(+)-2-methyl-4-carboxyphenylglycine (LY367385) selectively antagonises metabotropic glutamate mGluR1 receptors

被引:111
作者
Clark, BP
Baker, SR
Goldsworthy, J
Harris, JR
Kingston, AE
机构
[1] Eli Lilly and Co., Lilly Research Centre Ltd., Windlesham, Surrey GU20 6PH, Erl Wood Manor
关键词
D O I
10.1016/S0960-894X(97)10071-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of three novel 4-carboxyphenylglycine derivatives is described. 2-Methyl substituents increase the antagonist potency compared to (S)-4CPG at mGluR1 receptors. Resolution of compound 1 showed that the activity resided in the (+)-isomer LY367385. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:2777 / 2780
页数:4
相关论文
共 16 条
  • [1] BAKER SR, 1995, BIOORG MED CHEM LETT, V5, P223
  • [2] Pharmacology and functions of metabotropic glutamate receptors
    Conn, PJ
    Pin, JP
    [J]. ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, 1997, 37 : 205 - 237
  • [3] PALLADIUM CATALYZED ALKOXYCARBONYLATION OF PHENOLS TO BENZOATE ESTERS
    DOLLE, RE
    SCHMIDT, SJ
    KRUSE, LI
    [J]. JOURNAL OF THE CHEMICAL SOCIETY-CHEMICAL COMMUNICATIONS, 1987, (12) : 904 - 905
  • [4] USEFUL SYNTHESIS OF ALPHA-AMINONITRILES BY MEANS OF ALUMINA AND ULTRASOUND
    HANAFUSA, T
    ICHIHARA, J
    ASHIDA, T
    [J]. CHEMISTRY LETTERS, 1987, (04) : 687 - 690
  • [5] Identification of carbonyl compounds through conversion into hydantoins
    Henze, HR
    Speer, RJ
    [J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1942, 64 : 522 - 523
  • [6] PHARMACOLOGICAL ANALYSIS OF 4-CARBOXYPHENYLGLYCINE DERIVATIVES - COMPARISON OF EFFECTS ON MGLUR1-ALPHA AND MGLUR5A SUBTYPES
    KINGSTON, AE
    BURNETT, JP
    MAYNE, NG
    LODGE, D
    [J]. NEUROPHARMACOLOGY, 1995, 34 (08) : 887 - 894
  • [7] Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): A potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties
    Monn, JA
    Valli, MJ
    Massey, SM
    Wright, RA
    Salhoff, CR
    Johnson, BG
    Howe, T
    Alt, CA
    Rhodes, GA
    Robey, RL
    Griffey, KR
    Tizzano, JP
    Kallman, MJ
    Helton, DR
    Schoepp, DD
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (04) : 528 - 537
  • [8] Moroni F, 1997, J PHARMACOL EXP THER, V281, P721
  • [9] OMSTEIN PL, 1996, TRENDS PHARMACOL SCI, V17, P429
  • [10] 1-AMINOINDAN-1,5-DICARBOXYLIC ACID - A NOVEL ANTAGONIST AT PHOSPHOLIPASE C-LINKED METABOTROPIC GLUTAMATE RECEPTORS
    PELLICCIARI, R
    LUNEIA, R
    COSTANTINO, G
    MARINOZZI, M
    NATALINI, B
    JAKOBSEN, P
    KANSTRUP, A
    LOMBARDI, G
    MORONI, F
    THOMSEN, C
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (19) : 3717 - 3719