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肾上腺素能激动剂不与拮抗剂(-)3-[¹²⁵I]碘氰吲哚洛尔竞争结合大鼠胸膜或腹膜肥大细胞肾上腺素能受体。

Adrenergic agonists do not compete with the antagonist (-)3-[125I]iodocyanopindolol for binding to rat pleural or peritoneal mast cell adrenergic receptor.

作者信息

Botana L M

出版信息

Gen Pharmacol. 1987;18(3):263-7. doi: 10.1016/0306-3623(87)90009-7.

Abstract

(-)3-[125I]iodocyanopindolol (ICYP), a high selective, high specific beta antagonist is employed to characterize beta-adrenoceptors on rat pleural and peritoneal mast cell populations. Results show that non specific binding is low, and that pleural mast cells exhibit greater number of receptors per cell (140,000) than peritoneal cells (90,000). Dissociation constants (Kd) are 0.37 +/- 0.01 and 0.55 +/- 0.02 nM for pleural and peritoneal cells, respectively. Competition experiments show that isoproterenol do not displaces ICYP neither in pleural nor in peritoneal cells. Low concentrations of propranolol displace ICYP from its binding sites, but atenolol does not. Results point to the existence in mast cells of mainly atypical. beta 2-receptors, since the agonist isoproterenol does not compete with the antagonist ICYP.

摘要

(-)3 - [¹²⁵I]碘氰吲哚洛尔(ICYP),一种高选择性、高特异性的β受体拮抗剂,被用于表征大鼠胸膜和腹膜肥大细胞群体上的β肾上腺素能受体。结果表明,非特异性结合较低,且胸膜肥大细胞每个细胞显示出比腹膜细胞(90,000个)更多的受体数量(140,000个)。胸膜和腹膜细胞的解离常数(Kd)分别为0.37±0.01和0.55±0.02 nM。竞争实验表明,异丙肾上腺素在胸膜细胞和腹膜细胞中均不能取代ICYP。低浓度的普萘洛尔能将ICYP从其结合位点上取代,但阿替洛尔则不能。结果表明肥大细胞中主要存在非典型的β₂受体,因为激动剂异丙肾上腺素不能与拮抗剂ICYP竞争。

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