The Administrators of the Tulane Educational Fund;Department of Veterans Affairs (US)
发明人:
James E. ZADINA,Laszlo HACKLER
申请号：
US15450259
公开号：
US20170369531A1
申请日:
2017.03.06
申请国别(地区):
US
年份:
2017
代理人:
摘要：
The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic pentapeptide and hexapeptide analogs of endomorphin that have (i) a carboxy-terminal extension with an amidated hydrophilic amino acid and (ii) a substitution in amino acid position 2, and in some embodiments, a 2′,6′-dimethyltyrosine (Dmt) residue in place of the N-terminal tyrosine residue a position 1. These peptide analogs exhibit increased solubility compared to similar tetrapeptide analogs while maintaining favorable or improved therapeutic ratios of analgesia to side effects.
