Chlorpheniramine maleate (NCI-C55265) is a histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma.

H1 receptor:12 nM

在卵清蛋白活性皮肤过敏刺激的BALB/c小鼠和皮下注射组胺的ICR小鼠中,口服 Chlorpheniramine（10 mg/kg）能够抑制短期刮伤.在组胺诱导豚鼠中（ED50=0.17 mg/kg）,口服Chlorpheniramine能够抑制死亡.在大鼠中,Chlorpheniramine（20 mg/kg ）处理后,能够阻断产生快速眼动睡眠的组胺或胆碱机制.

Chlorpheniramine能够抑制[3H]美吡拉敏与豚鼠皮层组胺H1受体结合（IC50=8.8 nM）。在MCF-7,MDA-MB 231和Ehrlich细胞中,Chlorpheniramine（250 μM）降低鸟氨酸脱羧酶mRNA翻译,抑制的增殖细胞增殖。在恶性疟原虫的CQS菌株（D6）（IC50=61.2uM）和MDR菌株（Dd2）（IC50=3.9uM）中,Chlorpheniramine具有抗疟活性。在伴刀豆球蛋白A诱导的鼠脾淋巴细胞中（IC50=33.4 μM）,Chlorpheniramine具有细胞毒性。

H1-Antihistaminic Activity: The segments (1 cm) of isolated ileum from guinea pigs are suspended in an organ bath containing Tyrode solution (ventilation, 32 °C). The contractile responses to histamine (0.54 μM) are measured with an isotonic transducer. A set concentration of Chlorpheniramine is added in the organ bath 5 minutes before the addition of histamine. IC50 value of Chlorpheniramine is calculated by the probit methond.

Cells are exposed to various concentrations of Chlorpheniramine for 48 hours. Cells are washed, detached, and counted with a Coulter counter for the determination of cell growth.(Only for Reference)