von Kügelgen I, Starke K
Pharmakologisches Institut, Freiburg, Federal Republic of Germany.
Naunyn Schmiedebergs Arch Pharmacol. 1991 Oct;344(4):419-29. doi: 10.1007/BF00172581.
Effects of electrical stimulation and nicotine on ATP and tritium outflow and smooth muscle tension were studied in the guinea-pig isolated vas deferens preincubated with [3H]-noradrenaline. ATP was measured using the luciferase technique. Electrical stimulation caused biphasic contractions and an acceleration of ATP and tritium outflow. The contraction amplitude and the overflow of ATP increased markedly, whereas the overflow of tritium increased only slightly with the frequency of stimulation (1-10 Hz; constant number of 60 pulses). The contraction amplitude did not increase with an increase in pulse number (20-540 pulses; constant frequency of 5 Hz), whereas the overflow of ATP increased slightly, and that of tritium markedly. Nicotine caused monophasic, transient contractions and, again, an acceleration of ATP and tritium outflow. Contractions, ATP and tritium overflow increased with the concentration of nicotine (56-320 mumol/l) in an approximately parallel manner. The influence of some drugs on responses to electrical stimulation (60 pulses, 5 Hz) and nicotine (180 mumol/l) was investigated. Tetrodotoxin blocked all effects of electrical stimulation but did not change those of nicotine. The reverse was true for hexamethonium. Neither electrical stimulation nor nicotine caused contraction or an increase in ATP outflow after pretreatment with 6-hydroxydopamine. The main effects of prazosin 0.3 mumol/l were to reduce electrically evoked contractions (above all second phase) as well as nicotine-evoked contractions and the nicotine-evoked overflow of ATP (the latter by about 81%). Prazosin also tended to diminish the electrically evoked overflow of ATP. alpha,beta-Methylene-ATP 10 mumol/l elicited a transient contraction and ATP overflow on its own. The main change in the subsequent state of desensitization was a decrease of the first phase of electrically evoked contractions. The main effects of prazosin combined with desensitization by alpha,beta-methylene-ATP were marked decreases of electrically evoked contractions (by 94%), the electrically evoked overflow ATP (by 66%), nicotine-evoked contractions (by 97%) and the nicotine-evoked overflow of ATP (by 70%). It is concluded that both electrical stimulation and nicotine release noradrenaline and ATP in guinea-pig vas deferens. Only part of the evoked overflow of ATP (about 32%) is neural in origin. Another part probably originates from smooth muscle cells where it is released by neurogenic noradrenaline acting at alpha 1-adrenoceptors. Corelease leads to cotransmission: electrically as well as nicotine-evoked contractions consist of adrenergic and purinergic components. Varying types of stimulation release cotransmitter mixtures of varying composition.(ABSTRACT TRUNCATED AT 400 WORDS)
在预先用[3H] - 去甲肾上腺素孵育的豚鼠离体输精管中,研究了电刺激和尼古丁对ATP及氚外流和平滑肌张力的影响。采用荧光素酶技术测定ATP。电刺激引起双相收缩以及ATP和氚外流加速。收缩幅度以及ATP的外流显著增加,而随着刺激频率(1 - 10Hz;固定60个脉冲数)增加,氚的外流仅略有增加。随着脉冲数增加(20 - 540个脉冲;固定频率5Hz),收缩幅度并未增加,而ATP的外流略有增加,氚的外流则显著增加。尼古丁引起单相、短暂收缩,同样也使ATP和氚外流加速。收缩、ATP和氚外流随尼古丁浓度(56 - 320μmol/L)增加而大致呈平行增加。研究了某些药物对电刺激(60个脉冲,5Hz)和尼古丁(180μmol/L)反应的影响。河豚毒素阻断电刺激的所有效应,但不改变尼古丁的效应。六甲铵则相反。用6 - 羟基多巴胺预处理后,电刺激和尼古丁均未引起收缩或ATP外流增加。0.3μmol/L哌唑嗪的主要作用是减少电诱发的收缩(尤其是第二相)以及尼古丁诱发的收缩和尼古丁诱发的ATP外流(后者减少约81%)。哌唑嗪还倾向于减少电诱发的ATP外流。10μmol/L的α,β - 亚甲基ATP自身可引起短暂收缩和ATP外流。随后脱敏状态的主要变化是电诱发收缩第一相的减少。哌唑嗪与α,β - 亚甲基ATP脱敏联合使用的主要作用是显著减少电诱发收缩(减少94%)、电诱发的ATP外流(减少66%)、尼古丁诱发的收缩(减少97%)以及尼古丁诱发的ATP外流(减少70%)。结论是,电刺激和尼古丁在豚鼠输精管中均释放去甲肾上腺素和ATP。所诱发的ATP外流中只有一部分(约32%)源于神经。另一部分可能源于平滑肌细胞,在这里它由作用于α1 - 肾上腺素能受体的神经源性去甲肾上腺素释放。共同释放导致共传递:电刺激以及尼古丁诱发的收缩均由肾上腺素能和嘌呤能成分组成。不同类型的刺激释放不同组成的共递质混合物。(摘要截于400字)