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四种不同β-肾上腺素能受体阻断药物对淋巴细胞异丙肾上腺素刺激的环磷酸腺苷生成的比较。

Comparison of four different beta-adrenoceptor blocking drugs on lymphocyte isoprenaline-stimulated cyclic AMP production.

作者信息

Lima D R, Kilfeather S, Hedges A, Turner P

出版信息

Br J Clin Pharmacol. 1981 Jun;11(6):555-9. doi: 10.1111/j.1365-2125.1981.tb01170.x.

Abstract

1 The influence of acebutolol, atenolol, pindolol and timolol on human lymphocyte cyclic AMP (cAMP) and its stimulation by isoprenaline in vitro has been studied. 2 Acebutolol and atenolol (10(-8)-10(-6)M) had no significant influence on lymphocyte cAMP levels or on isoprenaline-stimulated increase in cAMP. 3 Pindolol and timolol significantly antagonised the effect of isoprenaline, and pA2 values were calculated to be 8.12 and 8.04 respectively. This suggests that beta 2-adrenoceptors are involved in this phenomenon. 4 Only pindolol produced a significant increase in lymphocyte cAMP, which is consistent with its partial agonist activity.

摘要
  1. 已研究了醋丁洛尔、阿替洛尔、吲哚洛尔和噻吗洛尔对人淋巴细胞环磷酸腺苷(cAMP)的影响及其在体外对异丙肾上腺素刺激cAMP的作用。

  2. 醋丁洛尔和阿替洛尔(10⁻⁸ - 10⁻⁶M)对淋巴细胞cAMP水平或异丙肾上腺素刺激的cAMP增加无显著影响。

  3. 吲哚洛尔和噻吗洛尔显著拮抗异丙肾上腺素的作用,计算出的pA2值分别为8.12和8.04。这表明β₂肾上腺素能受体参与了这一现象。

  4. 仅吲哚洛尔使淋巴细胞cAMP显著增加,这与其部分激动剂活性一致。

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1
Beta-adrenoceptors in human lung, bronchus and lymphocytes.人肺、支气管及淋巴细胞中的β-肾上腺素能受体。
Br J Clin Pharmacol. 1980 Nov;10(5):425-32. doi: 10.1111/j.1365-2125.1980.tb01783.x.
7
The assessment of beta-adrenoceptor blocking drugs in man.人体中β-肾上腺素能受体阻断药物的评估。
Br J Clin Pharmacol. 1977 Aug;4(4):413-25. doi: 10.1111/j.1365-2125.1977.tb00756.x.

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