103613-72-5Relevant articles and documents
Design and synthesis of peptides passing through the blood-brain barrier
Wakamiya, Tateaki,Kamata, Makoto,Kusumoto, Shoichi,Kobayashi, Hiroyuki,Sai, Yoshimichi,Tamai, Ikumi,Tsuji, Akira
, p. 699 - 709 (2007/10/03)
The blood-brain barrier (BBB) is a highly selective membranous barrier regulating the transport of substances in blood into the brain parenchyma. At present, delivery of biologically active peptides or peptide drugs into the brain is quite an important subject from the standpoint of chemotherapy for brain diseases H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)8NH2 termed 001-C8 was first synthesized to elucidate the structural specificity of peptides for passing through the BBB. The Na-methylamino acid and D-amino acid residues were appropriately situated in this peptide to protect against the digestion by peptidase. Furthermore, a number of basic peptides were prepared as 001-C8 analogs for studying the relationship between structure and BBB permeability of peptides.
Synthesis and structure-activity relationships of dynorphin A-(1-8) amide analogues
Yoshino,Nakazawa,Arakawa,Kaneko,Tsuchiya,Matsunaga,Araki,Ikeda,Yamatsu,Tachibana
, p. 206 - 212 (2007/10/02)
In order to study the structure-activity relationships of dynorphin A-(1-8) amide [Dyn(1-8)-NH2], 20 analogues were synthesized by the solution method. Their biological activities were determined in the three bioassays [guinea pig ileum (GPI),