(Chemical Equation Presented) No gain with pain: At least when it comes to analgesics! Here we show that enkephalin analogues with the Gly 3-Phe 4 peptide bond replaced by a stereochemically defined trifluoroethylamine function display binding affinities in the nanomolar range for the - and -opioid receptors, only 30- to 80-fold lower than those of the natural compounds, whereas the Gly 2-Gly 3 trifluoroethylamine analogues have lower affinity. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.

Synthesis and in vitro evaluation of trifluoroethylamine analogues of enkephalins / Sinisi, R.; Ghilardi, A.; Ruiu, S.; Lazzari, P.; Malpezzi, L.; Sani, M.; Pani, L.; Zanda, M.. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 4:9(2009), pp. 1416-1420. [10.1002/cmdc.200900158]

Synthesis and in vitro evaluation of trifluoroethylamine analogues of enkephalins

Pani L.;
2009

Abstract

(Chemical Equation Presented) No gain with pain: At least when it comes to analgesics! Here we show that enkephalin analogues with the Gly 3-Phe 4 peptide bond replaced by a stereochemically defined trifluoroethylamine function display binding affinities in the nanomolar range for the - and -opioid receptors, only 30- to 80-fold lower than those of the natural compounds, whereas the Gly 2-Gly 3 trifluoroethylamine analogues have lower affinity. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.
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Synthesis and in vitro evaluation of trifluoroethylamine analogues of enkephalins / Sinisi, R.; Ghilardi, A.; Ruiu, S.; Lazzari, P.; Malpezzi, L.; Sani, M.; Pani, L.; Zanda, M.. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 4:9(2009), pp. 1416-1420. [10.1002/cmdc.200900158]
Sinisi, R.; Ghilardi, A.; Ruiu, S.; Lazzari, P.; Malpezzi, L.; Sani, M.; Pani, L.; Zanda, M.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11380/1211965
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