A nonpeptide agonist of the invertebrate receptor for SchistoFLRFamide (PDVDHVFLRFamide), a member of a subfamily of insect FMRFamide-related peptides

Proc Natl Acad Sci U S A. 1995 Sep 26;92(20):9250-3. doi: 10.1073/pnas.92.20.9250.

Abstract

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.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Benzethonium / pharmacology*
  • Binding, Competitive
  • FMRFamide
  • Female
  • Grasshoppers / physiology*
  • Insect Hormones / metabolism
  • Kinetics
  • Molecular Sequence Data
  • Muscle Contraction / drug effects
  • Muscle, Smooth / drug effects
  • Muscle, Smooth / physiology
  • Neuropeptides / metabolism*
  • Oviducts / drug effects
  • Oviducts / physiology
  • Receptors, Peptide / agonists*
  • Sequence Homology, Amino Acid

Substances

  • Insect Hormones
  • Neuropeptides
  • Receptors, Peptide
  • SchistoFLRFamide receptor
  • SchistoFLRFamide
  • Benzethonium
  • FMRFamide