The preclinical properties of a novel group II metabotropic glutamate receptor agonist LY379268.

Imre G

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The preclinical properties of a novel group II metabotropic glutamate receptor agonist LY379268.

机译：新型II型代谢型谷氨酸受体激动剂LY379268的临床前特性。

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Activation of group II metabotropic glutamate (mGlu2/3) receptors reduces excessive glutamate release that is often associated with neurodegenerative and psychiatric disorders. This finding encouraged the search for potent and selective agonists as potential therapeutic agents. The search led to the discovery of LY379268 {(-)-2-oxa-4-aminobicyclo[3.1.0]hexane-4,6-dicarboxylic acid}, which is a highly potent and systemically available mGlu2/3 receptor agonist. LY379268 was effective in several animal models of stroke, epilepsy, drug abuse, schizophrenia, and pain. Suppression of motor activity is the major side effect of LY379268. Upon repeated administration tolerance develops to this side effect, while the therapeutic effects of LY379268 remain. To date, no clinical data with LY379268 are available. This review article summarizes the preclinical pharmacology of LY379268.

机译：II型代谢型谷氨酸（mGlu2 / 3）受体的激活减少了通常与神经退行性疾病和精神疾病有关的过量谷氨酸释放。这一发现鼓励寻找有效和选择性激动剂作为潜在的治疗剂。搜索导致发现了LY379268 {（-）-2-oxa-4-氨基双环[3.1.0]己烷-4,6-二羧酸}，它是一种高效且可系统使用的mGlu2 / 3受体激动剂。 LY379268在中风，癫痫，药物滥用，精神分裂症和疼痛的几种动物模型中均有效。抑制运动活性是LY379268的主要副作用。反复给药后，对该副作用产生了耐受性，而LY379268的治疗作用仍然存在。迄今为止，尚无LY379268的临床数据。这篇综述文章总结了LY379268的临床前药理作用。

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《CNS drug reviews》 |2007年第4期|共21页
作者
Imre G;
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正文语种 eng
中图分类药学;
关键词
LY 379268; novel; receptor; Glutamate;

机译：LY 379268;新颖;受体;谷氨酸;

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1. The preclinical properties of a novel group II metabotropic glutamate receptor agonist LY379268. [J] . Imre G CNS drug reviews . 2007,第4期

机译：新型II型代谢型谷氨酸受体激动剂LY379268的临床前特性。
2. Regulation of Akt and Wnt signaling by the group II metabotropic glutamate receptor antagonist LY341495 and agonist LY379268. [J] . Sutton LP, Rushlow WJ Journal of Neurochemistry: Offical Journal of the International Society for Neurochemistry . 2011,第6期

机译：II组代谢型谷氨酸受体拮抗剂LY341495和激动剂LY379268对Akt和Wnt信号的调节。
3. Modulation of stress-induced and stimulated hyperprolactinemia with the group II metabotropic glutamate receptor selective agonist, LY379268. [J] . Johnson M, Chamberlain M Neuropharmacology . 2002,第5期

机译：II组代谢型谷氨酸受体选择性激动剂LY379268对应激诱导和刺激的高泌乳素血症的调节。
4. Inverse agonists to explore the mechanisms of metabotropic glutamate receptor activity [C] . L. Prezeau, M.L. Parmentier, R Carroll, Fundaci髇 Dr. Antonio Esteve . 2003

机译：反向激动剂探讨代谢谷氨酸受体活性的机制
5. Modulation of long -term potentiation and epileptiform activity in the rat dentate gyrus by the group II metabotropic glutamate receptor subtype mGluR3 [D] . Lea, Paul Milward, IV 2000

机译：II型代谢型谷氨酸受体亚型mGluR3对大鼠齿状回的长期增强和癫痫样活性的调节
6. The Preclinical Properties of a Novel Group II Metabotropic Glutamate Receptor Agonist LY379268 [O] . Gabor Imre 2007

机译：新型II族代谢型谷氨酸受体激动剂LY379268的临床前特性
7. Metabotropic glutamate receptor 3 neuroprotection A. Berent-Spillson and J. W. Russell Received June 12, 2006; revised manuscript received October 3, 2006; accepted October 5, 2006. Address correspondence and reprint requests to James W. Russell, Department of Neurology, University of Maryland School of Medicine, 22 South Greene Street, Baltimore, MD 21201-1595, USA. E-mail: jruss@umich.edu Abbreviations used : APDC , 2 R ,4 R -4-aminopyrrolidine-2,4-dicarboxylate (specific metabotropic glutamate receptor 3 agonist) ; BSO , buthionine sulfoximine (GSH synthesis inhibitor) ; caspase , cysteine-requiring aspartate protease ; CysGly , cysteinylglycine (GSH degradation product) ; DAPI , 4′-6-diamidino-2-phenylindole ; DCF , dichlorodihydrofluorescein ; DCFDA , 5-(and 6)-chloromethyl-2′,7′-dichlorodihydrofluorescein diacetate, acetyl ester ; DHE , dihydroethidium ; DRG , dorsal root ganglion ; FCCP , carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone (electron transport uncoupler) ; GCP II/III , glutamate carboxypeptidase II/III ; GSH , glutathione ; GSH-EE , glutathione ethyl ester ; GST , glutathione-s-transferase ; H 2 O 2 , hydrogen peroxide ; HBSS , Hank’s balanced salt solution ; JC-1 , 5,5′,6,6′-tetrachloro-1,1′,3,3′-tetraethylbenzimidazolylcarbocyanine iodide ; MCB , monochlorobimane ; mGluR , metabotropic glutamate receptor ; NAAG , N -acetyl-aspartyl-glutamate ; PBS , phosphate-buffered saline ; PCD , programmed cell death ; Rh123 , rhodamine123 ; ROS , reactive oxygen species ; δψ μ , inner mitochondrial membrane potential . Metabotropic glutamate receptor 3 protects neurons from glucose-induced oxidative injury by increasing intracellular glutathione concentration [O] . Berent-Spillson Alison, Russell James W. 2007

机译：代谢型谷氨酸受体3神经保护a. Berent-spillson和J. W. Russell于2006年6月12日收到;修订稿于2006年10月3日收到; 2006年10月5日接受。美国马里兰州巴尔的摩市南格林街22号，马里兰大学医学院神经病学系James W. Russell的地址通信和重印申请。电子邮件：jruss@umich.edu使用的缩写：apDC，2R，4R-4-氨基吡咯烷-2,4-二羧酸酯（特异性代谢型谷氨酸受体3激动剂）; BsO，丁硫氨酸亚砜亚胺（GsH合成抑制剂）;半胱天冬酶，半胱氨酸需要的天冬氨酸蛋白酶; CysGly，半胱氨酰甘氨酸（GsH降解产物）; DapI，4'-6-二脒基-2-苯基吲哚; DCF，二氯二氢荧光素; DCFDa，5-（和6） - 氯甲基-2'，7'-二氯二氢荧光素二乙酸酯，乙酰酯; DHE，二氢乙锭; DRG，背根神经节; FCCp，羰基氰化物4-（三氟甲氧基）苯腙（电子传输解偶联剂）; GCp II / III，谷氨酸羧肽酶II / III;谷胱甘肽;谷胱甘肽; GsH-EE，谷胱甘肽乙酯; GsT，谷胱甘肽-s-转移酶; H 2 O 2，过氧化氢; HBss，Hank的平衡盐溶液; JC-1,5,5'，6,6'-四氯-1,1'，3,3'-四乙基苯并咪唑基酞菁碘化物; mCB，monochlorobimane; mGluR，代谢型谷氨酸受体; NaaG，N-乙酰基 - 天冬氨酰谷氨酸; pBs，磷酸盐缓冲盐水; pCD，程序性细胞死亡; Rh123，罗丹明123;活性氧，活性氧; δψμ，线粒体内膜电位。代谢型谷氨酸受体3通过增加细胞内谷胱甘肽浓度来保护神经元免受葡萄糖诱导的氧化损伤
8. Group II Metabotropic Glutamate Receptors as Potential Pharmaceutical Targets for Neurofibroma Formation [R] . Stern, M. 2011

机译：第II组代谢型谷氨酸受体作为神经纤维瘤形成的潜在药物靶标

The preclinical properties of a novel group II metabotropic glutamate receptor agonist LY379268.

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