[3H]LY341495, a highly potent, selective and novel radioligand for labeling group II metabotropic glutamate receptors

被引:40
作者
Ornstein, PL [1 ]
Arnold, MB [1 ]
Bleisch, TJ [1 ]
Wright, RA [1 ]
Wheeler, WJ [1 ]
Schoepp, DD [1 ]
机构
[1] Eli Lilly & Co, Lilly Res Labs, Lilly Corp Ctr, Indianapolis, IN 46285 USA
关键词
D O I
10.1016/S0960-894X(98)00329-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
We report herein the synthesis and pharmacological characterization of a tritiated version of the potent and selective cyclopropyl amino acid LY341495 as a radioligand to label group II metabotropic glutamate receptors in rat brain homogenates. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1919 / 1922
页数:4
相关论文
共 11 条
  • [1] MOLECULAR NEUROBIOLOGY OF GLUTAMATE RECEPTORS
    GASIC, GP
    HOLLMANN, M
    [J]. ANNUAL REVIEW OF PHYSIOLOGY, 1992, 54 : 507 - 536
  • [2] AGONIST ANALYSIS OF 2-(CARBOXYCYCLOPROPYL)GLYCINE ISOMERS FOR CLONED METABOTROPIC GLUTAMATE RECEPTOR SUBTYPES EXPRESSED IN CHINESE-HAMSTER OVARY CELLS
    HAYASHI, Y
    TANABE, Y
    ARAMORI, I
    MASU, M
    SHIMAMOTO, K
    OHFUNE, Y
    NAKANISHI, S
    [J]. BRITISH JOURNAL OF PHARMACOLOGY, 1992, 107 (02) : 539 - 543
  • [3] 3,5-DIHYDROXYPHENYLGLYCINE - A POTENT AGONIST OF METABOTROPIC GLUTAMATE RECEPTORS
    ITO, I
    KOHDA, A
    TANABE, S
    HIROSE, E
    HAYASHI, M
    MITSUNAGA, S
    SUGIYAMA, H
    [J]. NEUROREPORT, 1992, 3 (11) : 1013 - 1016
  • [4] LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors
    Kingston, AE
    Ornstein, PL
    Wright, RA
    Johnson, BG
    Mayne, NG
    Burnett, JP
    Belagaje, R
    Wu, S
    Schoepp, DD
    [J]. NEUROPHARMACOLOGY, 1998, 37 (01) : 1 - 12
  • [5] Synthesis of the four isomers of 4-aminopyrrolidine-2,4-dicarboxylate: Identification of a potent, highly selective, and systemically-active agonist for metabotropic glutamate receptors negatively coupled to adenylate cyclase
    Monn, JA
    Valli, MJ
    Johnson, BG
    Salhoff, CR
    Wright, RA
    Howe, T
    Bond, A
    Lodge, D
    Spangle, LA
    Paschal, JW
    Campbell, JB
    Griffey, K
    Tizzano, JP
    Schoepp, DD
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (15) : 2990 - 3000
  • [6] 2-substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors.: 2.: Effects of aromatic substitution, pharmacological characterization, and bioavailability
    Ornstein, PL
    Bleisch, TJ
    Arnold, MB
    Kennedy, JH
    Wright, RA
    Johnson, BG
    Tizzano, JP
    Helton, DR
    Kallman, MJ
    Schoepp, DD
    Hérin, M
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (03) : 358 - 378
  • [7] 2-substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl)glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 1. Effects of alkyl, arylalkyl, and diarylalkyl substitution
    Ornstein, PL
    Bleisch, TJ
    Arnold, MB
    Wright, RA
    Johnson, BG
    Schoepp, DD
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1998, 41 (03) : 346 - 357
  • [8] PIN JP, 1995, NEUROPHARMACOLOGY, V34, P1, DOI 10.1016/0028-3908(94)00129-G
  • [9] 1S,3R-ACPD-SENSITIVE (METABOTROPIC) [H-3] GLUTAMATE RECEPTOR-BINDING IN MEMBRANES
    SCHOEPP, DD
    TRUE, RA
    [J]. NEUROSCIENCE LETTERS, 1992, 145 (01) : 100 - 104
  • [10] The novel metabotropic glutamate receptor agonist 2R,4R-APDC potentiates stimulation of phosphoinositide hydrolysis in the rat hippocampus by 3,5-dihydroxyphenylglycine: Evidence for a synergistic interaction between group 1 and group 2 receptors
    Schoepp, DD
    Salhoff, CR
    Wright, RA
    Johnson, BG
    Burnett, JP
    Mayne, NG
    Belagaje, R
    Wu, S
    Monn, JA
    [J]. NEUROPHARMACOLOGY, 1996, 35 (12) : 1661 - 1672