(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.
Pubblicazioni consigliate
I metadati presenti in IRIS UNIMORE sono rilasciati con licenza Creative Commons CC0 1.0 Universal, mentre i file delle pubblicazioni sono rilasciati con licenza Attribuzione 4.0 Internazionale (CC BY 4.0), salvo diversa indicazione.
In caso di violazione di copyright, contattare Supporto Iris
