氯苯那敏可抑制疟原虫寄生虫（D6 和 Dd2 菌株的 IC50 值分别为 61.2 和 3.9 μM）[4]。氯苯那敏可降低 BV2 小胶质细胞中的质子电流 (IC50: 43 μM)[1]。

氯苯那敏（50、100、200μg/kg；肌肉注射；3次，间隔1周）可增强外周血中的白细胞[2]。在 BALB/c 小鼠中，口服氯苯那敏 (10 mg/kg) 可抑制卵清蛋白诱导的抓挠活动 [3]。

细胞活力测定
细胞类型：小鼠小胶质细胞 BV2 细胞[1]。
测试浓度： 100 μM
孵育时间： 5 分钟
实验结果： 抑制质子电流，具有中等效力。

Animal/Disease Models: SD (Sprague-Dawley) rats[2].
Doses: 50, 100 and 200 μg/kg
Route of Administration: Chlorpheniramine (50, 100 and 200 μg/kg; IM; 3 times, at intervals of 1 week)
Experimental Results: Enhanced white blood cells in the peripheral blood, mostly due to the increases of B cells and monocytes, but not T cells and NK cells.

Absorption, Distribution and Excretion
Absorbed well in the gastrointestinal tract.
Human and experimental animal studies have shown that (3) H-H-maleic acid chlorpheniramine can be rapidly and massively absorbed from the intestine. Despite prolonged total plasma radioactivity levels, the plasma half-life of chlorpheniramine is only 12-15 hours in humans and only 3 hours in dogs. The human half-life is approximately 3 times the duration of therapeutic effect…
H1 receptor antagonists are well absorbed in the gastrointestinal tract. After oral administration, peak plasma concentrations are reached within 2 to 3 hours, and the effect typically lasts 4 to 6 hours; however, some drugs have a longer duration of action… /Histamine antagonists: H1 receptor antagonists/
H1 receptor blockers are among many drugs that can induce hepatic microsomal enzymes, which may promote their own metabolism. /Histamine antagonists: H1 receptor antagonists/
Metabolism/Metabolites

Primarily metabolized in the liver by cytochrome P450 (CYP450) enzymes. The primary site of metabolic transformation is the liver. Antihistamines are mainly metabolized by hepatic cytochrome P450 (CYP450) enzymes. Half-life: 21-27 hours. In the human body… the plasma half-life of chlorpheniramine is… 12-15 hours… although the total radioactivity level in the plasma may be prolonged… Elimination: 14 to 25 hours.

Toxicity Summary
Chlorpheniramine binds to histamine H1 receptors. This blocks the action of endogenous histamine, thus temporarily relieving histamine-induced adverse symptoms. Toxicity Data
Oral LD50 (Rat): 306 mg/kg Oral LD50 (Mouse): 130 mg/kg Oral LD50 (Guinea Pig): 198 mg/kg LD50: 306 mg/kg (Human) (A308) Interactions Concomitant use of ototoxic drugs and antihistamines may mask ototoxic symptoms such as tinnitus, dizziness, or vertigo. /Antihistamines/ Monoamine oxidase (MAO) inhibitors may prolong and enhance the anticholinergic and central nervous system depressant effects of antihistamines; concomitant use is not recommended. /Antihistamines/
Concomitant use with alcohol or other central nervous system depressants may enhance the central nervous system depressant effects of these drugs or antihistamines; in addition, concomitant use with maprotiline or tricyclic antidepressants may enhance the anticholinergic effects of antihistamines or these drugs. /Antihistamines/
The anticholinergic effect may be enhanced when anticholinergic drugs or other drugs with anticholinergic activity are used in combination with antihistamines; patients should be advised to report gastrointestinal problems promptly, as concomitant use may lead to paralytic ileus. Antihistamines
Concomitant use of other photosensitizing drugs and antihistamines may produce additive photosensitizing effects.

[1]. Jiwon Kim, etal. Inhibitory effects of antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells. Eur J Pharmacol. 2017 Mar 5;798:122-128.

[2]. Kyung-Jin Jung, etal. Enhancement of B cell and monocyte populations in rats exposed to chlorpheniramine. Arch Pharm Res. 2012 Dec;35(12):2183-9.

[3]. Takano, N., I. Arai, and M. Kurachi, Analysis of the spontaneous scratching behavior by NC/Nga mice: a possible approach to evaluate antipruritics for subjects with atopic dermatitis. Eur J Pharmacol, 2003. 471(3): p. 223-8.

[4]. Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. Antimicrob Agents Chemother, 2007. 51(11): p. 4133-40.

Therapeutic Uses

Antihistamine; Antipruritic; Histamine H1 Receptor Antagonist
Antihistamines are indicated for the prevention and treatment of perennial and seasonal allergic rhinitis, vasomotor rhinitis, and allergic conjunctivitis caused by inhaled allergens and foods. /Antihistamines; included on the US product label/
Antihistamines are indicated for the treatment of itching associated with allergic reactions, as well as mild, uncomplicated allergic skin manifestations such as urticaria and angioedema, dermatographia, and transfusion-associated urticaria. /Antihistamines; included on the US product label/
Antihistamines are also used to treat itching associated with pityriasis rosea. /Antihistamines; not included on the US product label/
For more complete data on the therapeutic uses of chlorpheniramine (10 in total), please visit the HSDB record page.

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Drug Warning
This medication is not recommended for newborns or premature infants, as this age group is more sensitive to anticholinergic side effects (such as central nervous system excitation) and more prone to seizures. Children taking antihistamines may experience paradoxical reactions characterized by hyperexcitability. /Anthistamines/
Elderly patients are more likely to experience dizziness, sedation, confusion, and hypotension after taking antihistamines. Elderly patients are particularly susceptible to the anticholinergic side effects of antihistamines, such as dry mouth and urinary retention (especially in men). If these side effects occur and persist or are severe, discontinuation of the medication should be considered. /Anthistamines/
Prolonged use of antihistamines…may reduce or inhibit saliva production, leading to tooth decay, periodontal disease, oral candidiasis, and discomfort. /Antihistamines/
Antihistamines may help reduce serum reactions, but they have no therapeutic value…and may even enhance the toxicity of venom…/Antihistamines/
For more complete data on drug warnings for chlorpheniramine (14 in total), please visit the HSDB records page.

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Pharmacodynamics
In an allergic reaction, the allergen interacts with and cross-links with IgE antibodies on the surface of mast cells and basophils. Once the mast cell-antibody-antigen complex is formed, a series of complex reactions occur, ultimately leading to cell degranulation and the release of histamine (and other chemical mediators) from mast cells or basophils. After histamine release, it can react with local or systemic tissues via histamine receptors. Histamine acts on H1 receptors, causing itching, vasodilation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability, intensifying pain. Chlorpheniramine is an alkylamine histamine H1 receptor antagonist (more precisely, a histamine inverse agonist). It competes with histamine for normal H1 receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. It can effectively and temporarily relieve symptoms such as sneezing, watery and itchy eyes, and runny nose caused by hay fever and other upper respiratory allergies.

C17H20CLN

274.124

132-22-9

Chlorpheniramine maleate;113-92-8;Chlorpheniramine-d6 maleate;1219806-45-7

2725

OILY LIQUID

25 °C (lit.)

3.818

16.13

0

2

5

19

249

0

CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2

SOYKEARSMXGVTM-UHFFFAOYSA-N

InChI=1S/C16H19ClN2/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13/h3-9,11,15H,10,12H2,1-2H3

3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine

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。