Selective stimulation of insulin secretion by CCK-4 analogues having N-terminal modifications.
Synthetic analogues of CCK-4 in which Trp was replaced by D-Pro (peptide I), Thz (peptide II) and delta Pro (peptide III) have been studied for their insulin and glucagon releasing activities from the islets of Langerhans in vitro. Peptide I has been found to be the most potent insulin releaser among the three analogues and its activity is comparable to that of CCK-4. Unlike CCK-4, its three analogues (peptides I-III) do not stimulate the release of glucagon with basal concentration of glucose in the medium. However, with increasing glucose concentration, all the three analogues potentiate the glucose stimulus for insulin release.
Ahmad
F
F
Division of Biochemistry, Central Drug Research Institute, Lucknow, India.
Kundu
B
B
Khan
M M
MM
Rastogi
A K
AK
Mathur
K B
KB
Kidwai
J R
JR
D000818:Animals; D005934:Glucagon / Q000378:metabolism; D005947:Glucose / Q000494:pharmacology; D066298:In Vitro Techniques; D007328:Insulin / Q000378:metabolism*; D000078790:Insulin Secretion; D007515:Islets of Langerhans / Q000187:drug effects / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D012844:Sincalide / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013758:Tetragastrin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*
D007328:Insulin; D013758:Tetragastrin; D005934:Glucagon; D005947:Glucose; D012844:Sincalide