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Title: A NONPEPTIDE AGONIST OF THE INVERTEBRATE SCHISTOFLRFAMIDE RECEPTOR

Author
item LANGE, ANGELA - UNIVERSITY OF TORONTO
item ORCHARD, IAN - UNIVERSITY OF TORONTO
item WANG, ZHIXANG - UNIVERSITY OF TORONTO
item Nachman, Ronald

Submitted to: Proceedings of the National Academy of Sciences (PNAS)
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: 8/5/1995
Publication Date: N/A
Citation: N/A

Interpretive Summary: Because of the problems with the development of resistance to conventional chemical control procedures for many major pest species, there is a critical need for new concepts and alternative approaches in controlling such pests. The basic premise of this research is that peptides serve as internal messengers in insects to regulate vital functions. Peptides themselves are unsuitable for control measures due to their instability to insect digestive enzymes and environmental factors. New, selective control measures may be developed by designing and/or discovering chemicals that actively inhibit or stimulate peptide regulated functions, resulting in disruption of the internal environment of the insect. We describe the first nonpeptide analog of a insect neuropeptide family. In this report, we show that the nonpeptide interacts with the same site of action, or "receptor," as the insect myosuppressin peptides. This family of peptides are potent inhibitors of heart and digestive tract muscles, and in additio to having effects on skeletal muscle, longitudinal flight muscles, and salivary glands. This milestone discovery provides a unique opportunity to finally target an insect neuropeptide system for the development of future pest management strategies.

Technical Abstract: The first nonpeptide mimetic analog of an invertebrate peptide receptor is described. Benzethonium chloride (Bztc) is an agonist of the SchistoFLRFamide (PDVDHVFLRFamide) receptors found on locust oviducts. Bztc competitively displaces [**125I-Y**1]SchistoFLRFamide ([**125I- Y**1]DVDHVFLRFamide) binding to both high and low affinity receptors of membrane preparations. Bztc mimics the physiological effects of SchistoFLRFamide on locust oviduct, 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.