European Journal of Medicinal Chemistry p. 115 - 122 (1995)
Update date:2022-08-30
Topics:
Thurieau
Janiak
Krantic
Guyard
Pillon
Kucharczyk
Vilaine
Fauchere
We report on the synthesis and pharmacological properties of a new series of somatostatin analogs. Two lower homologs of lysine, 2,3-diaminopropanoic acid and 2,4-diaminobutyric acid, were prepared and used for cyclization via amide formation with the side chain of aspartic or glutamic acid in place of natural cystine present in many somatostatin analogs. One resulting compound, although having low binding affinities for somatostatin receptors, displayed a strong potency in inhibiting neointima formation induced by balloon injury in rats at the dose of 100 μg·kg-1·d-1. This dissociation of the antiproliferative effect from the endocrine effect seems to indicate that myointimal growth is not related to a change in growth hormone secretion.
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