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Stimulation of Insulin Secretion From Pancreatic Islets by the Cholecystokinin-Tetrapeptide Analogs Trp-Pro-Asp-Phe-NH2 and Trp-Pro-Asp-Phe(4'-NO2)-NH2

Stimulation of Insulin Secretion From Pancreatic Islets by the Cholecystokinin-Tetrapeptide Analogs Trp-Pro-Asp-Phe-NH2 and Trp-Pro-Asp-Phe(4'-NO2)-NH2

J J Knittel, B Hafner, D G Patel, E J Verspohl

Pept Res. Sep-Oct 1990;3(5):224-7.

PMID: 2134065

Abstract:

The cholecystokinin-tetrapeptide (CCK4) analogs Trp-Pro-Asp-Phe-NH2 (3) and Trp-Pro-Asp-Phe-(4'-NO2)-NH2 (4) were found to be nearly equipotent to cholecystokinin-octapeptide (CCK8) in potentiating glucose-induced insulin secretion from islets of Langerhans isolated from rat pancreas. This stimulatory action was found to be dose-dependent and, in the case of 4, to exhibit a biphasic dose-response curve; i.e., at concentrations greater than 1.0 nM, the stimulating effect of 4 is reversed. These results suggest that conformational restriction of CCK4 and/or modification of the phenylalanine residue could produce more potent analogs capable of stimulating insulin release. Such compounds could have potential therapeutic utility in the treatment of non-insulin-dependent diabetes mellitus (NIDDM).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
IAR4249422	2-Aminobenzoyl-Ala-Phe-Ala-Phe-Asp-Val-Phe-Tyr(NO2)-Asp			Price

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