Morin-Surun M P, Boudinot E, Gacel G, Champagnat J, Roques B P, Denavit-Saubie M
Eur J Pharmacol. 1984 Feb 17;98(2):235-40. doi: 10.1016/0014-2999(84)90594-6.
The involvement of different opiate receptor subtypes in opiate-induced respiratory depression was studied in the unanaesthetized rat. Synthetic opioid agonists, specific for mu or delta receptors, were administered intraperitoneally in freely moving rats while respiratory parameters were recorded by means of the whole body plethysmographic method. TRIMU-4 (Tyr-D-Ala-Gly-NH-CH(CH3)-CH2-CH(CH3)2), a specific agonist of the mu receptor, reduced the tidal volume and did not change the respiratory frequency. DSLET (Tyr-D-Ser-Gly-Phe-Leu-Thr), a relatively specific agonist of the delta receptor subtype, reduced respiratory frequency and was significantly less effective on tidal volume than was TRIMU-4. It is concluded that the respiratory depression occurring after the administration of opiates in clinical practice is a dual complementary effect involving mu and delta receptors.
在未麻醉的大鼠中研究了不同阿片受体亚型在阿片类药物所致呼吸抑制中的作用。对μ或δ受体具有特异性的合成阿片类激动剂,经腹腔注射给予自由活动的大鼠,同时采用全身体积描记法记录呼吸参数。μ受体特异性激动剂TRIMU-4(酪氨酰-D-丙氨酰-甘氨酰-NH-CH(CH3)-CH2-CH(CH3)2)可降低潮气量,但不改变呼吸频率。δ受体亚型相对特异性激动剂DSLET(酪氨酰-D-丝氨酰-甘氨酰-苯丙氨酰-亮氨酰-苏氨酸)可降低呼吸频率,且对潮气量的作用明显弱于TRIMU-4。得出结论,临床实践中给予阿片类药物后发生的呼吸抑制是涉及μ和δ受体的双重互补效应。