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Adrenergic receptors in the bovine mammary artery.

机译:牛乳腺动脉中的肾上腺素能受体。

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摘要

The response of isolated preparations of bovine mammary artery was investigated, with the aim of characterising further the adrenergic receptor subtypes present. Noradrenaline (NA) and the alpha(1) agonist phenylephrine gave sigmoidal dose-response curves with pEC(50) values of 5.97+/-0.07 (N=34) and 6.21+/-0.32 (N=8), respectively. Stimulation of alpha(2) receptors with UK 14,304 produced a weak response with pEC(50) of 6.78+/-0.38 (N=7), and maximal contraction of 17.8+/-9.9% relative to NA. A61603, an alpha(1A) agonist, gave a curve parallel to NA, but shifted to the left (pEC(50) of 6.98+/-0.19 (N=5)); this drug had an increased potency of 10-fold relative to NA, and 4-fold relative to phenylephrine. Schild analysis of curves obtained with the alpha(1) antagonist prazosin gave a pA(2) of 8.70+/-0.47 (N=6-9), whereas the alpha(2) antagonist yohimbine resulted in a pA(2) of 7.65+/-0.16 (N=4). The alpha(1A) receptor antagonists WB4101 and 5-methylurapidil gave pA(2) values of 9.39+/-0.69 (N=4) and 7.72+/-0.02 (N=2-3), respectively. The irreversible alpha(1B) inhibitor CEC reduced the pEC(50) from 5.39+/-0.12 to 4.31+/-0.18 (N=7) only at the highest dose used, and high doses of the alpha(1D) antagonist BMY 7378 produced a shift to the right at giving a pA(2) of 7.37+/-0.08 (N=3). These results suggest major involvement of the alpha(1B) adrenergic receptor subtype in contraction of the bovine mammary artery, which is similar to the human internal mammary artery.
机译:为了进一步表征存在的肾上腺素能受体亚型,研究了牛乳腺动脉分离制剂的反应。去甲肾上腺素(NA)和α(1)激动剂去氧肾上腺素给出的S型剂量反应曲线的pEC(50)值分别为5.97 +/- 0.07(N = 34)和6.21 +/- 0.32(N = 8)。 UK 14,304刺激alpha(2)受体产生较弱的响应,pEC(50)为6.78 +/- 0.38(N = 7),相对于NA的最大收缩为17.8 +/- 9.9%。 A61603是一种alpha(1A)激动剂,其曲线与NA平行,但向左移动(pEC(50)为6.98 +/- 0.19(N = 5));该药物相对于NA的效力提高了10倍,相对于去氧肾上腺素增加了4倍。用阿尔法(1)拮抗剂哌唑嗪获得的曲线的Schild分析得出pA(2)为8.70 +/- 0.47(N = 6-9),而阿尔法(2)拮抗剂育亨宾导致的pA(2)为7.65 +/- 0.16(N = 4)。 alpha(1A)受体拮抗剂WB4101和5-甲基尿嘧啶的pA(2)值分别为9.39 +/- 0.69(N = 4)和7.72 +/- 0.02(N = 2-3)。不可逆的alpha(1B)抑制剂CEC仅在最高剂量和高剂量的alpha(1D)拮抗剂BMY 7378的作用下将pEC(50)从5.39 +/- 0.12降低到4.31 +/- 0.18(N = 7)产生右移,给出的pA(2)为7.37 +/- 0.08(N = 3)。这些结果表明,α(1B)肾上腺素能受体亚型主要参与牛乳腺动脉的收缩,这与人的乳内动脉相似。

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