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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >R-zacopride, a 5-HT3 antagonist/5-HT4 agonist, reduces sleep apneas in rats.
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R-zacopride, a 5-HT3 antagonist/5-HT4 agonist, reduces sleep apneas in rats.

机译：R-zacopride是5-HT3拮抗剂/ 5-HT4激动剂，可减轻大鼠的睡眠呼吸暂停。

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摘要

The effects of R-zacopride, a benzamide with potent 5-HT3 receptor antagonist and 5-HT4 receptor agonist properties, on spontaneous apneas were studied in 10 Sprague-Dawley rats by monitoring respiration and sleep for 6 h. R-zacopride (0.5, 1.0 and 10.0 mg/kg) suppressed spontaneous central apneas during non-rapid-eye-movement (NREM) sleep by 50% (P=.05 for 0.5 mg/kg, P=.02 for 1.0 mg/kg and P=.001 for 10.0 mg/kg dose vs. control), and during rapid-eye-movement (REM) sleep by 80% by all doses tested (P<.0007) for at least 2 h after intraperitoneal injection. We conclude that R-zacopride, over a 20-fold dose range, significantly reduces central apnea expression during NREM and REM sleep in the rat. The efficacy of this compound to suppress central apneas most probably arises from its antagonist actions at 5-HT3 receptors or from its mixed agonist/antagonist profile at 5-HT4/5-HT3 receptors.
机译：通过监测呼吸和睡眠6小时，研究了10只Sprague-Dawley大鼠中R-zacopride（一种具有有效的5-HT3受体拮抗剂和5-HT4受体激动剂特性的苯甲酰胺）对自发性呼吸暂停的影响。 R-zacopride（0.5、1.0和10.0 mg / kg）将非快速眼动（NREM）睡眠期间的自发性中枢性呼吸暂停抑制了50％（0.5 mg / kg时P = .05,1.0 mg时P = .02 / kg，对于10.0 mg / kg剂量，与对照组相比，P = .001），并且在所有试验剂量的快速眼动（REM）睡眠期间，至少2 h（P <.0007）睡眠至少2小时。我们得出的结论是，R-扎克必利在20倍剂量范围内，可显着降低大鼠NREM和REM睡眠期间的中枢性呼吸暂停表达。该化合物抑制中枢性呼吸暂停的功效最可能源于其对5-HT3受体的拮抗作用或源自其对5-HT4 / 5-HT3受体的混合激动剂/拮抗剂特性。

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