Diuretic activity of C-terminal group analogues of the insect kinins in Acheta domesticus

Peptides. 1995;16(5):809-13. doi: 10.1016/0196-9781(95)00047-n.


A series of insect kinin analogues, AFFPWG-X, modified at the C-terminal group, were evaluated in a cricket Malpighian tubule secretion bioassay. The results were compared with activity profiles observed in a cockroach hindgut myotropic bioassay for these analogues. Although the replacement of the C-terminal amide group with a negatively charged acid leads to a precipitious drop in diuretic activity, it can be partially restored with the introduction of ester groups such as methyl or benzyl. The presence of branched chain character in the C-terminal group or a C-terminal alpha-carbon-amide distance spanning five methylene group spacers is incompatible with the receptor interaction required for biological activity. Significant diuretic activity is retained with four or fewer methylene groups in this region. C-terminal group analogues containing -SCH3, -NHCH2CH2OCH3, or -OCH2(C6H5) offered the greatest retention of diuretic activity while providing increased hydrophobicity and/or steric bulk. The data are of potential value in the development of mimetic analogues of this insect neuropeptide family. Mimetic analogues are potentially valuable tools to insect neuroendocrinologists studying diuresis and/or engaged in the development of future pest management strategies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Digestive System / drug effects
  • Digestive System Physiological Phenomena
  • Diuretics / chemistry
  • Diuretics / pharmacology*
  • Grasshoppers
  • Gryllidae
  • In Vitro Techniques
  • Insect Hormones / chemistry*
  • Insect Hormones / pharmacology*
  • Kinins / chemistry*
  • Kinins / pharmacology*
  • Malpighian Tubules / drug effects
  • Malpighian Tubules / metabolism
  • Molecular Sequence Data
  • Muscle Contraction / drug effects
  • Peptide Fragments / chemistry
  • Peptide Fragments / pharmacology
  • Structure-Activity Relationship


  • Diuretics
  • Insect Hormones
  • Kinins
  • Peptide Fragments