Pharmacological properties of endothelin-1 in the rabbit corpus cavernosum.
Pharmacological properties of endothelin-1 in the rabbit corpus cavernosum.
复制标题
兔海绵体内内皮素-1的药理学特性。
作者：
F. Mumtaz;D. H. Lau;E. Siddiqui;C. Thompson;R. Morgan;D. Mikhailidis
背景
内皮素（ET-1）可能在勃起的调节中起作用，但尚未得到最终证实。在暴露于ET-1和苯肾上腺素（PE; α-1激动剂）后，大鼠海绵体平滑肌（CSM）收缩增强。本研究的目的是评估ET-1的作用及其在勃起过程中的α 1-肾上腺素能通路中的可能作用。
材料和方法
对从12只年龄匹配的新西兰白色兔获得的阴茎CSM条进行器官浴研究。评估了在不存在和存在ETA（BQ 123）和ETB（BQ 788）拮抗剂的情况下，ET-1和PE单独对CSM张力的影响。组织反应测量为张力（牛顿，N）。EC 50值表示为平均值+/- S.E.M.。
结果
PE（10（8）~ 10（-4）M）和ET-1（10（-10）~ 10（-6）M）对兔CSM条产生浓度依赖性收缩。EC 50值分别为1.7 x 10（-7）M +/- 1.1和3.4 x 10（-9）M +/- 1.5。BQ 123 10（-5）M比BQ 788 10（-5）M显著抑制ET-1介导的CSM收缩（均为ANOVA p<0.01）。EC 50分别为1.3 x 10（-6）M +/- 2.6和2.0 x 10（-7）M +/- 2.1。ETA或ETB受体拮抗剂对α 1-肾上腺素能受体介导的CSM收缩均无显著影响。
结论
ETA受体在ET-1诱导的兔脊髓平滑肌收缩和消肿过程中可能起着比ETB受体更大的作用。α 1-肾上腺素能依赖性途径不涉及ETA或ETB受体。
BACKGROUND
Endothelin (ET-1) may play a role in the regulation of erection but this has not been conclusively demonstrated. Augmented cavernosal smooth muscle (CSM) contraction in the rat occurs following exposure to both ET-1 and phenylephrine (PE; alpha-1 agonist). The aim of this study was to assess the effect of ET-1 and its possible role in the alpha1-adrenergic pathway during the erectile process.
MATERIALS AND METHODS
Organ bath studies were performed on CSM strips of penises obtained from 12 age-matched New Zealand White rabbits. The effect of ET-1 and PE alone on CSM tone in the absence and presence of ETA (BQ123) and ETB (BQ788) antagonists was assessed. Tissue responses were measured as tension (newton, N). EC50 values are expressed as mean +/- S.E.M.
RESULTS
PE (10(8) - 10(-4) M) and ET-1 (10(-10) - 10(-6) M) produced a concentration-dependent contraction in rabbit CSM strips. The EC50 values were 1.7 x 10(-7) M +/- 1.1 and 3.4 x 10(-9) M +/- 1.5, respectively. BQ123 10(-5) M significantly inhibited ET-1-mediated CSM contractions more than BQ788 10(-5) M (both ANOVA p<0.01). The EC50 were 1.3 x 10(-6) M +/- 2.6 and 2.0 x 10(-7) M +/- 2.1, respectively. Neither the ETA or ETB receptor antagonist had a significant influence on alpha1-adrenergic receptor-mediated CSM contraction.
CONCLUSION
ETA receptors may play a greater role than ETB receptors in ET-1-induced rabbit CSM contraction and the detumescence process. The a1-adrenergic-dependent pathway does not involve the ETA or ETB receptors.
影响因子：
6.6
作者：
BUSH, PA;ARONSON, WJ;IGNARRO, LJ
通讯作者：
IGNARRO, LJ
内皮素-1 诱导的 α1-肾上腺素能激动剂对人海绵体平滑肌引起的收缩反应的调节。
DOI：
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发表时间：
1996
期刊：
International journal of impotence research.
影响因子：
--
作者：
Kim,DC;Gondre,CM;Christ,GJ
通讯作者：
Christ,GJ