The United States of America, As Represented by the Secretary, Department of Health and Human Services

The United States of America As Represented by the Department of Health

Teikoku Seiyaku Co., Ltd.

Kobe Gakuin University

Lawrence H Lazarus

Severo Salvadori

Yoshio Okada

Yuko Tsuda

Toshio Yokoi

Tingyou Li

Sharon D Bryant

Piero Andrea Temussi

The present invention relates to symmetric and asymmetric dimeric Dmt (2',6&#x2032;-ditnethyl) compounds and Dmt derivative compounds with dual &#x3b4; and &#x3bc; opioid receptor antagonist activity. Also, the present invention provides compositions comprising these compounds and it provides methods of using these compounds.

Dmt-derivative compounds and related compositions and methods of use

A compound of formula:wherein X is a spacer comprising one or more amino acid residues and Y comprises an aromatic group and related compositions and methods of use.

Dmt-Tic di-and tri-peptidic derivatives and related compositions and methods of use

1. A peptide derivative represented by the following formula (1) or a salt thereof;wherein Ris hydrogen atom or methyl group, Ris hydrogen atom or hydroxy group and n is an integer of 1-8, provided that Ris hydrogen atom when Ris hydrogen atom, which has specific and high binding affinity with the &#x3bc;-opioid receptor.

Opioid derivative

Dmt-Tic di- and tri-peptide derivatives and related compositions and methods of use

Novel opioidmimetic dipeptides, tripeptides and cyclic peptides exhibit enhanced affinity and selectivity for .delta. opioid receptors. The peptides are represented by the formulas L/D-Dmt-L-/D-Tic-R', L/D-Dmt-L-/D-Tic-R-R' and cyclic (L/D-Dmt-L/D-Tic) wherein Dmt is 2',6',-dimethyl-L/D-tyrosine Tic is L-/D-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, R is a natural or unusual aliphatic amino residue and R' is a functional group at the carboxyl terminus of the peptide. Pharmacological and therapeutic and compositions are also provided.

Ultraselective opioidmimetic peptides and pharmacological and

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Durham, NC, United States of America

Lawrence H Lazarus