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首页> 外文期刊>Neurochemistry International: The International Journal for the Rapid Publication of Critical Reviews, Preliminary and Original Research Communications in Neurochemistry >Pre- and postsynaptic mechanisms in the clonidine- and oxymetazoline-induced inhibition of gastric motility in the rat.
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Pre- and postsynaptic mechanisms in the clonidine- and oxymetazoline-induced inhibition of gastric motility in the rat.

机译：可乐定和羟甲唑啉诱导的大鼠胃动力抑制的突触前和突触后机制。

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The inhibitory effect of clonidine (non-selective alpha2-adrenoceptor agonist) and oxymetazoline (alpha2A-adrenoceptor selective agonist) was compared on basal and stimulated gastric motor activity (gastric tone and contractions) using the balloon method in the rat. It was shown that oxymetazoline (0.2-1.7 micromol/kg, i.v.) decreased the basal motility, while clonidine (1.9-3.8 micromol/kg, i.v.) failed to affect it. When motility was stimulated centrally by insulin (5 IU/rat, i.v.), both clonidine (1.9-3.8 micromol/kg, i.v.) and oxymetazoline (0.1-3.4 micromol/kg, i.v.) inhibited the gastric motor activity. However, while the effect of clonidine was antagonized by the non-selective alpha2-adrenoceptor antagonist yohimbine (5 micromol/kg, i.v.) and the alpha2A-adrenoceptor selective antagonist BRL 44408 (3 micromol/kg, i.v.), the effect of oxymetazoline was only partially affected. Prazosin (alpha1- and alpha2B-adrenoceptor antagonist, 0.07-0.28 micromol/kg, i.v.) also failed to reverse the effect of oxymetazoline. Furthermore, when gastric motility was stimulated peripherally by activation of postsynaptic cholinergic muscarinic receptors by the combination of carbachol (0.14 micromol/kg, i.v.) and hexamethonium (37 micromol/kg, i.v.), clonidine (3.8 micromol/kg, i.v.) failed to affect the increased motor activity, however, oxymetazoline (0.8-3.4 micromol/kg, i.v.) exerted a pronounced inhibition. These results suggest that different mechanisms may be involved in the inhibitory effect of clonidine and oxymetazoline; while clonidine reduces the gastric motility by activation of presynaptic alpha2-adrenoceptors, postsynaptic component in the effect of oxymetazoline has also been raised.
机译：使用气球法比较了可乐定（非选择性α2-肾上腺素受体激动剂）和羟甲唑啉（α2A-肾上腺素受体激动剂）对大鼠基础和刺激胃运动活动（胃肌张力和收缩）的抑制作用。结果表明，羟甲唑啉（0.2-1.7 micromol / kg，静脉内）降低了基础运动能力，而可乐定（1.9-3.8 micromol / kg，静脉内）对此没有影响。当胰岛素（5 IU /大鼠，静脉）集中刺激运动时，可乐定（1.9-3.8 micromol / kg，静脉）和​​羟甲唑啉（0.1-3.4 micromol / kg，静脉）均会抑制胃运动。然而，尽管可乐定的作用被非选择性的α2-肾上腺素受体拮抗剂育亨宾（5μmol/ kg，iv）和α2A-肾上腺素选择性拮抗剂BRL 44408（3μmol/ kg，iv）所拮抗，但羟甲唑啉的作用却是仅部分受影响。吡唑嗪（α1-和α2B-肾上腺素受体拮抗剂，0.07-0.28μmol/ kg，静脉内）也未能逆转羟甲唑啉的作用。此外，当通过卡巴胆碱（0.14 micromol / kg，iv）和六甲铵（37 micromol / kg，iv）的结合通过突触后胆碱能毒蕈碱受体的活化来刺激胃蠕动时，可乐定（3.8 micromol / kg，iv）未能发挥作用羟甲唑啉（0.8-3.4 micromol / kg，iv）具有明显的抑制作用。这些结果表明可乐定和羟甲唑啉的抑制作用可能涉及不同的机制。尽管可乐定通过激活突触前的α2-肾上腺素能受体来降低胃动力，但在羟甲唑啉中，突触后的成分也有所提高。

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