Hassen A H, Feuerstein G, Faden A I
Neuropharmacology. 1984 Apr;23(4):407-15. doi: 10.1016/0028-3908(84)90248-x.
The respiratory and cardiovascular effects of the highly selective mu opioid agonist, D-Ala2, MePhe4, Gly- ol5 enkephalin ( DAGO ) and the relatively selective delta agonist, D-Leu5 enkephalin (DADL) were compared following injection (0.1 microliter) into the nucleus ambiguus (NA) of spontaneously-breathing and artificially-respired, pentobarbital-anesthetized rats. In non-ventilated animals, the opioids elicited dose-related (3 X 10(-11) -3 X 10(-9) M), naloxone-reversible depression of respiratory rate (RR) without altering the tidal volume. Mean arterial pressure (MAP) was unchanged at small doses and decreased at the largest dose; heart rate (HR) was unchanged. In artificially-respired animals, both peptides elicited dose-related, naloxone-reversible increases in mean arterial pressure and heart rate; DAGO was significantly more potent than DADL (P less than 0.01). Given the relative potency and selectivity of the opioids tested, these findings are consistent with the conclusion that mu receptors may selectively mediate the respiratory and cardiovascular actions of opioids in an important brain stem cardiorespiratory center in the rat. Moreover, these data indicate the importance of respiratory effects on the cardiovascular activity of centrally administered opioids.
将高选择性μ阿片受体激动剂D - Ala2,MePhe4,Gly - ol5脑啡肽(DAGO)和相对选择性δ激动剂D - Leu5脑啡肽(DADL)注射(0.1微升)到戊巴比妥麻醉的自主呼吸和人工呼吸大鼠的疑核(NA)后,比较它们对呼吸和心血管系统的影响。在非通气动物中,阿片类药物引起剂量相关的(3×10^(-11) - 3×10^(-9) M)、纳洛酮可逆转的呼吸频率(RR)降低,而潮气量不变。小剂量时平均动脉压(MAP)不变,最大剂量时降低;心率(HR)不变。在人工呼吸的动物中,两种肽均引起剂量相关的、纳洛酮可逆转的平均动脉压和心率升高;DAGO的效力明显高于DADL(P < 0.01)。鉴于所测试阿片类药物的相对效力和选择性,这些发现与以下结论一致:μ受体可能在大鼠重要的脑干心肺呼吸中枢中选择性介导阿片类药物的呼吸和心血管作用。此外,这些数据表明呼吸效应对中枢给予阿片类药物心血管活动的重要性。