奎纳克林抑制兔醛氧化酶，IC50 值分别为 3.3 μM 和 10 μM[2]。电压钠通道被奎纳克林抑制 (IC50: 3.3 μM)[3]。奎纳克林（0–20 μM，24 小时）刺激和抑制 SGC-7901 细胞的发育 [7]。奎纳克林 (100 μM) 也是 PLA2 布拉格通道。

甘油三酯可引起急性肾损伤，但奎纳克林（3-30 mg/kg，腹腔注射，每天一次，连续三天）可以预防这种损伤[5]。奎纳克林（腹腔注射，2.5～10 mg/kg，每日一次，连续三天）。

细胞活力测定 [7]
细胞类型： SGC-7901 细胞
测试浓度： 0、5、10、15、20 μM
孵育时间：24 h
实验结果：抑制细胞生长，IC50值为16.18 μM。

Animal/Disease Models: Acute kidney injury rat model [5]
Doses: 3-30 mg/kg
Route of Administration: intraperitoneal (ip) injection
Experimental Results: Attenuated glycerol-induced structural and renal toxicity. Changes in kidney function.

Absorption, Distribution and Excretion
Absorbed rapidly from the gastrointestinal tract following oral administration.
Rapidly absorbed from the gastrointestinal tract following oral administration. Also rapidly absorbed after intrapleural administration.
Widely distributed; concentrates in the liver, spleen, lungs, and adrenal glands. Concentration in the liver may be 20,000 times that in the plasma. Also deposited in skin, fingernails, and hair. Cerebrospinal fluid (CSF) concentration are 1 to 5% of corresponding plasma level. Lowest concentrations are found in the brain, heart, skeletal muscles, and breast milk.
Less than 11% eliminated in the urine daily; acidification of urine increases urinary excretion of quinacrine by up to 14%; excreted slowly, significant amounts being excreted in the urine for 2 months or more after discontinuation of quinacrine. Small amounts also excreted in bile, sweat, and saliva.
Quinacrine crosses the placenta and concentrations of drugs in fetal tissue are similar to maternal concentrations.
A small amount of quinacrine is excreted in breast milk.

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Metabolism / Metabolites
Small amt of unchanged drug is eliminated (l-form; apparently d-form is metabolized completely) by man and other animals. Several metabolites have been found in small amt, but there is some disagreement as to their structure.
Mepacrine yields 6-chloro-9-(4-ethylamino-1-methylbutyl amino)-2-methoxyacridine in rabbits

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Biological Half-Life
5 to 14 days

Hepatotoxicity
Mepacrine has been reported to cause elevations in serum enzymes, but the frequency of such changes is unknown, arising after 1 to 6 weeks with a mixed pattern of enzyme elevations and resolving within 1 to 2 months of stopping. Most patients are asymptomatic and liver enzyme elevations can resolve with, and sometimes without dose modification. Clinically apparent liver injury from mepacrine has also been reported, but the clinical features of the injury have not been well defined. Because mepacrine causes a yellowing of the skin, jaundice is not a reliable finding and most reports of liver injury from mepacrine have not included bilirubin elevations. Nevertheless, several instances of acute liver failure and death have been attributed to mepacrine therapy, although the reports usually predated the availability of tests for hepatitis A, B and C and often lacked histological documentation. Mepacrine has also been implicated in cases of aplastic anemia and in hypersensitivity reactions with exfoliative dermatitis, suggestive of Stevens Johnson syndrome, conditions that can be associated with liver injury that may be severe.
Likelihood score: E* (unproven but suspected cause of clinically apparent liver injury).

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Protein Binding
80-90%

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Interactions
Convulsive seizures have occurred in patients receiving quinacrine and corticosteroids concomitantly. /Quinacrine hydrochloride/
Concurrent use /of primaquine/ with quinacrine may inhibit the metabolism of primaquine or may displace if from tissue-binding sites, thereby increasing serum concentrations and potential toxicity of primaquine.
Aldehyde dehydrogenase may be inhibited by quinacrine, resulting in acummulation of acetaldehyde after alcohol ingestion and possibly "disulfram-like" reaction...

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Non-Human Toxicity Values
LD50 Mouse 1300 mg/kg

[1]. Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein. J Med Chem. 2003 Aug 14;46(17):3563-4.

[2]. Aldehyde oxidase: an enzyme of emerging importance in drug discovery. J Med Chem. 2010 Dec 23;53(24):8441-60.

[3]. [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. J Med Chem. 1985 Mar;28(3):381-8.

[4]. Role of phospholipase A2 activation and calcium in CYP2E1-dependent toxicity in HepG2 cells. J Biol Chem. 2003 Sep 5;278(36):33866-77.

[5]. Protective effect of quinacrine against glycerol-induced acute kidney injury in rats. BMC Nephrol. 2017 Jan 28;18(1):41.

[6]. Quinacrine attenuates cyclosporine-induced nephrotoxicity in rats. Transplantation. 1996 Aug 27;62(4):427-35.

[7]. Quinacrine Inhibits Cell Growth and Induces Apoptosis in Human Gastric Cancer Cell Line SGC-7901. Curr Ther Res Clin Exp. 2012 Feb;73(1-2):52-64.

Therapeutic Uses
Mesh Heading: Anticestodal agents, antimalarials, antinematodal agents, antineoplastic agents, enzyme inhibitors
THERAP CAT: Anthelmintic (Cestodes); antimalarial.
THERAP CAT (VET): Antiprotozoal, teniacide.
MEDICATION (VET): Protozoacide, anthelmintic. /Used/...with varying results against flukes & poor results in coccidiosis of cattle; good results against moniezia expansa & m benedini in sheep, & trichomoniasis in chickens, ducks, & geese; effective against "ich" parasite in fish tank...in exptl histoplasmosis... /Quinacrine hydrochloride/
For more Therapeutic Uses (Complete) data for QUINACRINE (11 total), please visit the HSDB record page.

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Drug Warnings
Quinacrine should not be given to pregnant women because drug readily passes placenta and reaches fetus.
Quinacrine crosses the placenta and reaches the fetal circulation. There is one case of possible renal agenesis and hydrocephalus in an infant, although normal pregnancies have been reported after quinacrine ingestion during the first 4 weeks of gestation. If possible, quinacrine treatment for giardiasis in asymptomatic pregnant women should be postponed until after delivery.
Quinacrine may cause vomiting in children due to its bitter taste. The tablets may be crushed and mixed with jam, honey, or chocolate syrup or put in empty gelatin capsules to mask the taste. Children also tolerate quinacrine less well than do adults.
Adverse effects of quinacrine in dosages used for the treatment of malaria include mild transient headache, dizziness, and GI disorders such as diarrhea, anorexia, nausea, abdominal cramps, and rarely, vomiting. Transient psychoses lasting 2 to 4 weeks have been reported in some patients receiving quinacrine.
For more Drug Warnings (Complete) data for QUINACRINE (18 total), please visit the HSDB record page.

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Pharmacodynamics
Quinacrine has been used as an antimalarial drug and as an antibiotic. It is used to treat giardiasis, a protozoal infection of the intestinal tract, and certain types of lupus erythematosus, an inflammatory disease that affects the joints, tendons, and other connective tissues and organs. Quinacrine may be injected into the space surrounding the lungs to prevent reoccurrence of pneumothorax. The exact way in which quinacrine works is unknown. It appears to interfere with the parasite's metabolism.

C23H30CLN30

399.21

399.208

83-89-6

Quinacrine dihydrochloride;69-05-6;l-Atabrine dihydrochloride;56100-42-6;d-Atabrine dihydrochloride;56100-41-5;Quinacrine hydrochloride hydrate;6151-30-0

237

Bright yellow crystals

1.156 g/cm3

557.1ºC at 760 mmHg

247-250ºC

290.7ºC

6.045

37.39

1

4

9

28

461

0

CCN(CC)CCCC(C)N=C1C2=C(C=C(C=C2)Cl)NC3=C1C=C(C=C3)OC

GPKJTRJOBQGKQK-UHFFFAOYSA-N

InChI=1S/C23H30ClN3O/c1-5-27(6-2)13-7-8-16(3)25-23-19-11-9-17(24)14-22(19)26-21-12-10-18(28-4)15-20(21)23/h9-12,14-16H,5-8,13H2,1-4H3,(H,25,26)

4-N-(6-chloro-2-methoxyacridin-9-yl)-1-N,1-N-diethylpentane-1,4-diamine

Haffkinine; Erion

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。