Abstract:
:In this study, we described the synthesis and some pharmacological properties of four new analogues of arginine vasopressin (AVP). Two peptides are substituted in position 2 with L-1-naphthylalanine (L-1-Nal) or its D-enantiomer and in position 4 with valine. In the further two compounds, we combined the above modifications with placement into position 1 of 3-mercaptopropionic acid residue (Mpa). All new peptides were tested for vasopressor and antidiuretic activities. We also estimated the uterotonic activities of these compounds in vitro. Urine samples prior and after peptide administration were analyzed for electrolytes excretion. All analogues are potent oxytocin antagonists. One of them, namely [L-1-Nal2,Val4]AVP, which appears practically not to interact with V1a and V2 receptors, is exceptionally selective. Our results open new possibilities for the design of very potent and selective oxytocin antagonists in vitro.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Derdowska I,Prahl A,Kowalczyk W,Janecki M,Melhem S,Trzeciak HI,Lammek Bdoi
10.1016/j.ejmech.2004.09.011subject
Has Abstractpub_date
2005-01-01 00:00:00pages
63-8issue
1eissn
0223-5234issn
1768-3254pii
S0223-5234(04)00195-3journal_volume
40pub_type
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