New proctolin analogues and their myotropic effects on heart of yellow mealworm Tenebrio molitor L. and foregut of locust - Schistocerca gregaria L.

Mariola Kuczer*, Grzegorz Rosiński, Jonathan Issberner, Richard Osborne, Danuta Konopińska

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

Abstract

We have extended our work on structure/activity relationship of neuropeptide proctolin (H-Arg-Tyr-Leu-Pro-Thr-OH) by evaluating the effects of the following proctolin analogues: H-X1-Tyr-Leu-Pro-Thr-OH, where X1 - D-Arg (1), N-Me-Arg (2), Can (3), D, Tyr2, D-Leu3, D-Thr5]-proctolin (12). In analogues 1-9, the N-terminal Arg-residue was replaced by basic amino acid derivatives with peptides containing amino acid residue was replaced by basic amino acid derivatives with peptides containing amino acid residues with an isosteric system on the back side chain relative to Arg (compounds 3, 5 and 6) or homo-Arg (compound 7). Analogues 1-12 were evaluated for myotropic action on in vitro heart preparation of Tenebrio molitor, whereas peptides 2, 5 and 7-12 were tested for contractile action on isolated foregut of Schistocerca gregaria. Peptides 2 and 3 retained full cardiotropic activity in Tenebrio molitor while peptides 5 and 7 preserved 40% and 15%, respectively, locust-gut contracting activity of proctolin. Peptides 11 and 12 showed antagonistic activity in Schistocerca gregaria foregut.

Original languageEnglish
Pages (from-to)143-150
Number of pages8
JournalPolish Journal of Pharmacology
Volume50
Issue number2
Publication statusPublished - 1 Jan 1998

Keywords

  • Insect neuropeptide proctolin
  • Myotropic effects in insects
  • Proctolin and its analogues
  • Synthesis of proctolin analogues

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