| abstract |
Novel vasotocin derivatives having an inhibitory effect on uterine contractions, pharmaceutical compositions containing these derivatives, and the use thereof in the therapeutical treat- nent of excessive muscle contractions in the uterus are described. The derivatives differ from vasotocin in that the structure of the original hormone has been modified at positions 1, 2 and, optionally, 4 and/or 8. The vasotocin derivatives thus iave the formula whereinn Mpa is a 3-mercaptopropionyl residue (-S-CH 2 - CH 2 -CO-); A is the peptide residue of L- or D-tyrosine-O-ethyl ether (in other words, 4-ethoxy-L or D-phenyl alanine, i.e. L-or D-Tyr(Et)), or of a hydrophopic D-amino acid, such as D-tyrosine(D-Tyr) or D-tryptophane(D-Trp); Ile is the peptide residue of isoleucine; B is the peptide residue of glutamine (Gin), treonine (Thr) or valine (Val); Asn is the peptide residue of asparagin; Cys is the peptide residue of cysteine; Pro is the peptide residue of proline; C is the peptide residue of L- or D-arginine (Arg), ornithine (Orn) or citrullin (Cit); and Gly-NH 2 is the peptide residue of glycine amide. |