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小鼠输精管中的α-肾上腺素能受体及其对输精管电刺激反应的影响。

alpha-Adrenoceptors in the mouse vas deferens and their effects on its response to electrical stimulation.

作者信息

Marshall I, Nasmyth P A, Nicholl C G, Shepperson N B

出版信息

Br J Pharmacol. 1978 Jan;62(1):147-51. doi: 10.1111/j.1476-5381.1978.tb07018.x.

Abstract

1 Noradrenaline (ID50, 0.75 micrometer) and clonidine (ID50, 2.8 nM) produced a dose-related inhibition of the twitch response of the isolated vas deferens of the mouse to electrical stimulation, their effectiveness decreasing as frequency of stimulation increased from 0.2 to 16 hertz. 2 Phenylephrine (1.0--2.0 micrometer) produced a dose-related contraction of the mouse isolated vas deferens and potentiated the responses to field stimulation. 3 Yohimbine (10 nM) antagonized the inhibitory effects of noradrenaline and clonidine, but had no effect on the motor activity of phenylephrine. At a concentration of 128 nM yohimbine potentiated the twitch response by 110% at 1 Hz, but its effectiveness decreased with increasing frequency of stimulation up to 16 hertz. 4 Thymoxamine (0.3 micrometer) antagonized the effects of phenylephrine, but not those of clonidine. 5 From a consideration of the known characteristics of pre- and postsynaptic alpha-adrenoceptors, it is concluded that the inhibitory effect of noradrenaline is produced by stimulation of the former and the effects of phenylephrine by stimulation of the latter.

摘要
  1. 去甲肾上腺素(半数抑制浓度,0.75微摩尔)和可乐定(半数抑制浓度,2.8纳摩尔)对小鼠离体输精管对电刺激的抽搐反应产生剂量相关的抑制作用,随着刺激频率从0.2赫兹增加到16赫兹,它们的效力降低。2. 去氧肾上腺素(1.0 - 2.0微摩尔)使小鼠离体输精管产生剂量相关的收缩,并增强对场刺激的反应。3. 育亨宾(10纳摩尔)拮抗去甲肾上腺素和可乐定的抑制作用,但对去氧肾上腺素的运动活性无影响。在128纳摩尔浓度下,育亨宾在1赫兹时使抽搐反应增强110%,但其效力随着刺激频率增加到16赫兹而降低。4. 百里胺(0.3微摩尔)拮抗去氧肾上腺素的作用,但不拮抗可乐定的作用。5. 根据已知的突触前和突触后α-肾上腺素能受体的特性,得出结论:去甲肾上腺素的抑制作用是由前者的刺激产生的,而去氧肾上腺素的作用是由后者的刺激产生的。

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5
Selectivity of blocking agents for pre-and postsynaptic alpha-adrenoceptors.
Br J Pharmacol. 1977 May;60(1):91-6. doi: 10.1111/j.1476-5381.1977.tb16752.x.

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