生物活性 | |||
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靶点 |
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描述 | Cimetidine is a histamine H2 receptor blocker with Ki and IC50 values of about 0.75 and 0.85 uM, respectively. It inhibits acid release from stomach and is used for gasterointestinal diseases and could inhibit converting hydrogen peroxide (H2O2) in a non-competitive manner. Cimetidine could non-competitively inhibit the liver catalase with high affinity. Binding of cimetidine to the enzyme induced conformational alteration in the enzyme[3]. Cimetidine, an H2-receptor antagonist, has been shown to enhance a variety of immunologic functions both in vivo and in vitro because of its inhibitory effects on suppressor-cell function. Patients receiving cimetidine have been shown to exhibit enhanced cell-mediated immunity as evaluated by increased response to skin-test antigens, restoration of sensitivity following development of acquired tolerance, and increased responses of lymphocytes to mitogen stimulation[4]. The clearance (Cl) of CsA (Cyclosporine) was significantly reduced following treatment with cimetidine when compared to the Cl value obtained in the control group (15.46 versus 10.36 ml/min/kg). Cimetidine is an inhibitor of the mixed function oxidase system enzyme system, it inhibits the metabolism of CsA[5]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.96mL 0.79mL 0.40mL |
19.81mL 3.96mL 1.98mL |
39.63mL 7.93mL 3.96mL |
参考文献 |
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[4]Kumar A. Cimetidine: an immunomodulator. DICP. 1990 Mar;24(3):289-95 |