| Literature DB >> 19642675 |
Gianfranco Balboni1, Claudio Trapella, Yusuke Sasaki, Akihiro Ambo, Ewa D Marczak, Lawrence H Lazarus, Severo Salvadori.
Abstract
To improve the structure-activity studies of the lead delta opioid agonist H-Dmt-Tic-Asp*-Bid, we synthesized and pharmacologically characterized a series of analogues in which the side chain next to 1H-benzimidazole-2-yl (Bid) was substituted by those endowed with different chemical properties. Interesting results were obtained: (1) only Gly, Ala, and Asp resulted in delta agonism, (2) Phe yielded delta antagonism, (3) and all other residues except Glu (devoid of any activity) gave mu agonism.Entities:
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Year: 2009 PMID： 19642675 DOI： 10.1021/jm900686q
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446