ANALOGUES OF 8-D-HOMOARGININE VASOPRESSIN

摘要

Report of the invention Analogues of 8-D-homoarginine vasopressin Using a step-wise synthesis on solid phase, analogues of 8-D-homoarginine vasopressin were prepared with the general formula , where X is L-O-methyltyrosine, L-p-ethylphenylalanine, D-p-ethylphenylalanine, L-p-methylphenylalanine or D-methylphenylalanine and R is cysteine or ?mercaptopropionic acid. These vasopressin analogues exhibited an increased affinity to uterus receptors for oxytocin where they acted as oxytocin antagonists. Moreover, the analogues of deamino vasopressin have a significantly reduced antidiuretic activity in comparison with ¢8-D-arginine!vasopressin.