234450-13-6Relevant academic research and scientific papers
Oral Bioavailability of a New Class of μ-Opioid Receptor Agonists Containing 3,6-Bis[Dmt-NH(CH2)n]-2(1H)-pyrazinone with Central-Mediated Analgesia
Jinsmaa, Yunden,Miyazaki, Anna,Fujita, Yoshio,Li, Tingyou,Fujisawa, Yutaka,Shiotani, Kimitaka,Tsuda, Yuko,Yokoi, Toshio,Ambo, Akihiro,Sasaki, Yusuke,Bryant, Sharon D.,Lazarus, Lawrence H.,Okada, Yoshio
, p. 2599 - 2610 (2007/10/03)
The inability of opioid peptides to be transported through epithelial membranes in the gastrointestinal tract and pass the blood-brain barrier limits their effectiveness for oral application in an antinociceptive treatment regime. To overcome this limitat
Synthesis of pyrazinone ring-containing opioid mimetics and examination of their opioid receptor-binding activity
Okada, Yoshio,Fukumizu, Atsuko,Takahashi, Motohiro,Yokoi, Toshio,Tsuda, Yuko,Bryant, Sharon D.,Lazarus, Lawrence H.
, p. 1193 - 1195 (2007/10/03)
Cyclization of dipeptidyl chloromethyl ketones gave 6-(4-aminobutyl)-3- carboxyethyl-5-methyl-2(1H)-pyrazinone, 3-(4-aminobutyl)-6-carboxyethyl-5- methyl-2(1H)-pyrazinone, and 3,6-bis(4-aminobutyl)-5-methyl-2(1H)-pyrazinone, which were inserted into the enkephalin sequence to give opioid mimetics. Thus, it was confirmed that a pyrazinone ring can be easily inserted into a peptide sequence in order to evaluate structural components required for biologically active peptides.
