Copyright © 1998 by Institute of Pharmacology
Polish Academy of Sciences 		Pol. J. Pharmacol., 1998, 50, 143-150
ISSN 1230-6002
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NEW PROCTOLIN ANALOGUES AND THEIR MYOTROPIC EFFECTS ON HEART OF YELLOW MEALWORM TENEBRIO MOLITOR L. AND FOREGUT OF LOCUST - SCHISTOCERCA GREGARIA L.
 Mariola Kuczer1, Grzegorz Rosiński2, Jonathan Issberner3, Richard Osborne3, Danuta Konopińska1#
 1 Faculty of Chemistry, University of Wroc³aw, F. Joliot-Curie 14, PL 50-383 Wroc³aw, Poland,
2 Department of Animal Physiology, A. Mickiewicz University, Fredry 10, PL 61-701 Poznań, Poland,
3 Department of Biology, University of the West of England, Bristol, UK

New proctolin analogues and their myotropic effects on heart of yellow mealworm Tenebrio molitor L. and foregut of locust - Schistocerca gregaria L. M. KUCZER, G. ROSIŃSKI, J. ISSBERNER, R. OSBORNE, D. KONOPIŃSKA. Pol. J. Pharmacol. 1998, 50, 143-150.

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 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.

Key words: insect neuropeptide proctolin, proctolin and its analogues, synthesis of proctolin analogues, myotropic effects in insects
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