Wallis D I, Connell L A, Kvaltinova Z
Department of Physiology, University of Wales College of Cardiff, Great Britain.
Naunyn Schmiedebergs Arch Pharmacol. 1991 Apr;343(4):344-52. doi: 10.1007/BF00179038.
Using the hemisected spinal cord of the neonate rat, the effects of altered external Ca, thyrotrophin-releasing hormone (TRH) and a number of antagonists were tested on depolarizations evoked by 5-hydroxytryptamine (5-HT). Responses of populations of motoneurones were recorded via a ventral root. 5-Hydroxytryptamine depolarizations were not Ca-dependent but were enhanced in amplitude in Ca-free solutions. Raised Mg reversed this enhancement. 5-Hydroxytryptamine depolarizations persisted in the presence of Mn (1.5-3 mmol/l). TRH depolarized motoneurones; there was no evidence of modulation of 5-HT responses on concurrent application of TRH. Ritanserin (0.1 mumol/l) had a modest blocking action on 5-hydroxytryptamine depolarizations reducing the maximum; 1 mumol/l ritanserin caused a greater antagonism which was unsurmountable (pIC50 5.2). Ritanserin (0.1 or 1 mumol/l) did not depress responses to noradrenaline (NA). Ketanserin (0.1 mumol/l) caused a blockade of slow onset, equilibrium with the receptors requiring 1 h. Blockade by 0.01, 0.1 and 1 mumol/l ketanserin was concentration-dependent (pIC50 6.2). Ketanserin 1 mumol/l, but not at lower concentrations, depressed noradrenaline responses. Mianserin (0.1 mumol/l) also caused a blockade of slow onset; 0.1 or 1 mumol/l produced a flattening of the 5-hydroxytryptamine concentration-response curve but did not depress noradrenaline responses (pIC50 4.7). The pIC50 for spiperone was 8.0. DOI (10-100 mumol/l) had no detectable agonist action but at concentrations of 0.01 and 0.1 mumol/l it acted as an antagonist. Equilibration with the receptors occurred over 2 h. DOI (0.01 mumol/l) depressed 5-hydroxytryptamine but not noradrenaline responses; higher concentrations of DOI also depressed noradrenaline responses.(ABSTRACT TRUNCATED AT 250 WORDS)
利用新生大鼠的半切脊髓,测试了细胞外钙改变、促甲状腺激素释放激素(TRH)及多种拮抗剂对5-羟色胺(5-HT)诱发的去极化的影响。通过腹根记录运动神经元群的反应。5-羟色胺去极化不依赖于钙,但在无钙溶液中其幅度增强。镁离子浓度升高可逆转这种增强作用。在锰离子(1.5 - 3 mmol/L)存在的情况下,5-羟色胺去极化依然存在。TRH使运动神经元去极化;同时应用TRH时,没有证据表明其对5-羟色胺反应有调节作用。利坦色林(0.1 μmol/L)对5-羟色胺去极化有适度的阻断作用,降低了最大值;1 μmol/L利坦色林引起更大的拮抗作用,且不可克服(pIC50为5.2)。利坦色林(0.1或1 μmol/L)不抑制对去甲肾上腺素(NA)的反应。酮色林(0.1 μmol/L)引起缓慢起效的阻断作用,与受体达到平衡需要1小时。0.01、0.1和1 μmol/L酮色林的阻断作用呈浓度依赖性(pIC50为6.2)。1 μmol/L酮色林可抑制去甲肾上腺素反应,但较低浓度时无此作用。米安色林(0.1 μmol/L)也引起缓慢起效的阻断作用;0.1或1 μmol/L使5-羟色胺浓度-反应曲线变平,但不抑制去甲肾上腺素反应(pIC50为4.7)。螺哌隆的pIC50为8.0。DOI(10 - 100 μmol/L)未检测到激动剂作用,但在0.01和0.1 μmol/L浓度时作为拮抗剂起作用。与受体达到平衡需要2小时。DOI(0.01 μmol/L)抑制5-羟色胺反应,但不抑制去甲肾上腺素反应;更高浓度的DOI也抑制去甲肾上腺素反应。(摘要截选至250字)