The Administrators of The Tulane Educational Fund;United States Department Of Veterans Affairs
发明人:
Zadina, James E.,Hackler, Laszlo
申请号：
HRP20171119
公开号：
HRP20171119T1
申请日:
2017.07.20
申请国别(地区):
HR
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. These peptide analogs exhibit increased solubility compared to similar tetrapeptide analogs while maintaining favorable or improved therapeutic ratios of analgesia to side effects.
