68800-26-0Relevant articles and documents
SYNTHESIS OF ENKEPHALINS BY THE METHOD OF POLYMERIC ACTIVATED ESTERS BASED ON 4-HYDROXY-3-NITROBENZOPHENONE
Grigor'ev, E. I.,Chernova, S. V.
, p. 468 - 474 (2007/10/02)
Leucine- and methionine-enkephalins have been synthesized by the successive growth of the peptide chain from the C-end by the method of polymeric activated esters based on 4-hydroxy-3-nitrobenzophenone with yields of 90 and 70percent, respectively, calculated on the initial C-terminal amino acid.Polystyrene with 2percent of divinylbenzene was used as the polymeric matrix.Using the synthesis of methionine-enkephalin as an example, the possibility has been shown of using polymeric activated esters for the synthesis of peptides with a free carboxy group.
Synthesis and biological evaluation of a metazocine-containing enkephalinamide. Evidence for nonidentical roles of the tyramine moiety in opiates and opioid peptides
Ramakrishnan,Portoghese
, p. 1423 - 1427 (2007/10/02)
In an effort to test the hypothesis that the tyramine moiety present in opiates and in opioid peptides plays an identical functional role at opioid receptors, a hybrid enkephalinamide (3) that contains (-)-metazocine in place of Tyr1 was synthesized. It was found that 3 and its congeners are inactive or feebly active in the electrically stimulated guinea pig ileum and mouse vas deferens preparations. The results of these studies suggest that the tyramine moiety in opiates and related structures does not play the same functional role as that in the opioid peptides. It is suggested that the different functional roles of the tyramine moiety in opiates and opioid peptides is a consequence of different modes of interaction with common receptors.
Synthesis of fragments of human β-lipotropin, β(h)-LPH. Part III. The synthesis of des-1-tyrosine-γ-endorphin, i.e. β-LPH-(62-77)
Greven,Bijl,Van Nispen
, p. 63 - 64 (2007/10/02)
It was deemed of interest to study the effect of endorphin fragments other than the already described α-and γ-endorphin on behavioural activity as observed in the pole-jumping test or in other test models. Together with effects observed in other tests (pa