Bugajski J, Janusz Z
Life Sci. 1983 Sep 19;33(12):1179-89. doi: 10.1016/0024-3205(83)90023-1.
In conscious rats histamine, the H1-receptor agonist 2-pyridylethylamine (PEA), and the H2-receptor agonists dimaprit and impromidine given intracerebroventriculary (i.c.v.) increased the hypophyseal-adrenocortical response, evaluated indirectly through the corticosterone concentration in the blood serum. On a molar basis histamine was the most potent drug whereas its agonists were less potent in inducing an increased corticosterone response. Impromidine however, was far more active than dimaprit and PEA. The effect of histamine was significantly yet not totally antagonized by either mepyramine, a H1-receptor antagonist, or cimetidine, a H2-receptor blocker. The combination of mepyramine and cimetidine caused a considerably stronger inhibition than that induced by either antagonist given separately. Mepyramine impaired the corticosterone response to PEA, and the responses to impromidine and dimaprit were significantly diminished by cimetidine. The results suggest that i.c.v. histamine increases the pituitary-adrenocortical activity via both H1- and H2-receptors, and there seems to be no significant prevalence of either of these receptors in mediating this action of histamine.
在清醒大鼠中，组胺、H1受体激动剂2-吡啶乙胺（PEA）以及H2受体激动剂二甲双胍和英普咪定经脑室内（i.c.v.）给药后，通过血清中皮质酮浓度间接评估，可增强垂体-肾上腺皮质反应。按摩尔计算，组胺是最有效的药物，而其激动剂在诱导皮质酮反应增加方面效力较弱。然而，英普咪定比二甲双胍和PEA活性高得多。组胺的作用可被H1受体拮抗剂美吡拉敏或H2受体阻滞剂西咪替丁显著但未完全拮抗。美吡拉敏和西咪替丁联合使用引起的抑制作用比单独使用任何一种拮抗剂都要强得多。美吡拉敏削弱了对PEA的皮质酮反应，西咪替丁使对英普咪定和二甲双胍的反应显著减弱。结果表明，脑室内注射组胺通过H1和H2受体增加垂体-肾上腺皮质活性，并且在介导组胺的这一作用中，这两种受体似乎均无明显优势。
