Gordon D, Lewis G P, Nouri A M
Br J Pharmacol. 1981 Sep;74(1):137-41. doi: 10.1111/j.1476-5381.1981.tb09965.x.
1 The effects of histamine and chemical analogues were examined on mitogen-stimulated human lymphocyte proliferation. 2 Compounds with selective agonist activity at either H1- or H2-receptors were found to inhibit proliferative responses, although N-3-methyl-histamine which does not act on either receptor was as inhibitory as histamine itself. 3 The H2-receptor agonist, dimaprit, had a profound inhibitory effect on proliferation, however nordimaprit, which has little or no H2-agonist activitiy, was more active on lymphocytes. Impromidine, although a potent H2-agonist, failed to produce such inhibition. 4 The effects of dimaprit and nordimaprit were not reversed by H2-receptor antagonists, cimetidine or metiamide. 5 These results do not support the view that the antiproliferative effects of histamine and related compounds are mediated via conventional H1-or H2-receptors. 6 SKF 93390 was found to be the most active of the dimaprit analogues tested, which could represent a novel series of potential immunosuppressive agents.
研究了组胺及其化学类似物对丝裂原刺激的人淋巴细胞增殖的影响。
发现对H1或H2受体具有选择性激动剂活性的化合物可抑制增殖反应，尽管对这两种受体均无作用的N - 3 - 甲基组胺与组胺本身的抑制作用相同。
H2受体激动剂二甲双胍对增殖有显著抑制作用，然而几乎没有或没有H2激动剂活性的去甲二甲双胍对淋巴细胞的活性更强。英普咪定虽然是一种强效H2激动剂，但未能产生这种抑制作用。
H2受体拮抗剂西咪替丁或甲硫米特不能逆转二甲双胍和去甲二甲双胍的作用。
这些结果不支持组胺及相关化合物的抗增殖作用是通过传统的H1或H2受体介导的观点。
发现SKF 93390是所测试的二甲双胍类似物中活性最高的，它可能代表了一系列新型的潜在免疫抑制剂。
