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肾上腺素、去甲肾上腺素和异丙肾上腺素对豚鼠回肠纵肌中抑制性α和β肾上腺素能受体的作用。

The effects of adrenaline, noradrenaline and isoprenaline on inhibitory alpha- and beta-adrenoceptors in the longitudinal muscle of the guinea-pig ileum.

作者信息

Kosterlitz H W, Lydon R J, Watt A J

出版信息

Br J Pharmacol. 1970 Jun;39(2):398-413. doi: 10.1111/j.1476-5381.1970.tb12903.x.

Abstract
  1. Two preparations, a segment of the ileum and the myenteric plexuslongitudinal muscle preparation, have been used for an analysis of the inhibitory effects of adrenaline, noradrenaline and isoprenaline on the contractor responses of the longitudinal muscle to acetylcholine or to electrical, coaxial or field, stimulation.2. Since the inhibitory effects of adrenaline, noradrenaline and isoprenaline on the acetylcholine-induced contractions were not affected by phenoxybenzamine but were antagonized by propranolol, it is concluded that beta-adrenoceptors are present on the muscle cells.3. The responses to electrical stimulation were suppressed by adrenaline or noradrenaline but only partly inhibited by isoprenaline. Propranolol antagonized the effect of isoprenaline and, to some extent, that of noradrenaline, but scarcely affected the action of adrenaline. Phenoxybenzamine, on the other hand, antagonized most of the effect of adrenaline and, to some extent, that of noradrenaline; it usually potentiated the effect of isoprenaline.4. The output of acetylcholine evoked by electrical stimulation was diminished by adrenaline or noradrenaline but was not affected by isoprenaline. The depressant effect on acetylcholine release was antagonized by phenoxybenzamine but not affected by propranolol; therefore these effects of adrenaline and noradrenaline are mediated by alpha-adrenoceptors.5. It may be assumed that alpha-adrenoceptors in situ are stimulated mainly by circulating adrenaline and possibly noradrenaline and thus cause a prejunctional inhibition at the nerve-smooth muscle junction.
摘要
  1. 两种标本,一段回肠和肠肌丛-纵行肌标本,已被用于分析肾上腺素、去甲肾上腺素和异丙肾上腺素对纵行肌对乙酰胆碱或电刺激、同轴刺激或场刺激的收缩反应的抑制作用。

  2. 由于肾上腺素、去甲肾上腺素和异丙肾上腺素对乙酰胆碱诱导的收缩的抑制作用不受酚苄明影响,但被普萘洛尔拮抗,因此得出结论,肌肉细胞上存在β-肾上腺素能受体。

  3. 肾上腺素或去甲肾上腺素抑制对电刺激的反应,但异丙肾上腺素仅部分抑制该反应。普萘洛尔拮抗异丙肾上腺素的作用,并在一定程度上拮抗去甲肾上腺素的作用,但几乎不影响肾上腺素的作用。另一方面,酚苄明拮抗肾上腺素的大部分作用,并在一定程度上拮抗去甲肾上腺素的作用;它通常增强异丙肾上腺素的作用。

  4. 电刺激诱发的乙酰胆碱释放量被肾上腺素或去甲肾上腺素减少,但不受异丙肾上腺素影响。对乙酰胆碱释放的抑制作用被酚苄明拮抗,但不受普萘洛尔影响;因此,肾上腺素和去甲肾上腺素的这些作用是由α-肾上腺素能受体介导的。

  5. 可以假定,原位的α-肾上腺素能受体主要由循环中的肾上腺素以及可能的去甲肾上腺素刺激,从而在神经-平滑肌接头处引起节前抑制。

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