,专注于信号通路和疾病研究领域。
Diphenhydramine  (Synonyms: 苯海拉明) 纯度: 99.08%

Diphenhydramine 是第一代具有抗胆碱能作用的组胺 H1 受体 (histamine H1-receptor) 拮抗剂。Diphenhydramine hydrochloride 能透过血脑屏障。

Diphenhydramine                                          (Synonyms: 苯海拉明)

Diphenhydramine Chemical Structure

CAS No. : 58-73-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥495 In-stock
250 mg ¥450 In-stock
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1 g   询价  

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生物活性

Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) [1][2][3].

IC50 & Target

H1 Receptor

 

NMDA Receptor

24.6 μM (IC50)

体外研究
(In Vitro)

Diphenhydramine (1-300 μM, 30 s) 可阻断 NMDA 激活的膜电流,这一特性可负责或增加其镇静、镇痛和记忆相关的作用[2]

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Diphenhydramine 相关抗体:

Cell Viability Assay[2]

Cell Line: Human TsA cells
Concentration: 1-300 μM
Incubation Time: 10-30 s
Result: Did not discriminate between different GluN2 receptor subunits.
The IC50 value of Diphenhydramine against GluN1/GluN2B was 24.6 µM.
The IC50 values of Diphenhydramine against GluN1/GluN2A and GluN1_A652C/GluN2A were 24.4 µM and 89.6 µM, respectively, indicating that the receptor modification reduces sensitivity for diphenhydramine.
The inhibitory potency of Diphenhydramine did not be overcome with increasing NMDA concentrations.
The inhibitory potency of Diphenhydramine did not increase with increasing agonist concentration.

体内研究
(In Vivo)

Diphenhydramine (0-10 mg/kg, i.v. and p.o.) 与茶苯海明 Dimenhydrinate (HY-B1215) 联合使用时,口服生物利用度更好[3]
Diphenhydramine (20 mg/kg, i.p.) 可改善顺铂Cisplatin (CDDP) (HY-17394) 对小鼠引起的肾损伤,同时不会影响到顺铂的抗肿瘤效果[4]

药代动力学分析[3]

Route Dose (mg/kg) AUClast (ng·h/mL) C0 (ng/Ml) CL (Ml/h/kg) T1/2 (h) Kel (1/h) MRT (h) Vss_obs (mL/kg) Cmax (ng/mL) Tmax (h) Vz (mL/kg) F (%)
i.v. 5 391.20 266.10 2833.04 1.89 0.45 2.47 6582.36 / / / /
p.o. 5 153.80 / / 4.98 0.59 6.97 / 35.80 1.30 180157.36 7.75

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: healthy, fasted mixed-breed dogs[3]
Dosage: 1/5/10 mg/kg
Administration: i.v., p.o.
Result: Oral absorption of diphenhydramine was approximately three times greater with a longer half-life when it was administered as the combination product Dimenhydrinate (HY-B1215).

Clinical Trial

分子量

255.35

Formula

C17H21NO

CAS 号

58-73-1

性状

液体

颜色

Colorless to light yellow

中文名称

苯海拉明

结构分类
  • Alkaloids
  • Other Alkaloids
初始来源
  • 内源性代谢物
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (391.62 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 3.9162 mL 19.5810 mL 39.1619 mL
5 mM 0.7832 mL 3.9162 mL 7.8324 mL
10 mM 0.3916 mL 1.9581 mL 3.9162 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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量

=

浓度

×

体积

×

分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×

体积 (start)

V1

=

浓度 (final)

C2

×

体积 (final)

V2

In Vivo:

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.79 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。

    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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):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 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.79 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。

    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。

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动物溶解方案

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

g

每只动物的给药体积

μL

动物数量

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 Shanghai Jinpan Biotech Co Ltd 网站选购。 ,Tween 80,均可在 Shanghai Jinpan Biotech Co Ltd 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)。
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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

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

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: 99.08%

Data Sheet (625 KB) SDS (393 KB)

COA (170 KB) HNMR (227 KB) LCMS (84 KB)

产品使用指南 (1538 KB)

参考文献
  • [1]. Jason P Berninger, et al. Effects of the antihistamine diphenhydramine on selected aquatic organisms. Environ Toxicol Chem. 2011 Sep;30(9):2065-72.  [Content Brief]

    [2]. Föhr KJ, et al. Open channel block of NMDA receptors by diphenhydramine. Neuropharmacology. 2015 Dec;99:459-70.  [Content Brief]

    [3]. Ehling S, et al. Diphenhydramine pharmacokinetics after oral and intravenous administration of diphenhydramine and oral administration of dimenhydrinate to healthy dogs, and pharmacodynamic effect on histamine-induced wheal formation: a pilot study. Vet Dermatol. 2019 Apr;30(2):91-e24.  [Content Brief]

    [4]. Hamano H, et al. Diphenhydramine may be a preventive medicine against cisplatin-induced kidney toxicity. Kidney Int. 2021 Apr;99(4):885-899.  [Content Brief]

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