Abstract：
:The metabotropic glutamate receptor subtype 5 (mGlu5) and glutamatergic neurotransmission are associated with the pathophysiology of disorders such as anxiety, depression or chronic pain. Human and rat mGlu5 receptors have been cloned and characterized previously. We now describe the cloning of the mouse mGlu5b receptor gene from adult mouse brain and its expression using an ecdysone-inducible system. This subtype has an extra 96 bp sequence which is inserted to the cytoplasmic tail and is identical to the insert present in human and rat mGlu5b. Mouse mGlu5b receptor expression was induced in HEK-293EcR cells by incubation with ponasterone A, an analogue of the insect hormone ecdysone. A fluorometric calcium transient assay system was used to characterize the basic pharmacologic profile of an isolated stable cell line. Quisqualic acid was the most potent receptor agonist (EC(50) approximately 7 nM) although the cells also responded to l-glutamic acid and the Group I-selective receptor agonist, 3,5-dihydroxyphenylglycine (3,5-DHPG). The calcium transients stimulated by these agonists were potently inhibited by reference allosteric mGlu5 antagonists - 2-methyl-6-(phenylethynyl)pyridine (MPEP), 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine (MTEP) and 3-methoxy-5-(pyridine-2-ylethynyl)pyridine (methoxy-PEPy) (IC(50) ranges: 0.8-66 nM). The availability of this mouse mGlu5b receptor-expressing cell line will facilitate in vitro characterization of mGlu5 receptor-selective agonists or antagonists prior to in vivo pharmacologic testing.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Salisbury BG,Mukhopadhyay G,Kostich M,Laz TM,Norris EDdoi
10.1016/j.ejphar.2007.10.004subject
Has Abstractpub_date
2008-01-28 00:00:00pages
34-9issue
1-3eissn
0014-2999issn
1879-0712pii
S0014-2999(07)01104-1journal_volume
579pub_type
杂志文章abstract：:The contribution of tyrosine kinase activity to vasoreactivity in normotensive Wistar-Kyoto (WKY) and spontaneously hypertensive (SHR) rats was investigated on isolated aortic preparations by the use of two tyrosine kinase inhibitors: methyl-2,5-dihydroxycinnamate (30 microM) and genistein (30 microM). The pretreatmen...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00304-0
更新日期：1999-06-11 00:00:00
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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doi：10.1016/j.ejphar.2017.05.027
更新日期：2017-08-15 00:00:00
abstract：:Diabetic osteopenia can result in an increased incidence of bone fracture and a delay in fracture healing. Quercetin, one of the most widely distributed flavonoids in plants, possesses antioxidant property and beneficial effect on osteoporosis in ovariectomized mice. All these properties make quercetin a potential can...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2011.08.014
更新日期：2011-11-16 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90280-7
更新日期：1978-12-01 00:00:00
abstract：:Preeclampsia is reported in pregnant women around the world and often causes maternal/fetal mortality and morbidity. In the current study, we assessed the efficacy of celastrol on a rat preeclampsia model induced by Nω-nitro-L-arginine methyl ester hydrochloride (L-NAME). Pregnant rats were administered L-NAME to esta...
journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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更新日期：1992-11-24 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2009.11.051
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90125-n
更新日期：1992-04-22 00:00:00
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(91)90055-m
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
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journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90025-0
更新日期：1978-11-01 00:00:00
abstract：:Clinically, dexamethasone is known to reduce cerebral edema. To further investigate the mechanism of this neuroprotection, an in vitro model of brain-derived microvessel endothelial cells (BME cells) was used to investigate the effect of dexamethasone on hypoxia-induced hyperpermeability. Furthermore, the expression o...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(00)00915-8
更新日期：2001-01-12 00:00:00
