Head G A, de Jong W
J Cardiovasc Pharmacol. 1985 Mar-Apr;7(2):321-6. doi: 10.1097/00005344-198503000-00018.
The possible involvement of endogenous opioid peptides in the cardiovascular responses observed following central alpha-adrenoceptor stimulation with clonidine, alpha-methyldopa (alpha-MD), and 6-hydroxydopamine (6-OHDA) was examined in conscious normotensive Wistar and spontaneously hypertensive (SHR) rats. Clonidine [2.5 micrograms intracisternally (i.c.)] produced rapid hypotension (-36 +/- 2 mm Hg) and bradycardia (-53 +/- 5 beats/min) in SHR that were similar to observations in animals given either naloxone (50 micrograms i.c. or 10 mg/kg i.p.) or appropriate saline control injections. Peripheral doses of naloxone (1-2 mg/kg) or saline did not further change arterial pressure or heart rate in either Wistar rats or SHR given alpha-MD (1.0 mg i.c.) 3 h earlier. In addition, central doses of naloxone (3 X 50 micrograms i.c.) given at hourly intervals did not affect the responses to alpha-MD. Central administration of 6-OHDA acutely releases noradrenaline which produces an initial fall in arterial blood pressure and heart rate. Intracisternal 6-OHDA (400 micrograms) produced similar time course and maximum circulatory effects in rats given naloxone (50 micrograms i.c. before and at each subsequent hour) as in saline-treated animals. Naloxone (1 mg/kg s.c.) significantly attenuated morphine-induced analgesia. These findings do not support a critical role of endogenous opioids in mediating the acute antihypertensive actions of clonidine and alpha-MD or in the cardiovascular responses produced by noradrenaline release following central 6-OHDA.
在清醒的正常血压Wistar大鼠和自发性高血压(SHR)大鼠中,研究了内源性阿片肽是否参与可乐定、α-甲基多巴(α-MD)和6-羟基多巴胺(6-OHDA)中枢α-肾上腺素能受体刺激后所观察到的心血管反应。可乐定[脑池内注射(i.c.)2.5微克]在SHR中引起快速低血压(-36±2毫米汞柱)和心动过缓(-53±5次/分钟),这与给予纳洛酮(脑池内注射50微克或腹腔注射10毫克/千克)或适当生理盐水对照注射的动物的观察结果相似。外周给予纳洛酮(1 - 2毫克/千克)或生理盐水,对3小时前给予α-MD(脑池内注射1.0毫克)的Wistar大鼠或SHR的动脉血压或心率没有进一步影响。此外,每小时间隔给予脑池内剂量的纳洛酮(3×50微克)不影响对α-MD的反应。中枢给予6-OHDA可急性释放去甲肾上腺素,导致动脉血压和心率最初下降。脑池内注射6-OHDA(400微克)在给予纳洛酮(每次脑池内注射50微克,每次注射前及之后每小时一次)的大鼠中产生的时间进程和最大循环效应与生理盐水处理的动物相似。皮下注射纳洛酮(1毫克/千克)可显著减弱吗啡诱导的镇痛作用。这些发现不支持内源性阿片类物质在介导可乐定和α-MD的急性降压作用或中枢给予6-OHDA后去甲肾上腺素释放所产生的心血管反应中起关键作用。