Epinastine, a highly specific antagonist of insect neuronal octopamine receptors
Epinastine, a highly specific antagonist of insect neuronal octopamine receptors
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DOI：
10.1016/s0014-2999(98)00192-7
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发表时间：
1998-05-22
影响因子：
5
通讯作者：
Gewecke, M
中科院分区：
文献类型：
--
作者：
Roeder, T;Degen, J;Gewecke, M
四环化合物依匹斯汀（3-氨基-9，13 b-二氢-1H-二苯并（c，f）咪唑并（1，5a）氮杂卓盐酸盐）最近作为脊椎动物组胺H1受体拮抗剂引入，其对昆虫神经元章鱼胺受体也具有高亲和力。这对于来自蝗虫（Ki = 2Nm）以及来自蜜蜂神经系统（Ki = 1.1Nm）的神经元章鱼胺受体同样适用。除了高亲和力外，它还具有高度的特异性。它对其他昆虫生物胺受体的亲和力，如5-羟色胺，多巴胺，组胺和酪胺，至少低四个数量级。因此，依匹斯汀可以作为一种高度特异性的章鱼胺受体拮抗剂，使昆虫神经系统内的章鱼胺能神经传递的生理解剖。为了证明这些能力，使用依匹斯汀来抑制视觉通路中已鉴定的中间神经元的视觉诱发活性，已知该中间神经元由章鱼胺调节。(C)1998 Elsevier Science B. V.保留所有权利。
The tetracyclic compound epinastine (3-amino-9, 13b-dihydro-1H-dibenz(c,f)imidazo(l,5a)azepine hydrochloride) that was recently introduced as a vertebrate histamine H, receptor antagonist has also high affinity for insect neuronal octopamine receptors. This holds true for the neuronal octopamine receptor from the locust (K-i = 2 Nm) as well as from the honey bee nervous system (K-i = 1.1 Nm). In addition to its high affinity, it has a high degree of specificity. Its affinity for other insect receptors for biogenic amines, such as 5-hydroxytryptamine, dopamine, histamine, and tyramine, is at least four orders of magnitude lower. Therefore, epinastine could serve as a highly specific antagonist of octopamine receptors that enables physiological dissection of octopaminergic neurotransmission within the nervous system of insects. To demonstrate these abilities, epinastine was used to inhibit the visually evoked activity of an identified interneuron in the visual pathway which is known to be modulated by octopamine. (C) 1998 Elsevier Science B.V. All rights reserved.