Yaris Ersin, Kesim Murat, Kadioglu Mine, Kalyoncu Nuri Ihsan, Ulku Cunay, Ozyavuz Rasin
Department of Pharmacology, School of Medicine, Karadeniz Technical University, TR-61187 Trabzon, Turkey.
Pharmacol Res. 2003 Oct;48(4):335-45. doi: 10.1016/s1043-6618(03)00157-9.
The aim of the present study is to evaluate whether paroxetine (a selective serotonin re-uptake inhibitor) can modify the contractile responses of isolated vas deferens. Some contractile agents, potassium chloride (KCl), adenosine 5'-triphosphate (ATP), noradrenaline (NA), and electrical field stimulation (EFS) caused contractions both in epididymal and prostatic portions of vas deferens. Paroxetine (PX) in concentrations 10(-7) and 10(-6)M potentiated the contractions to KCl and ATP only in epididymal portion but in higher concentrations (10(-5) and 10(-4)M) inhibited the responses in both portions. NA responses were inhibited by PX in all concentrations used, both in prostatic and epididymal portions. Prazosin (PR), an alpha adrenergic receptor blocking agent, inhibited PX-induced potentiation observed for higher concentrations of KCl. PR also inhibited PX-induced potentiation on the responses to ATP in epididymal portion. Pretreatment with PX (10(-7) to 10(-6)M) increased the contractions to EFS but in 10(-5) and 10(-4)M concentrations inhibited them. Even though the preparations were washed out, the inhibited responses of contractile agents could not be restored. After a washout period for PX, when Bay K 8644 (calcium channel activator) was added to the bath medium, the contractile responses to KCl were partially restored. In calcium-free medium, KCl caused contractions in concentrations higher than 80 mM with lower amplitudes which were not affected by PX. Reserpinization did not change the inhibitory pattern of PX's effect on exogenously applied NA in all concentrations tested. In reserpinized rats, the potentiation caused by PX in exogenously applied ATP responses was not observed. In conclusion, we can say that PX has two different effects: inhibition and potentiation of contractions to various agonists. The inhibitory effect of the drug can be explained by a calcium channel blocking activity. The potentiating effect of the drug is mainly related to its presynaptic action, such as NA re-uptake inhibitory effect.
本研究的目的是评估帕罗西汀(一种选择性5-羟色胺再摄取抑制剂)是否能改变离体输精管的收缩反应。一些收缩剂,氯化钾(KCl)、5'-三磷酸腺苷(ATP)、去甲肾上腺素(NA)和电场刺激(EFS)均可引起输精管附睾部和前列腺部收缩。浓度为10^(-7)和10^(-6)M的帕罗西汀(PX)仅增强了附睾部对KCl和ATP的收缩反应,但在较高浓度(10^(-5)和10^(-4)M)时则抑制了两部分的反应。在所使用的所有浓度下,NA反应在前列腺部和附睾部均被PX抑制。哌唑嗪(PR),一种α肾上腺素能受体阻断剂,抑制了高浓度KCl时观察到的PX诱导的增强作用。PR也抑制了附睾部对ATP反应的PX诱导的增强作用。用PX(10^(-7)至10^(-6)M)预处理可增强对EFS的收缩反应,但在10^(-5)和10^(-4)M浓度时则抑制了这种反应。即使冲洗标本,收缩剂的受抑制反应也无法恢复。在冲洗掉PX一段时间后,当向浴液中加入Bay K 8644(钙通道激活剂)时,对KCl的收缩反应部分恢复。在无钙培养基中,KCl在浓度高于80 mM时引起收缩,幅度较小,且不受PX影响。利血平化并未改变PX对外源性应用的所有浓度NA作用的抑制模式。在利血平化的大鼠中,未观察到PX对外源性应用的ATP反应的增强作用。总之,我们可以说PX有两种不同的作用:对各种激动剂收缩反应的抑制和增强。药物的抑制作用可通过钙通道阻断活性来解释。药物的增强作用主要与其突触前作用有关,如NA再摄取抑制作用。