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.
Publication types
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Research Support, N.I.H., Intramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Benzimidazoles / chemical synthesis
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Benzimidazoles / chemistry*
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Benzimidazoles / metabolism
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Benzimidazoles / pharmacology*
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Dipeptides / chemistry*
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Humans
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Inhibitory Concentration 50
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Narcotic Antagonists* / chemical synthesis
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Narcotic Antagonists* / chemistry*
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Narcotic Antagonists* / metabolism
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Narcotic Antagonists* / pharmacology*
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Receptors, Opioid / metabolism
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Substrate Specificity
Substances
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Benzimidazoles
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Dipeptides
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Narcotic Antagonists
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Receptors, Opioid
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benzimidazole