作为促有丝分裂原诱导淋巴细胞激活抑制剂的地马普明、去甲地马普明、甲胺和氯喹的比较。
A comparison of dimaprit, nordimaprit, methylamine and chloroquine as inhibitors of mitogen-induced lymphocyte activation.
作者信息
Dale M M, Ladd R
出版信息
Br J Pharmacol. 1984 Sep;83(1):293-8. doi: 10.1111/j.1476-5381.1984.tb10145.x.
Methylamine and chloroquine both 'lysosomotropic' agents (i.e. agents which sequester in lysosomes) caused a dose-related inhibition of mitogen-induced lymphocyte activation in the concentrations which have previously been shown to increase the pH of lysosomes. The dose-response curves of inhibition of mitogen-induced lymphocyte activation for chloroquine and methylamine are very steep and are similar to the dose-response curves obtained with dimaprit and nordimaprit, but very different from the flat dose-response curves previously described for histamine. Approximate IC50 values were methylamine 6.4 mM, dimaprit 0.13 mM, nordimaprit 0.03 mM and chloroquine 18 microM. It is suggested that the mechanism of action of methylamine and chloroquine may be related to their lysosomotropic action and consequent interference with ligand-receptor processing, and that dimaprit and nordimaprit but not histamine may act by a similar mechanism.
甲胺和氯喹都是“溶酶体亲和性”药物（即聚集于溶酶体的药物），在先前已证明可提高溶酶体pH值的浓度下，它们对有丝分裂原诱导的淋巴细胞活化产生剂量相关的抑制作用。氯喹和甲胺对有丝分裂原诱导的淋巴细胞活化的抑制作用剂量反应曲线非常陡峭，与用二甲双胍和去甲二甲双胍获得的剂量反应曲线相似，但与先前描述的组胺的平坦剂量反应曲线非常不同。近似的IC50值分别为：甲胺6.4 mM、二甲双胍0.13 mM、去甲二甲双胍0.03 mM和氯喹18 microM。有人提出，甲胺和氯喹的作用机制可能与其溶酶体亲和性作用以及随之而来的对配体-受体加工的干扰有关，并且二甲双胍和去甲二甲双胍而非组胺可能通过类似机制起作用。
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