Foldes A, Hall R C
Br J Pharmacol. 1979 Nov;67(3):329-35. doi: 10.1111/j.1476-5381.1979.tb08684.x.
1 The effects of a subconstrictor dose of histamine (9 x 10(-7) mol/l) on the responses of the isolated perfused ear artery of the rabbit to electrical stimulation (E.S.) and to exogenous noradrenaline (NA) were investigated.2 Both intraluminal (I/L) and extraluminal (E/L) histamine potentiated responses to E.S. and to I/L NA to the same extent.3 Mepyramine alone (2.5 x 10(-6) mol/l) had no effect on the response of the ear artery to either stimulus, but in the presence of this concentration of mepyramine, the potentiation by histamine of the response to I/L NA was significantly decreased and that to E.S. was replaced by inhibition.4 The H(1)-receptor agonist, 2(2-pyridyl) ethylamine, applied I/L potentiated responses to I/L NA at both concentrations used (5.1 and 51 x 10(-7) mol/l), but only potentiated the effects of E.S. at the higher concentration.5 The H(2)-receptor antagonist, metiamide (4 x 10(-6) mol/l), alone did not alter the extent of potentiation of responses to either E.S. or I/L NA by histamine. This suggests relatively weak H(2)-receptor activity in the rabbit ear artery. In the presence, but not the absence of metiamide, the potentiation by histamine of the I/L NA response was reversible, an observation suggesting an interaction between metiamide and the non-reversible component of the potentiating effect of histamine.6 These results are interpreted in terms of postsynaptic H(1)-receptors which potentiate and presynaptic H(2)-receptors which inhibit contractile responses in the ear artery.
研究了亚收缩剂量的组胺(9×10⁻⁷摩尔/升)对兔离体灌注耳动脉对电刺激(E.S.)和外源性去甲肾上腺素(NA)反应的影响。
管腔内(I/L)和管腔外(E/L)组胺对E.S.和I/L NA反应的增强程度相同。
单独使用美吡拉敏(2.5×10⁻⁶摩尔/升)对耳动脉对任何一种刺激的反应均无影响,但在该浓度的美吡拉敏存在下,组胺对I/L NA反应的增强作用显著降低,对E.S.的增强作用则被抑制所取代。
I/L应用H₁受体激动剂2-(2-吡啶基)乙胺,在所用的两种浓度(5.1和51×10⁻⁷摩尔/升)下均增强了对I/L NA的反应,但仅在较高浓度下增强了E.S.的作用。
H₂受体拮抗剂甲硫米特(4×10⁻⁶摩尔/升)单独使用时,并不改变组胺对E.S.或I/L NA反应的增强程度。这表明兔耳动脉中H₂受体活性相对较弱。在有甲硫米特存在而非不存在时,组胺对I/L NA反应的增强作用是可逆的,这一观察结果提示甲硫米特与组胺增强作用的不可逆成分之间存在相互作用。
这些结果可解释为,耳动脉中存在增强收缩反应的突触后H₁受体和抑制收缩反应的突触前H₂受体。