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I 型和 II 型选择性代谢型谷氨酸受体激动剂对新生大鼠大脑皮层磷酸肌醇代谢的调节

Regulation of phosphoinositide turnover in neonatal rat cerebral cortex by group I- and II- selective metabotropic glutamate receptor agonists.

作者信息

Mistry R, Golding N, Challiss R A

机构信息

Department of Cell Physiology and Pharmacology, University of Leicester.

出版信息

Br J Pharmacol. 1998 Feb;123(3):581-9. doi: 10.1038/sj.bjp.0701626.

Abstract
  1. The interactive effects of different metabotropic glutamate (mGlu) receptor subtypes to regulate phosphoinositide turnover have been studied in neonatal rat cerebral cortex and hippocampus by use of agonists and antagonists selective between group I and II mGlu receptors. 2, The group II-selective agonist 2R,4R-4-aminopyrrolidine-2,4-dicarboxylate (2R,4R-APDC; 100 microM) had no effect on basal total inositol phosphate ([3H]-InsPx) accumulation (in the presence of Li+) in myo-[3H]-inositol pre-labelled slices, but enhanced the maximal [3H]-InsPx response to the group I-selective agonist (S)-3,5-dihydroxyphenylglycine (DHPG) by about 100% in both hippocampus and cerebral cortex. In cerebral cortex the enhancing effect of 2R,4R-APDC occurred with respect to the maximal responsiveness and had no effect on EC50 values for DHPG (-log EC50 (M): control, 5.56+/-0.05; +2R,4R-APDC, 5.51+/-0.08). 2R,4R-APDC also caused a significant enhancement of the DHPG-stimulated inositol 1,4,5-trisphosphate (Ins(1,4,5)P3) mass response over an initial 0-300 s time-course. 3. The enhancing effects of 2R,4R-APDC on DHPG-stimulated [3H]-InsPx accumulation were observed in both the presence and nominal absence of extracellular Ca2+, and irrespective of whether 2R,4R-APDC was added before, simultaneous with, or subsequent to DHPG. Furthermore, increasing the tissue cyclic AMP concentration up to 100 fold had no effect on DHPG-stimulated Ins(l,4,5)P3 accumulation in the absence or presence of 2R,4R-APDC. 4. 2R,4R-APDC and (2S, 1'R, 2'R, 3'R)-2-(2,3-dicarboxylcyclopropyl)glycine (DCG-IV), the latter agent in the presence of MK-801 to prevent activation of NMDA-receptors, each inhibited forskolin-stimulated cyclic AMP accumulation by about 50%, with respective EC50 values of 1.3 and 0.04 microM (-log EC 50 (M): 2R,4R-APDC, 5.87+/-0.09; DCG-IV, 7.38+/-0.05). In the presence of DHPG (30 microM), 2R,4R-APDC and DCG-IV also concentration-dependently increased [3H]-InsPx accumulation with respective EC50 values of 4.7 and 0.28 microM (-log EC50 (M): 2R,4R-APDC, 5.33+/-0.04; DCG-IV, 6.55+/-0.09) which were 3-7 fold rightward-shifted relative to the adenylyl cyclase inhibitory responses. 5. The group II-selective mGlu receptor antagonist LY307452 (30 microM) caused parallel rightward shifts in the concentration-effect curves for inhibition of forskolin-stimulated adenylyl cyclase, and enhancement of DHPG-stimulated [3H]-InsPx accumulation, by 2R,4R-APDC yielding similar equilibrium dissociation constants (KdS, 3.7+/-1.1 and 4.1+/-0.4 microM respectively) for each response. 6. The ability of 2R,4R-APDC to enhance receptor-mediated [3H]-InsPx accumulation appeared to be agonist-specific; thus although DHPG (100 microM) and the muscarinic cholinoceptor agonist carbachol (10 microM) stimulated similar [3H]-InsPx accumulations, only the response to the former agonist was enhanced by co-activation of group II mGlu receptors. 7. These data demonstrate that second messenger-generating phosphoinositide responses stimulated by group I mGlu receptors are positively modulated by co-activation of group II mGlu receptors in cerebral cortex and hippocampus. The data presented here are discussed with respect to the possible mechanisms which might mediate the modulatory activity, and the physiological and pathophysiological significance of such crosstalk between mGlu receptors.
摘要
  1. 利用I组和II组代谢型谷氨酸(mGlu)受体之间具有选择性的激动剂和拮抗剂,在新生大鼠大脑皮层和海马体中研究了不同mGlu受体亚型调节磷酸肌醇代谢的相互作用。2. II组选择性激动剂2R,4R-4-氨基吡咯烷-2,4-二羧酸(2R,4R-APDC;100微摩尔)对用肌醇-[3H]预标记切片中基础总肌醇磷酸([3H]-InsPx)积累(在Li+存在下)无影响,但在海马体和大脑皮层中均使对I组选择性激动剂(S)-3,5-二羟基苯甘氨酸(DHPG)的最大[3H]-InsPx反应增强约100%。在大脑皮层中,2R,4R-APDC的增强作用发生在最大反应性方面,对DHPG的EC50值无影响(-log EC50(M):对照组,5.56±0.05;+2R,4R-APDC,5.51±0.08)。在最初0 - 300秒的时间进程中,2R,4R-APDC还使DHPG刺激的肌醇1,4,5-三磷酸(Ins(1,4,5)P3)质量反应显著增强。3. 在细胞外Ca2+存在和名义上不存在的情况下,均观察到2R,4R-APDC对DHPG刺激的[3H]-InsPx积累的增强作用,且与2R,4R-APDC是在DHPG之前、同时还是之后添加无关。此外,将组织环磷酸腺苷浓度提高到100倍,在不存在或存在2R,4R-APDC的情况下,对DHPG刺激的Ins(1,4,5)P3积累均无影响。4. 2R,4R-APDC和(2S,1'R,2'R,3'R)-2-(2,3-二羧基环丙基)甘氨酸(DCG-IV),后者在MK-801存在下以防止NMDA受体激活,各自使福斯可林刺激的环磷酸腺苷积累抑制约50%,各自的EC50值为1.3和0.04微摩尔(-log EC50(M):2R,4R-APDC,5.87±0.09;DCG-IV,7.38±0.05)。在DHPG(30微摩尔)存在下,2R,4R-APDC和DCG-IV也浓度依赖性地增加[3H]-InsPx积累,各自的EC50值为4.7和0.28微摩尔(-log EC50(M):2R,4R-APDC,5.33±0.04;DCG-IV,6.55±0.

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