Analogues of 8-d-homoarginine vasopressin

Details Analogues of 8-d-homoarginine vasopressin Analogues of 8-d-homoarginine vasopressin

C - Chemistry, Metallurgy

07

K

530/7.06, 530/7.

C07K 7/16 (2006.01)

Patent

CA 2022865

Report of the invention Analogues of 8-D-homoarginine vasopressin Using a step-wise synthesis on solid phase, analogues of 8-D-homoarginine va- sopressin were prepared with the general formula Image , 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.

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