Lange A B, Orchard I, Wang Z, Nachman R J
Department of Zoology, University of Toronto, ON, Canada.
Proc Natl Acad Sci U S A. 1995 Sep 26;92(20):9250-3. doi: 10.1073/pnas.92.20.9250.
We describe a nonpeptide mimetic analog of an invertebrate peptide receptor. Benzethonium chloride (Bztc) is an agonist of the SchistoFLRFamide (PDVDHVFLRFamide) receptors found on locust oviducts. Bztc competitively displaces [125I-labeled Y1]SchistoFLRFamide binding to both high- and low-affinity receptors of membrane preparations. Bztc mimics the physiological effects of SchistoFLRFamide on locust oviduct, by inhibiting myogenic and induced contractions in a dose-dependent manner. Bztc is therefore recognized by the binding and activation regions of the SchistoFLRFamide receptors. This discovery provides a unique opportunity within insects to finally target a peptide receptor for the development of future pest management strategies.
我们描述了一种无脊椎动物肽受体的非肽模拟类似物。苄索氯铵（Bztc）是在蝗虫输卵管上发现的血吸虫FLRF酰胺（PDVDHVFLRF酰胺）受体的激动剂。Bztc竞争性地取代[125I标记的Y1]血吸虫FLRF酰胺与膜制剂的高亲和力和低亲和力受体结合。Bztc通过以剂量依赖的方式抑制肌源性和诱导的收缩，模拟了血吸虫FLRF酰胺对蝗虫输卵管的生理作用。因此，Bztc被血吸虫FLRF酰胺受体的结合和激活区域所识别。这一发现为昆虫体内最终靶向肽受体以制定未来害虫管理策略提供了独特的机会。
