Inhibition of morphine antinociception by centrally administered histamine H2 receptor antagonists.

Inhibition of morphine antinociception by centrally administered histamine H2 receptor antagonists.
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集中施用组胺 H2 受体拮抗剂抑制吗啡镇痛作用。

DOI:
10.1016/0014-2999(92)90610-g
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发表时间:
1992
影响因子:
5
通讯作者:
Nalwalk,JW
Nalwalk,JW
中科院分区:
医学2区
文献类型:
--
作者:
Hough,LB;Nalwalk,JW

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zolantidine dimaleate和其他5种组胺H2受体拮抗剂,给予大鼠侧脑室,在存在和不存在的全身给药吗啡的伤害性反应的行动进行了评估。在甩尾反应中,zolantidine诱导了时间和剂量依赖性的吗啡镇痛抑制,在没有吗啡的情况下对反应没有影响。唑兰替丁和另一种H_2受体拮抗剂噻替丁也能抑制吗啡热板反应。其他四种不同结构、脑穿透能力和H2效能的H2受体拮抗剂也诱导了吗啡甩尾反应的剂量相关抑制。这些化合物作为吗啡镇痛作用抑制剂的效力与H_2受体拮抗剂的效力高度相关(r= 0.98,P <0.005,n = 5)。考虑到以前的研究表明,这些化合物的选择性组胺H2受体,和抗伤害性的组胺,这些结果强烈建议的作用,脑组胺H2受体的表达吗啡抗伤害性。
The actions of zolantidine dimaleate and five other histamine H2receptor antagonists, given into the lateral ventricle of rats, were assessed on nociceptive responses in the presence and absence of systemically administered morphine. On the tail flick response, zolantidine induced a time- and dose-dependent inhibition of morphine antinociception, with no effect on responses in the absence of morphine. Zolantidine and another H2receptor antagonis, tiotidine, also inhibited morphine responses in the hot plate test. Four other H2receptor antagonists of varying structure, brain-penetrating ability, and H2potency also induced dose-related inhibition of morphine tail flick responses. Over three orders of magnitude, the potency of these compounds as inhibitors of morphine antinociception was highly correlated with H2receptor antagonist potency (r=0.98, P < 0.005, n = 5). Taken with previous studies showing the selectivity of these compounds for histamine H2receptors, and the antinociceptive properties of histamine, these results strongly suggest a role for brain histamine H2receptors in the expression of morphine antinociception.
DOI: --
发表时间: 1974
期刊: Brain Research
影响因子: 2.9
作者:
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发表时间: 1983
期刊:
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作者:
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