2004 Peptides

PeptidesU 0400 N-Acyl 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline: The First Orexin-2 Recep-

tor Selective Non-Peptide Antagonist. — Substitution of the acyl portion of a recent-ly discovered, non-selective orexin antagonist with tert-leucine and introduction of a pyridylmethyl substituent onto the amino function of tert-levcine leads to the identifi-cation of compound (I), a potent hOX2R antagonist with high selectivity and high water solubility. — (HIROSE*, M.; EGASHIRA, S.-I.; GOTO, Y.; HASHIHAYATA, T.; OHTAKE, N.; IWAASA, H.; HATA, M.; FUKAMI, T.; KANATANI, A.; YAMADA, K.; Bioorg. Med. Chem. Lett. 13 (2003) 24, 4497-4499; Tsukuba Res. Inst., Banyu Pharm. Co., Ltd., Tsukuba, Ibaraki 300-33, Japan; Eng.) — H. Hoennerscheid

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