Actions of the insecticide 2(nitromethylene)tetrahydro-1,3-thiazine on insect and vertebrate nicotinic acetylcholine receptors.
Actions of the insecticide 2(nitromethylene)tetrahydro-1,3-thiazine on insect and vertebrate nicotinic acetylcholine receptors.
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杀虫剂 2(硝基亚甲基)四氢-1,3-噻嗪对昆虫和脊椎动物烟碱乙酰胆碱受体的作用。
DOI：
10.1098/rspb.1989.0062
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发表时间：
1989
期刊：
影响因子：
--
通讯作者：
May,TE
中科院分区：
文献类型：
--
作者：
Sattelle,DB;Buckingham,SD;Wafford,KA;Sherby,SM;Bakry,NM;Eldefrawi,AT;Eldefrawi,ME;May,TE
硝基亚甲基杂环化合物2（nitromethylene）tetrahydro）1，3-thiazine（NMTHT）抑制[125 I] α-银环蛇毒素与蟑螂（Periplaneta americana）神经索膜和鱼（Torpedo californica）电器官膜的结合。电生理学研究表明，蟑螂的快速髋降压运动神经元（Df）的剂量依赖性去极化响应浴应用NMTHT。NMTHT对运动神经元Dfare细胞体膜的离子电渗作用的反应，受到浴用美卡拉明（1.0 x 10- 4 M）和α-银环蛇毒素（1.0 x 10- 7 M）的抑制。这些研究结果，再加上检测到的逆转电位接近估计的乙酰胆碱，提供了证据，这硝基亚甲基对昆虫神经元烟碱乙酰胆碱受体的激动剂作用。[~ 3 H] H_（12）-组蛋白毒素与电鳐膜的结合在NMTHT存在下增强，表明其对脊椎动物外周烟碱乙酰胆碱受体有激动作用。NMTHT在大鼠脑GABA A受体、大鼠脑L-谷氨酸受体和昆虫（家蝇）L-谷氨酸受体的放射性配体结合试验中无效。在毫摩尔浓度的NMTHT下检测到大鼠脑毒蕈碱乙酰胆碱受体的部分阻断。因此，硝基亚甲基似乎表现出对乙酰胆碱受体的选择性和对烟碱乙酰胆碱受体的阿比坦激动剂作用。
The nitromethylene heterocyclic compound 2(nitromethylene)tetrahydro) 1, 3-thiazine (NMTHT) inhibits the binding of [125I)α-bungarotoxin to membranes prepared from cockroach (Periplaneta americana) nerve cord and fish (Torpedo californica) electric organ. Electrophysiological studies on the cockroach fast coxal depressor motorneuron (Df) reveal a dose-dependent depolarization in response to bath-applied NMTHT. Responses to ionophoretic application of NMTHT on to the cell-body membrane of motorneuron Dfare suppressed by bath-applied mecamylamine (1.0 x 10-4M) andα-bungarotoxin (1.0 x 10-7M). These findings, together with the detection of a reversal potential close to that estimated for acetylcholine, provide evidence for an agonist action of this nitromethylene on an insect neuronal nicotinic acetylcholine receptor. The binding of [3H]H12-histrionicotoxin toTorpedomembranes was enhanced in the presence of NMTHT indicating an agonist action at this vertebrate peripheral nicotinic acetylcholine receptor. NMTHT is ineffective in radioligand binding assays for rat brain GABAAreceptors, rat brain L-glutamate receptors and insect (Musca domestica) L-glutamate receptors. Partial block of rat brain muscarinic acetylcholine receptors is detected at millimolar concentrations of NMTHT. Thus nitromethylenes appear to exhibit selectivity for acetylcholine receptors and exhibitan agonist action at nicotinic acetylcholine receptors.