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异丙肾上腺素和去氧肾上腺素对豚鼠冷贮存及新鲜盲肠条腺苷3',5'-单磷酸含量和机械活性的影响

Effect of isoprenaline and phenylephrine on the adenosine 3',5'-monophosphate content and mechanical activity of cold-stored and fresh taenia caecum from the guinea-pig.

作者信息

Honda F, Katsuki S, Miyahara J T, Shibata S

出版信息

Br J Pharmacol. 1977 Aug;60(4):529-36. doi: 10.1111/j.1476-5381.1977.tb07531.x.

Abstract
  1. Cold storage treatment of the guinea-pig taenia caecum had a greater inhibitory effect on the isoprenaline-induced relaxation than that induced by phenylephrine. Prolonged cold storage (12-14 days) almost abolished the effect of isoprenaline but only reduced the phenylephrine effect. The ED50 of cyclic adenosine 3',5'-monophosphate (cyclic AMP) that elicited muscle relaxation was not altered by the prolonged cold storage. 2. After cold storage treatment, tissue cyclic AMP content was decreased; however, isoprenaline still caused a dose-dependent increase in the cyclic AMP level. The threshold dose of isoprenaline for cyclic AMP accumulation was the same in fresh and cold-stored preparations. 3. In the fresh preparation, the onset of the isoprenaline (10(-6)M)-induced relaxation preceded the increase in tissue cyclic AMP. 4. Isoprenaline, phenylephrine, adrenaline and noradrenaline at doses (ED50) sufficient to induce muscle relaxation did not always increase the cyclic AMP level. 5. Similarly, the responses to papaverine and nitroglycerine were not accompanied by an increase in cyclic AMP. 6. The adenylate cyclase and phosphodiesterase (low and high Km) activities of taenia caecum were not attenuated by the prolonged cold storage. 7. Propranolol inhibited both the isoprenaline-induced relazation and cyclic AMP accumulation; however, the pA2 values were significantly different for the two events. 8. Based on these results, both the relaxation and cyclic AMP accumulation caused by isoprenaline are mediated by activation of beta-adrenoceptors but are independent phenomena.
摘要
  1. 豚鼠盲肠带的冷藏处理对异丙肾上腺素诱导的舒张作用的抑制作用比对去氧肾上腺素诱导的舒张作用更强。长时间冷藏(12 - 14天)几乎消除了异丙肾上腺素的作用,但仅降低了去氧肾上腺素的作用。引起肌肉舒张的环磷腺苷(cAMP)的半数有效剂量(ED50)不受长时间冷藏的影响。2. 冷藏处理后,组织cAMP含量降低;然而,异丙肾上腺素仍能引起cAMP水平呈剂量依赖性增加。新鲜制剂和冷藏制剂中,异丙肾上腺素引起cAMP积累的阈剂量相同。3. 在新鲜制剂中,异丙肾上腺素(10⁻⁶M)诱导的舒张开始先于组织cAMP的增加。4. 足以诱导肌肉舒张的剂量(ED50)的异丙肾上腺素、去氧肾上腺素、肾上腺素和去甲肾上腺素并不总是增加cAMP水平。5. 同样,对罂粟碱和硝酸甘油的反应也不伴有cAMP的增加。6. 盲肠带的腺苷酸环化酶和磷酸二酯酶(低Km和高Km)活性不受长时间冷藏的减弱。7. 普萘洛尔抑制异丙肾上腺素诱导的舒张和cAMP积累;然而,这两个事件的pA2值有显著差异。8. 根据这些结果,异丙肾上腺素引起的舒张和cAMP积累均由β - 肾上腺素能受体激活介导,但它们是独立的现象。

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