Nonapeptides synthesis from pentapeptides - having neurohypophysal hormone and natriuretic activity

摘要

Cpds. of gen. formula (I): where Q = arginine or lysine residue; Mpr = beta-mercaptopropionyl; all amino acids with asymmetric C-atom have L-configuration; including pharmaceutically-acceptable, non-toxic acid-addn. salts of (I); are prepd. by e.g. removing protecting gps. of a cpd. (III): (where R1 = H or an amido-protecting gp. Q1 = NH-CH/-(CH2)3-NH-C(=NH-NHR2/-CO or -NH-CH/-(CH2)4-NHR3/-CO-; R2 = H or a guanidino-protecting gp; R3 = H or an -amino gp. of lysine-protecting gp). (I) have hormonal activity qualitatively equal to that of neurohypophysal hormones. They have esp. natriuretic act. and may be used in the treatment of all types of oedema and general disturbance of the electrolyte metabolism, esp. sodium retention. (I) are more active and are longer lasting in activity than natural (IIe3)-argininvasopressine or known (Leu4) oxytocine, with less hypertensive activity.