| 摘要 |
<p>The cyclic peptide (Phe2-Orn8-oxytocin) <PICT:1067935/C2/1> and its acid addition salts are prepared by oxidizing the linear peptide <PICT:1067935/C2/2> (and, if desired, salifying the product), the linear peptide being prepared from its N- and S-protected derivative by removal of the protecting groups. CBO - Cys(Bz) - Phe - Ile - Glu(NH2) - Asp-(NH2) - Cys(Bz) - Pro - Orn(Tos) - GlyNH2 is prepared through the following intermediates: CBO - Orn(Tos) - GlyOEt, CBO - Pro - Orn(Tos)-GlyNA2 and CBO - Glu(NH2) - Asp(NH2)-Cys(Bz) - Pro - Orn(Tos) - Gly - NH2 (where CBO is carbobenzyloxy, Bz is benzyl and Tos is tosyl).ALSO:Pharmaceutical compositions comprise Phe2-Orn8-oxytocin of the formula <FORM:1067935/A5-A6/1> or their acid addition salts and a carrier therefor, optionally with the addition of a local anaesthetic. The peptide shows high local vaso constructive activity. Examples are given of solutions for infiltration, block and surface anaesthesia.</p> |
