TY - JOUR
T1 - Further proctolin analogues modified in the position 2 of the peptide chain and their myotropic effects in insects Tenebrio molitor and Schistocerca gregaria
AU - Kuczer, Mariola
AU - Rosiński, Grzegorz
AU - Issberner, Jonathan
AU - Osborne, Richard
AU - Konopińska, Danuta
PY - 1999/4/7
Y1 - 1999/4/7
N2 - We have extended our studies on the structure-activity relationship in neuropeptide proctolin (Arg-Tyr-Leu-Pro-Thr) by evaluating the effects of a series of proctolin analogues modified in position 2 of the peptide chain, including: [Phe(p-Cl)2]-(1), [D-Phe(p-Cl)2]-(2), [N-Me-Tyr2]-(3), [D-Phe(p-NH2)2]-(4), [D-Phe(p-N,N-di-Me)2]-(5), [N-Me-Tyr(OMe)]-(6), [D-3-Pal2]-(7), [L-Nal2]-(8), [D-Nal2]-(9), [Lys(Nic)2]-(10), [D-Lys(Nic)2]-(11), [D-Phe-(p-NO2)2]-(12). These peptides were evaluated for myotropic activity on the heart of Tenebrio molitor and contractile activity of the foregut of Schistocerca gregaria. Analogues 1-5, 7-9, and 12 retained a weak cardiotropic activity in Tenebrio molitor while peptides 1, 8 and 12 preserved 15-25% of the locust-gut contracting activity of proctolin. Peptides 2, 4 and 7 showed weak inhibitory activity in Schistocerca gregaria foregut, whereas only peptides 2, 4 and 7 reduced the maximum response to appllied proctolin by 64% and 49% respectively, at the 10-6 M concentration.
AB - We have extended our studies on the structure-activity relationship in neuropeptide proctolin (Arg-Tyr-Leu-Pro-Thr) by evaluating the effects of a series of proctolin analogues modified in position 2 of the peptide chain, including: [Phe(p-Cl)2]-(1), [D-Phe(p-Cl)2]-(2), [N-Me-Tyr2]-(3), [D-Phe(p-NH2)2]-(4), [D-Phe(p-N,N-di-Me)2]-(5), [N-Me-Tyr(OMe)]-(6), [D-3-Pal2]-(7), [L-Nal2]-(8), [D-Nal2]-(9), [Lys(Nic)2]-(10), [D-Lys(Nic)2]-(11), [D-Phe-(p-NO2)2]-(12). These peptides were evaluated for myotropic activity on the heart of Tenebrio molitor and contractile activity of the foregut of Schistocerca gregaria. Analogues 1-5, 7-9, and 12 retained a weak cardiotropic activity in Tenebrio molitor while peptides 1, 8 and 12 preserved 15-25% of the locust-gut contracting activity of proctolin. Peptides 2, 4 and 7 showed weak inhibitory activity in Schistocerca gregaria foregut, whereas only peptides 2, 4 and 7 reduced the maximum response to appllied proctolin by 64% and 49% respectively, at the 10-6 M concentration.
KW - Agonists and antagonists of proctolin
KW - Insect neuropeptide proctolin and analogues
KW - Myotropic effect in insects
KW - Proctolin analogues
UR - http://www.scopus.com/inward/record.url?scp=0344938216&partnerID=8YFLogxK
M3 - Article
C2 - 10389148
AN - SCOPUS:0344938216
SN - 1230-6002
VL - 51
SP - 79
EP - 85
JO - Polish Journal of Pharmacology
JF - Polish Journal of Pharmacology
IS - 1
ER -