首页> 外文期刊>British Journal of Pharmacology >Prostanoid receptors of the EP_3 subtype mediate inhibition of evoked [~3H] acetylcholine release from isolated human bronchi
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Prostanoid receptors of the EP_3 subtype mediate inhibition of evoked [~3H] acetylcholine release from isolated human bronchi

机译:EP_3亚型的类前列腺素受体介导抑制诱发的分离人支气管中的[〜3H]乙酰胆碱释放

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摘要

The release of neuronal [~3H]acetylcholine (ACh) from isolated human bronchi after labelling with [~3H]choline was measured to investigate the effects of prostanoids. A first period of electrical field stimulation(S_1) caused a [~3H]ACh release of 320±70 and 200±40 Becquerel(Bq) g~-1 in epithelium-denuded and epithelium-containing bronchi respectively (P > 0.05). Subsequent periods of electrical stimulation(S_n, n =2, 3, and 4) released less [~3H]ACh, i.e. decreasing S_n/ S_1 values were obtained (0.76±0.09, 0.68±0.07 and 0.40±0.04, respectively). Cumulative concentrations(1-1000 nM) of EP-receptor agonists like prostaglandin E_2, nocloprost, And sulprostone(EP_1 and EP_3 selective)inhibited evoked[~3H]ACh release in a concentration dependent Manner with IC_50 values between 4-14 nM and maximal inhibition of about 70/100.
机译:用[〜3H]胆碱标记后,测量分离的人支气管中神经元[〜3H]乙酰胆碱(ACh)的释放,以研究类前列腺素的作用。电场刺激的第一阶段(S_1)分别导致上皮裸露的和含上皮的支气管中的[〜3H] ACh释放分别为320±70和200±40 Becquerel(Bq)g〜-1(P> 0.05)。随后的电刺激周期(S_n,n = 2、3和4)释放的[〜3H] ACh较少,即降低了S_n / S_1值(分别为0.76±0.09、0.68±0.07和0.40±0.04)。前列腺素E_2,诺氯前列素和舒普洛司通(EP_1和EP_3选择性)等EP受体激动剂的累积浓度(1-1000 nM),抑制了诱发的[〜3H] ACh释放,IC_50值为4-14 nM,最大值抑制约70/100。

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