A nonpeptide agonist of the invertebrate receptor for SchistoFLRFamide (PDVDHVFLRFamide), a member of a subfamily of insect FMRFamide-related peptides.
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.
Lange
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AB
Department of Zoology, University of Toronto, ON, Canada.
Orchard
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I
Wang
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Z
Nachman
R J
RJ
D000595:Amino Acid Sequence; D000818:Animals; D001558:Benzethonium / Q000494:pharmacology*; D001667:Binding, Competitive; D019835:FMRFamide; D005260:Female; D006110:Grasshoppers / Q000502:physiology*; D007301:Insect Hormones / Q000378:metabolism; D007700:Kinetics; D008969:Molecular Sequence Data; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D009479:Neuropeptides / Q000378:metabolism*; D010057:Oviducts / Q000187:drug effects / Q000502:physiology; D018000:Receptors, Peptide / Q000819:agonists*; D017386:Sequence Homology, Amino Acid
D007301:Insect Hormones; D009479:Neuropeptides; D018000:Receptors, Peptide; C095826:SchistoFLRFamide receptor; C059573:SchistoFLRFamide; D001558:Benzethonium; D019835:FMRFamide