Design of a highly potent anti-hypertensive peptide based on ovokinin(2-7).
作者： Yuko YAMADA , Nobuyuki MATOBA , Hachiro USUI , Kunihiko ONISHI , Masaaki YOSHIKAWA
DOI: 10.1271/BBB.66.1213
关键词: Pharmacology 、 Amino acid residue 、 Ovalbumin 、 Orally active 、 Endocrinology 、 Oral administration 、 Chemistry 、 Residue (chemistry) 、 Internal medicine 、 Peptide
摘要: Ovokinin(2-7) (RADHPF), an orally active anti-hypertensive peptide derived from ovalbumin, lowers blood pressure in SHRs at a dose of 10 mg/kg. Attempts were made to potentiate its activity by replacing the amino acid residues [Pro2, Phe3]-ovokinin(2-7), which was previously reported have 33-fold stronger than ovokinin(2-7). The Phe3]-ovokinin(2-7) improved replacement C-terminal Phe residue with Trp. Then, best other positions for effect selected. RPLKPW, most potent derivative obtained, showed significant activities 0.1 mg/kg after oral administration spontaneously hypertensive rats (SHRs). Thus, RPLKPW 100-fold more
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