期刊
FUTURE MEDICINAL CHEMISTRY
卷 9, 期 17, 页码 2099-2115出版社
FUTURE SCI LTD
DOI: 10.4155/fmc-2017-0104
关键词
agonism; antagonism; antinociception; bioavailability; CJ-15,208; drug abuse; endomorphin; molecular docking; opioid peptides; tryptophan
资金
- Umberto Veronesi Foundation, Milano, Roma, Italy
Recently, a new family of opioid peptides containing tryptophan came to the spotlight for the absence of the fundamental protonable tyramine 'message' pharmacophore. Structure-activity relationship investigations led to diverse compounds, characterized by different selectivity profiles and agonist or antagonist effects. Substitution at the indole of Trp clearly impacted peripheral/central antinociceptivity. These peculiarities prompted to gather all the compounds in a new class, and to coin the definition 'TryptophanContaining Non-Cationizable Opioid Peptides', in short 'TryCoNCOPs'. Molecular docking analysis suggested that the TryCoNCOPs can still interact with the receptors in an agonist-like fashion. However, most TryCoNCOPs showed significant differences between the in vitro and in vivo activities, suggesting that opioid activity may be elicited also via alternative mechanisms.
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