4.7 Article

New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores

期刊

JOURNAL OF MEDICINAL CHEMISTRY
卷 49, 期 18, 页码 5640-5643

出版社

AMER CHEMICAL SOC
DOI: 10.1021/jm0605785

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  1. Intramural NIH HHS [Z01 ES100472-06, Z99 ES999999, Z01 ES090053-20] Funding Source: Medline
  2. NIDA NIH HHS [K05 DA000360, R01 DA014251, K05-DA 00360, R01-DA14251] Funding Source: Medline

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Here, we report the synthesis of a designed multi-pharmacophore ligand derived from the linkage of a delta selective peptide antagonist (Dmt-Tic) and a mu/kappa morphinan agonist butorphan (MCL 101) through a two methylene spacer. The new compound MCL 450 maintains the same characteristics as those the two reference compounds. MCL 450 represents a useful starting point for the synthesis of other multiple opioid ligands endowed with analgesic properties with low tolerance and dependence.

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