Oral Bioavailability of a New Class of μ-Opioid Receptor Agonists Containing 3, 6-Bis [Dmt-NH (CH2) n]-2 (1 H)-pyrazinone with Central-Mediated Analgesia

…, Y Fujisawa, K Shiotani, Y Tsuda, T Yokoi…

Index: Okada, Yoshio; Fujisawa, Yutaka; Morishita, Akihisa; Shiotani, Kimitaka; Miyazaki, Anna; Fujita, Yoshio; Li, Tingyou; Tsuda, Yuko; Yokoi, Toshio; Bryant, Sharon D.; Lazarus, Lawrence H. Tetrahedron Letters, 2002 , vol. 43, # 45 p. 8137 - 8139

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Citation Number: 47

Abstract

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 limitation, we enhanced the hydrophobicity while maintaining the aqueous solubility properties in a class of opioid-mimetic substances by inclusion of two identical N-termini consisting of Dmt (2', 6 ...