Kirpekar S M, Garcia A G, Prat J C
J Pharmacol Exp Ther. 1980 Apr;213(1):133-8.
Interaction between 4-aminophrydine (4-AP) and nicotine on sympathetic nerve terminals was studied in the isolated cat spleen slices, labeled with [3H]norepinephrine ([3H]NE). Incubation of slices for 5 min at 37 degrees C in low (50 microM) and high (2 mM) concentrations of nicotine released 0.8 +/- 0.08 and 2.73 +/- 0.39% of tissue [3H]NE. Tetrodotoxin (TTX) blocked the response to low nicotine but not to high nicotine. Low nicotine did not release [3H]NE in the absence of calcium. Response to high nicotine which persisted in calcium-free solution was blocked by ethylene glycol bis(beta-aminoethyl ether)N,N'-tetra-acetic acid. 4-AP (1 mM) not only enhanced the response to low nicotine but it effectively antagonized the suppressant effects of TTX and calcium-free solution on release induced by low nitotine. Restoration of release by 4-AP from TTX-blocked preparations occurred in the absence of calcium in the perfusion medium, but lanthanum (1 mM) blocked it. Restoration of release from spleen slices incubated in calcium-free Krebs' solution by 4-AP was blocked by lanthanum and prolonged incubation in calcium-free ethylene glycol bis(beta-aminoethyl ether)N,N'-tetraaectic acid solution. It is concluded that at lower doses nicotine, by acting on nicotinic receptors, depolarizes the sympathetic nerve terminals to set off propagated action potentials which are responsible for NE release, and that 4-AP restores nicotine response in the presence of TTX or in the absence of calcium by mobilizing calcium both from extracellular and intracellular sources.
在标记有[3H]去甲肾上腺素([3H]NE)的离体猫脾脏切片中,研究了4-氨基吡啶(4-AP)与尼古丁对交感神经末梢的相互作用。将切片在37℃下于低浓度(50μM)和高浓度(2mM)尼古丁中孵育5分钟,分别释放出组织中0.8±0.08%和2.73±0.39%的[3H]NE。河豚毒素(TTX)阻断了对低浓度尼古丁的反应,但未阻断对高浓度尼古丁的反应。在无钙情况下,低浓度尼古丁不释放[3H]NE。在无钙溶液中持续存在的对高浓度尼古丁的反应被乙二醇双(β-氨基乙醚)N,N'-四乙酸阻断。4-AP(1mM)不仅增强了对低浓度尼古丁的反应,而且有效拮抗了TTX和无钙溶液对低浓度尼古丁诱导释放的抑制作用。在灌注介质中无钙的情况下,4-AP能使TTX阻断的制剂恢复释放,但镧(1mM)可阻断此作用。4-AP使在无钙Krebs溶液中孵育的脾脏切片恢复释放的作用被镧阻断,且在无钙乙二醇双(β-氨基乙醚)N,N'-四乙酸溶液中长时间孵育也可阻断此作用。结论是,低剂量尼古丁通过作用于烟碱受体使交感神经末梢去极化,引发负责NE释放的传播性动作电位,并且4-AP通过从细胞外和细胞内来源动员钙,在存在TTX或无钙的情况下恢复尼古丁反应。