Aminopyridines and synaptic transmission

Aminopyridines and synaptic transmission
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氨基吡啶和突触传递

DOI:
10.1016/0306-4522(80)90002-0
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发表时间:
1980
期刊:
影响因子:
3.3
通讯作者:
Stephen Thesleff
Stephen Thesleff
中科院分区:
医学3区
文献类型:
--
作者:
Stephen Thesleff

文献摘要

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Aminopyridines are compounds with a novel, unique and rather selective mode of action on the processes responsible for transmitter release at chemical synapses. The drugs are therefore of considerable interest to investigators of synaptic transmission. The aminopyridines(2-, 3-and 4-aminopyridines; AP) and the diaminopyridines(2, 3,-, 2, 6-and 3, 4-diaminopyridines; DAP) have long been known to stimulate the central nervous system, to elevate blood pressure and to exert an anti-curare action, 4-AP and 3, 4-DAP being particularly active, both effective in PM-concentrations. These actions on the nervous system result from effects on the processes responsible for nerve impulse-evoked transmitter release, the amount of transmitter liberated by each nerve impulse being enormously increased by the drugs. 4-Aminopyridines and 3, 4-diaminopyridines are blockers of the potassium channel in excitable tissue and this action might explain their selective effect on transmitter release evoked by action potentials, resting release being almost unaffected by the drugs. Another blocker of the potassium channel is tetraethylammonium which augments evoked transmitter release. However, it is less potent, acting in mM concentrations. Furthermore, tetraethylammonium is not as selective in its mode of action since it also is a potent blocker of nicotinic cholinergic receptors.