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

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.