A study of the possible influence of central 5-HT function on clonidine-induced hypoactivity responses in mice
A study of the possible influence of central 5-HT function on clonidine-induced hypoactivity responses in mice
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中枢 5-HT 功能对可乐定诱导的小鼠活动减退反应可能影响的研究
作者：
D. Heal;J. Philpot
给予 α2-肾上腺素受体激动剂可乐定 (0.1 mg/kg) 会导致小鼠活动减退。使用 5-HT 再摄取抑制剂齐美定（1 或 10 mg/kg）或 5-HT 激动剂奎帕嗪（0.25 或 2.5 mg/kg）预处理不会改变这种镇静反应。 5-HT1B 激动剂 RU 24969（0.2 或 1 mg/kg）在较高剂量下可增强活动减退反应。非选择性 5-HT 拮抗剂美西麦角 (methysergide)（1 或 10 mg/kg）和米角林（0.2 或 1 mg/kg）可增强可乐定引起的活动减退。然而，米角林产生的显着增强作用可能是由于其作为 α1-肾上腺素受体拮抗剂的有效作用。然而，5-HT2 拮抗剂利坦色林（0.1 或 1 mg/kg）和酮色林（0.1 或 1 mg/kg）均以剂量依赖性方式增强可乐定的活性减退。高剂量的 β-肾上腺素受体拮抗剂也会抑制 5-HT1 受体。吲哚洛尔（10 mg/kg）对镇静没有作用，但[-]-普萘洛尔（20 mg/kg）引起一定的镇静作用。后一种效应可能不是由于 5-HT1 受体的抑制所致，因为这种减少也发生在低剂量（2 mg/kg）下。通过脑室内注射 5,7-二羟色胺（50 μg）破坏 5-HT 神经元，导致活动减退略有增加。总之，这些数据表明中枢 5-HT 功能可以影响 α2-肾上腺素受体介导的活动减退反应。然而，由于这些作用通常只有在严格控制 5-HT 功能后才会显现出来，这表明虽然这些相互作用可能具有药理学意义，但它们可能不具有生理重要性。
Administration of the α2-adrenoceptor agonist clonidine (0.1 mg/kg) produces hypoactivity in mice. This sedation response was unaltered by pretreatment with either the 5-HT reuptake inhibitor zimeldine (1 or 10 mg/kg) or the 5-HT agonist quipazine (0.25 or 2.5 mg/kg). The 5-HT1B agonist RU 24969 (0.2 or 1 mg/kg) enhanced hypoactivity responses at the higher dose. The non-selective 5-HT antagonists methysergide (1 or 10 mg/kg) and metergoline (0.2 or 1 mg/kg) potentiated clonidine-induced hypoactivity. However, the marked enhancement produced by metergoline may have been due to its potent action as a α1-adrenoceptor antagonist. Nevertheless, the 5-HT2 antagonists ritanserin (0.1 or 1 mg/kg) and ketanserin (0.1 or 1 mg/kg) both potentiated clonidine hypoactivity in a dose-dependent manner. β-Adrenoceptor antagonists also inhibit 5-HT1 receptors at high dose. Pindolol (10 mg/kg) had no effect on sedation, but [-]-propranolol (20 mg/kg) caused some attenuation. This latter effect was probably not due to inhibition of 5-HT1 receptors, because this reduction also occurred at low dose (2 mg/kg). Destruction of 5-HT neurones by intracerebroventricular injection of 5,7-dihydroxytryptamine (50 μg) resulted in a marginal increase in hypoactivity. In conclusion, these data shown that central 5-HT function can influence α2-adrenoceptor-mediated hypoactivity responses. However, since these effects were usually only apparent after severe manipulation of 5-HT function, it suggests that while these interactions may be of pharmacological interest, they are probably not of physiological importance.
多种血清素受体：中缝病变的区域分布和影响。
影响因子：
5
作者：
Blackshear,MA;Steranka,LR;Sanders-Bush,E
通讯作者：
Sanders-Bush,E