Journal of Medicinal Chemistry p. 1828 - 1832 (1990)
Update date:2022-08-03
Topics:
Johnson, Rodney L.
Bontems, Roger J.
Yang, Kaipeen E.
Mishra, Ram K.
A series of analogues of Pro-Leu-Gly-NH2 (PLG) in which the leucine residue has been replaced with the aliphatic amino acids L-isoleucine, L-2-aminohexanoic acid (Ahx), L-2-aminopentanoic acid, and L-2-aminobutanoic acid and the aromatic amino acids L-phenylalanine, L-phenylglycine, L- and D-2-amino-4-phenylbutanoic acid, L-O-methyltyrosine, and L-4-nitrophenylalanine have been synthesized.These analogues were tested for their ability to enhance the binding of the dopamine receptor agonist 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (ADTN) to striatal dopamine receptors.Two of the abov e analogues, Pro-Ahx-Gly-NH2 (3) and Pro-Phe-Gly-NH2 (6), showed significant activity in this assay system.Pro-Ahx-Gly-NH2 produced a 16percent enhancement of ADTN binding at 0.1 μM, while Pro-Phe-Gly-NH2 enhanced the binding of ADTN by 31percent at a concentration of 1 μM.
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