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  • Title: Synthesis and some pharmacological properties of [4-threonine,7-sarcosine]oxytocin, a peptide with high oxytocic potency, and of [4-threonine,7-N-methylalanine]oxytocin.
    Author: Grzonka Z, Lammek B, Gazis D, Schwartz IL.
    Journal: J Med Chem; 1983 Dec; 26(12):1786-7. PubMed ID: 6685771.
    Abstract:
    Two analogues of oxytocin, [Thr4,Sar7]- and [Thr4,MeAla7]oxytocin, were synthesized and their pharmacological properties investigated. [Thr4,Sar7]oxytocin was found to exhibit high biological activity (uterotonic activity of 1174 +/- 104 and milk ejection activity of 731 +/- 57 units/mg) and high selectivity for oxytocin-like relative to vasopressin-like activities (antidiuretic activity of 0.037 +/- 0.012 unit/mg, undetectable pressor activity). [Thr4,MeAla7]oxytocin was characterized by markedly lower biological activities. In both analogues, the additivity of the effects of the residues in positions 4 and 7 of oxytocin on the biological activity of the analogues was ascertained.
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