Analogs of neurohypophysial hormones

摘要

Analogs of neurohypophysial hormones with inhibition properties are described. The hormones are of the formula wherein in all chiral amino acids are of the L-series and the aromatic amino acid in the position 2, indicated with an asterisk, is of the D-series, and where R1 and R2 are hydrogen or a methyl group, R3 is hydrogen, an amino group, or a triglycylamine grouping, R4 is hydrogen, a methyl, ethyl or ethoxy group, R5 is S-CH2 or S-S group, X1 is a residue of isoleucine or phenylalanine, X2 is a residue of leucine or lysine, and X3 is a glycinamide residue or a hydroxyl group. These compounds exhibit inhibition effects towards the uterotonic and pressor activity of natural hormones. The common structural feature of all these analogues is the presence of an aromatic hydrophobic D-amino acid in the position 2.