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(RS)-3,5-DHPG
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(RS)-3,5-DHPG图片
包装与价格:
包装价格(元)
1mg电议
10mg电议
50mg电议

产品介绍

DHPG ((RS)-3,5-DHPG) is an amino acid that is a selective potent agonist for group I mGluR (mGluR 1 and mGluR 5) and has no effect on Group II and III mGluR.

Cell lines

MUller cell

Preparation Method

(RS)-3,5-DHPG treatment induced the purification of cultured rat retinal Muller cells.

Reaction Conditions

(RS)-3,5-DHPG (10 μM) for 0.5-24 h.

Applications

(RS)-3,5-DHPG treatment induced down-regulation of Kir4.1 protein in cell membrane compartments of Muller cells.

Animal models

Adult male Sprague Dawley rats (250-280 g)

Preparation Method

To determine mechanisms underlying the effects of (RS)-3,5-DHPG infusion, some animals received two consecutive infusions conducted 10 min apart. Rats in these groups received infusions of ACSF followed by ACSF, ACSF followed by (RS)-3,5-DHPG (50 μmol), ACSF followed by the group I mGluR antagonist MPEP, or MPEP followed by (RS)-3,5-DHPG (50 μmol), ACSF followed by the PKD1 inhibitor followed by (RS)-3,5-DHPG (50 μmol).

Dosage form

50 μmol (RS)-3,5-DHPG for 5 days

Applications

Impairments of spatial memory induced by bilateral infusions of (RS)-3,5-DHPG (50 μmol) into the CA1 area. Dose-dependent changes in spatial memory induced by (RS)-3,5-DHPG infusion. Pre-infusion of MPEP or CID755673 prevented impairments of spatial memory induced by (RS)-3,5-DHPG infusion.

产品描述

DHPG ((RS)-3,5-DHPG) is an amino acid that is a selective potent agonist for group I mGluR (mGluR 1 and mGluR 5) and has no effect on Group II and III mGluR[1,6]. DHPG ((RS)-3,5-DHPG) is also a potent antagonist of mGluRs associated with phospholipase D[2].

(RS)-3,5-DHPG (10μM) treatment induced MUller cell gliosis, as evidenced by enhanced GFAP expression. In addition, (RS)-3,5-DHPG (10 and 100μM) treatment induced a transient decrease in Kir4.1 mRNA expression in the cells. Activation of mGluR I by (RS)-3,5-DHPG may decrease the number of functional Kir4.1 channels in purified cultured rat retinal MUller cells through modulating Kir4.1 protein and mRNA, thus contributing to MUller cell gliosis[5].

Impairments of spatial memory induced by bilateral infusions of (RS)-3,5-DHPG (50 μmol) into the CA1 area. Dose-dependent changes in spatial memory induced by (RS)-3,5-DHPG infusion. Pre-infusion of MPEP or CID755673 prevented impairments of spatial memory induced by (RS)-3,5-DHPG infusion[3]. Hippocampal GPR30 expression was reduced in middle-aged mice compared with young adult mice. a group I metabotropic glutamate receptor (mGluR) agonist (RS)-3,5-DHPG -induced long-term depression in mossy fiber-cornu ammonis 3 (MF-CA3) synapses but not SC-CA1 synapses was facilitated in brain slices from G1-treated middle-aged mice[4]. (RS)-3,5-DHPG elicited acute mechanical allodynia and thermal hyperalgesia in naIve mice from 1 h to 12 h following intrathecal (central/spinal) administration.The attenuation of intrathecal (RS)-3,5-DHPG -evoked acute pain by artesunate therapy in rats[7].

References:
[1]: Winder DG, Conn PJ. Metabotropic glutamate receptor (mGluR)-mediated potentiation of cyclic AMP responses does not require phosphoinositide hydrolysis: mediation by a group II-like mGluR. J Neurochem. 1995 Feb;64(2):592-9. doi: 10.1046/j.1471-4159.1995.64020592.x. PMID: 7830052.
[2]: Pellegrini-Giampietro DE, Torregrossa SA, Moroni F. Pharmacological characterization of metabotropic glutamate receptors coupled to phospholipase D in the rat hippocampus. Br J Pharmacol. 1996 Jun;118(4):1035-43. doi: 10.1111/j.1476-5381.1996.tb15503.x. PMID: 8799579; PMCID: PMC1909512.
[3]: Wang W, Duclot F, et,al. Hippocampal protein kinase D1 is necessary for DHPG-induced learning and memory impairments in rats. PLoS One. 2018 Apr 3;13(4):e0195095. doi: 10.1371/journal.pone.0195095. PMID: 29614089; PMCID: PMC5882104.
[4]: Xu W, Cao J, et,al. GPR30 activation improves memory and facilitates DHPG-induced LTD in the hippocampal CA3 of middle-aged mice. Neurobiol Learn Mem. 2018 Mar;149:10-19. doi: 10.1016/j.nlm.2018.02.005. Epub 2018 Feb 6. PMID: 29421611.
[5]: Gao F, Li F, et,al. Group I metabotropic glutamate receptor agonist DHPG modulates Kir4.1 protein and mRNA in cultured rat retinal MUller cells. Neurosci Lett. 2015 Feb 19;588:12-7. doi: 10.1016/j.neulet.2014.12.048. Epub 2014 Dec 27. PMID: 25549543.
[6]: Ito I, Kohda A, et,al. 3,5-Dihydroxyphenyl-glycine: a potent agonist of metabotropic glutamate receptors. Neuroreport. 1992 Nov;3(11):1013-6. PMID: 1362358.
[7]: Zhang L, Zhao Y, et,al.Artesunate Reduces Remifentanil-induced Hyperalgesia and Peroxiredoxin-3 Hyperacetylation via Modulating Spinal Metabotropic Glutamate Receptor 5 in Rats. Neuroscience. 2022 Apr 1;487:88-98. doi: 10.1016/j.neuroscience.2022.01.003. Epub 2022 Jan 11. PMID: 35026318.