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LY354740, a group II metabotropic glutamate receptor agonist with potential antiparkinsonian properties in rats.

作者信息

Konieczny J, Ossowska K, Wolfarth S, Pilc A

机构信息

Department of Neuro-Psychopharmacology, Institute of Pharmacology, Polish Academy of Sciences, Kraków.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1998 Oct;358(4):500-2. doi: 10.1007/pl00005284.

DOI:10.1007/pl00005284
PMID:9826074
Abstract

The aim of this study was to examine whether (+)-2-aminobicyclo[3.1.0]-hexane-2,6-dicarboxylate monohydrate (LY354740), a selective agonist of group II metabotropic glutamate receptors, possesses antiparkinsonian properties. Parkinsonian-like muscle rigidity was induced by pretreatment with haloperidol (1 mg/kg i.p.). It was measured as increased resistance developed by the rat's hind leg to passive extension and flexion. LY354740 (5 and 10 mg/kg i.p.) dose-dependently diminished the haloperidol-induced muscle rigidity. The present results suggest that LY354740 counteracts the muscle rigidity in an animal model of parkinsonism.

摘要

相似文献

1
LY354740, a group II metabotropic glutamate receptor agonist with potential antiparkinsonian properties in rats.
Naunyn Schmiedebergs Arch Pharmacol. 1998 Oct;358(4):500-2. doi: 10.1007/pl00005284.
2
The role of metabotropic glutamate receptor (mGluR) ligands in parkinsonian muscle rigidity.代谢型谷氨酸受体(mGluR)配体在帕金森病肌肉强直中的作用。
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Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors.与(+)-2-氨基双环[3.1.0]己烷-2,6-二羧酸(LY354740)相关的杂双环氨基酸的合成、药理学表征及分子模拟:两种新型强效、选择性且具有全身活性的II型代谢型谷氨酸受体激动剂的鉴定
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4
Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039).一种结构新颖、强效且选择性的代谢型谷氨酸2/3受体激动剂的药理学和药代动力学特性:激动剂(-)-(1R,4S,5S,6S)-4-氨基-2-磺酰基双环[3.1.0]己烷-4,6-二羧酸(LY404039)的体外特性研究
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Effects of a metabotropic glutamate receptor group II agonist LY354740 in animal models of positive schizophrenia symptoms and cognition.亲代谢型谷氨酸受体II组激动剂LY354740在精神分裂症阳性症状及认知动物模型中的作用
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Preliminary evidence of attenuation of the disruptive effects of the NMDA glutamate receptor antagonist, ketamine, on working memory by pretreatment with the group II metabotropic glutamate receptor agonist, LY354740, in healthy human subjects.在健康人类受试者中,通过用II型代谢型谷氨酸受体激动剂LY354740预处理,初步证明N-甲基-D-天冬氨酸(NMDA)谷氨酸受体拮抗剂氯胺酮对工作记忆的破坏作用有所减弱。
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7
LY354740 affects startle responding but not sensorimotor gating or discriminative effects of phencyclidine.LY354740影响惊吓反应,但不影响苯环利定的感觉运动门控或辨别效应。
Eur J Pharmacol. 2000 Jan 28;388(2):R3-4. doi: 10.1016/s0014-2999(99)00844-4.
8
Anxiolytic-like activity of the mGLU2/3 receptor agonist LY354740 in the elevated plus maze test is disrupted in metabotropic glutamate receptor 2 and 3 knock-out mice.代谢型谷氨酸受体2和3基因敲除小鼠在高架十字迷宫试验中,代谢型谷氨酸受体2/3激动剂LY354740的抗焦虑样活性受到破坏。
Psychopharmacology (Berl). 2005 Apr;179(1):284-91. doi: 10.1007/s00213-004-2098-x. Epub 2004 Dec 24.
9
Blockade of the metabotropic glutamate receptor subtype 5 (mGluR5) produces antiparkinsonian-like effects in rats.代谢型谷氨酸受体5(mGluR5)的阻断在大鼠中产生抗帕金森氏症样效应。
Neuropharmacology. 2001 Sep;41(4):413-20. doi: 10.1016/s0028-3908(01)00083-1.
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In vitro and in vivo evidence for a lack of interaction with dopamine D2 receptors by the metabotropic glutamate 2/3 receptor agonists 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-bicaroxylate monohydrate (LY354740) and (-)-2-oxa-4-aminobicyclo[3.1.0] Hexane-4,6-dicarboxylic acid (LY379268).代谢型谷氨酸2/3受体激动剂1S,2S,5R,6S - 2 - 氨基双环[3.1.0]己烷 - 2,6 - 二羧酸单水合物(LY354740)和( - ) - 2 - 氧杂 - 4 - 氨基双环[3.1.0]己烷 - 4,6 - 二羧酸(LY379268)与多巴胺D2受体缺乏相互作用的体外和体内证据。
J Pharmacol Exp Ther. 2009 Dec;331(3):1126-36. doi: 10.1124/jpet.109.160598. Epub 2009 Sep 15.

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