Synthesis and biological evaluation of oxytocin analogues containing L-alpha-t-butylglycine [Gly(Bu t)] in positions 8 or 9 |
| |
Authors: | Fragiadaki Maria Magafa Vassiliki Slaninová Jirina Cordopatis Paul |
| |
Institution: | Department of Pharmacy, Laboratory of Pharmacognosy and Chemistry of Natural Products, University of Patras, GR-26500 Patras, Greece. |
| |
Abstract: | We report the solid phase synthesis and some pharmacological properties of seventeen new oxytocin (OT) analogues. Basic modification at positions 8 and/or 9 (introduction of L-alpha-t-butylglycine Gly(Bu(t))]) was combined with D-Cys(6), D-Tyr(Et)(2), Mpa(1) or Pen(1) modifications and their various combinations. We also present properties of two previously reported re-synthesized analogues (Gly(Bu(t))(8)]OT and Mpa(1), Gly(Bu(t))(8)]OT). The analogues were tested for rat uterotonic activity in vitro, in the rat pressor assay and for binding affinity to human OTR. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|