作者: M. Manning , A. Misicka , A. Olma , K. Bankowski , S. Stoev
DOI: 10.1111/J.1365-2826.2012.02303.X
关键词:
摘要: We recently reviewed the status of peptide and nonpeptide agonists antagonists for V1a, V1b V2 receptors arginine vasopressin (AVP) oxytocin receptor (OT). In present review, we update peptides nonpeptides as: (i) research tools (ii) therapeutic agents. also our recent findings on design fluorescent ligands localisation OT dimerisation. note exciting discoveries regarding two novel naturally occurring analogues OT. Recent reports a selective VP V1a agonist point to continued potential in this field. To date, only nonpeptides, V2/V1a antagonist, conivaptan antagonist tolvaptan have received Food Drug Administration approval clinical use. The development AVP has been abandoned by Merck, Sanofi Pfizer. A promising Retosiban, developed at Glaxo SmithKline is currently Phase II trial prevention premature labour. number that were not successful trials are proving be valuable as tools. Peptide continue very widely used regard, data some most ligands, guide their use, especially with regard selectivity species differences.