The Administrators of the Tulane Educational Fund

The United States Government as Represented by the Department of Veterans Affairs

James E Zadina

Laszlo Hackler

Abba J Kastin

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 analogs of endomorphin. These peptide analogs exhibit decreased tolerance relative to morphine, increased solubility compared to similar tetrapeptide analogs, while maintaining favorable or improved therapeutic ratios of analgesia to side effects.

Mu opioid receptor agonist analogs of the endomorphins

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 decreased tolerance relative to morphine, increased solubility compared to similar tetrapeptide analogs, while maintaining favorable or improved therapeutic ratios of analgesia to side effects.

This invention relates to certain peptides and linear and cyclic analogs thereof that bind to the mu (morphine) opiate receptor with higher affinity, selectivity and potency than currently available peptides. This invention also relates to pharmaceutical preparations containing an effective amount of the peptides or salts thereof, and methods for providing analgesia, relief from gastrointestinal disorders such as diarrhea, and therapy for drug dependence containing a pharmaceutically effective amount of the peptides.

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Metairie, LA, United States of America

James E Zadina