在 N2A 细胞中，地芬尼多 (0.1-100 µM) 抑制 Na+ 电流，IC50 为 0.77 µM，希尔系数为 1.15 [1]。

在大鼠中，多非替多（0.77 mg/大鼠；鞘内注射；单剂量）抑制本体感觉、伤害感受和运动表现 [1]。地芬尼多（0.62、3.09 mg/kg；腹腔注射；每天一次，持续 7 天）可以成功逆转或完全阻断 CCI 引起的机械异常性疼痛的大鼠 [2]。

Animal/Disease Models: Male Spraguee Dawley rat (275-325 g) [1].
Doses: 0.77 mg/rat (2.50 µmol/rat)
Route of Administration: Intrathecal injection; single.
Experimental Results: Resulting in 100% obstruction of motor function, proprioception and nociception, with durations of approximately 51 minutes, 77 minutes and 123 minutes respectively.

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Animal/Disease Models: Male adult SD (SD (Sprague-Dawley)) rat (200-250 g; CCI rat model) [2].
Doses: 0.62, 3.09 mg/kg (2, 10 µmol/kg)
Route of Administration: intraperitoneal (ip) injection; single dose daily for 7 days.
Experimental Results: Blockade of CCI-induced low mechanical withdrawal threshold 1 hour after administration. Reduces TNF-α levels on day 7 and alleviates neuropathic tactile allodynia after CCI in rats.

Absorption, Distribution and Excretion
Well absorbed from gastrointestinal tract following oral administration.

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Metabolism / Metabolites
IN DOGS & IN MAN, PRINCIPAL URINARY METABOLITE OF DIPHENIDOL...WAS N-(4,4-DIPHENYL-4-HYDROXYBUTYL)-DELTA-AMINOVALERIC ACID...(NOT LESS THAN 50% OF DOSE)... MINOR URINARY METABOLITES INCL A PHENOL...& A LACTAM...

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Biological Half-Life
4 hours

Non-Human Toxicity Values
LD50 MICE ORAL 430 MG/KG /HCL/
LD50 MICE INTRAPERITONEAL 105 MG/KG /HCL/
LD50 MICE INTRAVENOUS 37 MG/KG /HCL/
LD50 RATS ORAL 515 MG/KG /HCL/
For more Non-Human Toxicity Values (Complete) data for DIPHENIDOL (6 total), please visit the HSDB record page.

[1]. Inhibition of voltage-gated K+ channels and Ca2+ channels by diphenidol. Pharmacol Rep. 2012;64(3):739-44.

[2]. Diphenidol inhibited sodium currents and produced spinal anesthesia. Neuropharmacology. 2010 Jun;58(7):1147-52.

[3]. Diphenidol inhibited sodium currents and produced spinal anesthesia. Neuropharmacology. 2010 Jun;58(7):1147-52.

[4]. Systemic diphenidol reduces neuropathic allodynia and TNF-alpha overexpression in rats after chronic constriction injury. Neurosci Lett. 2013 Sep 27;552:62-5.

[5]. Neuropharmacological mechanisms of emesis. I. Effects of antiemetic drugs on motion- and apomorphine-induced pica in rats. Methods Find Exp Clin Pharmacol. 1995 Nov;17(9):589-90.

Diphenidol is a tertiary alcohol that is butan-1-ol substituted by two phenyl groups at position 1 and a piperidin-1-yl group at position 4. It has a role as an antiemetic. It is a member of piperidines, a tertiary alcohol and a member of benzenes.
Diphenidol is an antiemetic agent used in the treatment of vomiting and vertigo. Diphenidol overdose may result in serious toxicity in children.
Diphenidol is an Antiemetic. The physiologic effect of diphenidol is by means of Emesis Suppression.

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Drug Indication
For use in the prevention and symptomatic treatment of peripheral (labyrinthine) vertigo and associated nausea and vomiting that occur in such conditions as Meniere's disease and surgery of the middle and inner ear. Also for the control of nausea and vomiting associated with postoperative states, malignant neoplasms, labyrinthine disturbances, antineoplastic agent therapy, radiation sickness, and infectious diseases.
FDA Label

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Mechanism of Action
The mechanism by which diphenidol exerts its antiemetic and antivertigo effects is not precisely known. It is thought to diminish vestibular stimulation and depress labyrinthine function and as an antimuscarinic agent. An action on the medullary chemoreceptive trigger zone may also be involved in the antiemetic effect. Diphenidol has no significant sedative, tranquilizing, or antihistaminic action. It has a weak peripheral anticholinergic effect.
EXPTL, IT HAS BEEN SHOWN TO EXHIBIT WEAK PARASYMPATHOLYTIC ACTIONS, BUT TO LACK SIGNIFICANT SEDATIVE, TRANQUILIZING, OR ANTIHISTAMINIC PROPERTIES.
.../DIPHENIDOL/ IS THOUGHT TO ACT UPON AURAL VESTIBULAR APPARATUS...

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Therapeutic Uses
Antiemetics; Histamine H1 Antagonists
...ANTIEMETIC AGENT FOR ORAL, RECTAL, IM, OR IV ADMIN, USEFUL IN MGMNT OF NAUSEA & VOMITING ASSOC WITH INFECTIOUS DISEASES, MALIGNANCIES, RADIATION SICKNESS, GENERAL ANESTHESIA, TREATMENT WITH ANTINEOPLASTIC AGENTS. ...ALSO USEFUL IN TREATMENT OF VERTIGO OF VESTIBULAR ORIGIN.
IN ADULTS, THIS DRUG ALSO IS EFFECTIVE IN...LABYRINTHITIS FOLLOWING SURGERY OF MIDDLE & INNER EAR, & MENIERE'S DISEASE. ITS USE IN TREATMENT OF VERTIGO IN CHILDREN HAS NOT BEEN INVESTIGATED. /HCL/

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Drug Warnings
SINCE DIPHENIDOL DOES POSSESS PARASYMPATHOLYTIC PROPERITES, IT SHOULD BE USED CAUTIOUSLY IN PT WITH GLAUCOMA, PROSTATIC HYPERTROPHY, PEPTIC ULCER, PYLORIC OR DUODENAL OBSTRUCTION, OR CARDIOSPASM.
...IT IS NOT RECOMMENDED FOR USE IN NAUSEA & VOMITING OF PREGNANCY, SINCE ITS SAFE USE IN THIS CONDITION HAS NOT BEEN ESTABLISHED.

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Pharmacodynamics
Diphenidol is used for control of nausea and vomiting. It has an antivertigo effect on the vestibular apparatus, inhibiting the chemoreceptor trigger zone to control nausea and vomiting, thus preventing motion sickness.

C21H27NO

309.4452

309.209

972-02-1

Diphenadol-d10

3055

NEEDLES FROM PETROLEUM ETHER
WHITE CRYSTALLINE POWDER

1.066 g/cm3

473.3ºC at 760 mmHg

105ºC

233.5ºC

1.5614 (estimate)

4.126

23.47

1

2

6

23

307

0

C1(C(C2C=CC=CC=2)(O)CCCN2CCCCC2)C=CC=CC=1

OGAKLTJNUQRZJU-UHFFFAOYSA-N

InChI=1S/C21H27NO/c23-21(19-11-4-1-5-12-19,20-13-6-2-7-14-20)15-10-18-22-16-8-3-9-17-22/h1-2,4-7,11-14,23H,3,8-10,15-18H2

1,1-diphenyl-4-piperidin-1-ylbutan-1-ol

SKF478 SKF-478 SKF 478

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。