发明名称 |
Mu opioid receptor agonist analogs of the endomorphins |
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. |
申请公布号 |
AU2011274522(A8) |
申请公布日期 |
2016.04.14 |
申请号 |
AU20110274522 |
申请日期 |
2011.07.08 |
申请人 |
UNITED STATES DEPARTMENT OF VETERANS AFFAIRS;THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND |
发明人 |
ZADINA, JAMES E.;HACKLER, LASZLO |
分类号 |
C07K5/12;A61K38/12;A61P1/12;C07K7/64;G01N33/68 |
主分类号 |
C07K5/12 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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