Document Detail


Antinociceptive profile of potent opioid peptide AM94, a fluorinated analogue of biphalin with non-hydrazine linker.
MedLine Citation:
PMID:  23136069     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
AM94 is a fluorinated analog of biphalin with non-hydrazine linker that has an in vitro affinity for μ-opioid and δ-opioid receptors tenfold higher than biphalin. Furthermore, in vivo evaluation in rats showed that AM94 has in hot plate test - after both intracerebroventricular and intravenous administrations - a greater and more durable efficacy than biphalin. Here, the antinociceptive profile of AM94 is further evaluated by following two different administration routes, intrathecal and subcutaneous, and two different animal species, rats and mice. The analgesic potency of AM94 is compared with that of both the parent peptide biphalin and morphine. Results show that in rats (tail flick test) and in mice (formalin test), AM94 has a higher and more durable analgesic effect than biphalin after intrathecal and subcutaneous administrations. Conformational properties of biphalin and AM94 were also investigated by variable-temperature (1) H NMR and energy minimization. Copyright © 2012 European Peptide Society and John Wiley & Sons, Ltd.
Authors:
Adriano Mollica; Roberto Costante; Azzurra Stefanucci; Francesco Pinnen; Gino Lucente; Stefano Fidanza; Stefano Pieretti
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-11-8
Journal Detail:
Title:  Journal of peptide science : an official publication of the European Peptide Society     Volume:  -     ISSN:  1099-1387     ISO Abbreviation:  J. Pept. Sci.     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-11-8     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9506309     Medline TA:  J Pept Sci     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012 European Peptide Society and John Wiley & Sons, Ltd.
Affiliation:
Dipartimento di Farmacia, Università di Chieti-Pescara "G. d'Annunzio", Via dei Vestini 31, 66100, Chieti, Italy. a.mollica@unich.it.
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