Abstract：
:The GABA(B) receptor has been shown to consist of a heterodimer of two related 7-transmembrane receptors GABAB-R1 and GABA(B)-R2. These receptors share close homology to the Ca2+-sensing receptor and also to the metabotropic glutamate receptors, which have also been shown to respond to extracellular calcium. We show here that the GABA(B) receptor also has Ca2+ sensing properties. Ca2+ (0.001-1 mM) potentiated the GABA stimulation of [35S]GTPgammaS binding in membranes prepared from CHO cells stably expressing the GABA(B)-R1/R2 heterodimer. The GABA EC50 was reduced from 72 to 7.7 microM by addition of 1 mM Ca2+, with no change in the maximum response. A similar effect was observed in membranes from rat brain cortex. Ca2+ also potentiated GABA inhibition of forskolin-stimulated cAMP levels in the CHO cells and enhanced coupling to GIRK K+ channels in Xenopus oocytes. Other divalent cations were ineffective. The effects of Ca2+ were found to be agonist dependent with baclofen having a reduced sensitivity compared to GABA. Calcium appears to act allosterically to enhance GABA responses at the GABA(B) receptor, however, unlike the Ca2+-sensing receptor and some of the mGluR family, Ca2+ does not act as a ligand in its own right.
journal_name
Neuropharmacologyjournal_title
Neuropharmacologyauthors
Wise A,Green A,Main MJ,Wilson R,Fraser N,Marshall FHdoi
10.1016/s0028-3908(99)00119-7subject
Has Abstractpub_date
1999-11-01 00:00:00pages
1647-56issue
11eissn
0028-3908issn
1873-7064pii
S0028390899001197journal_volume
38pub_type
杂志文章abstract：:The central nucleus of the amygdala (CeA) is a component of the limbic fear-anxiety circuit, and has also been implicated in regulation of the hypothalamic-pituitary-adrenal (HPA) stress axis. The CeA receives dense noradrenergic innervation, and is rich in expression of alpha(1)-adrenergic receptors. We hypothesized ...
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journal_title：Neuropharmacology
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pub_type： 杂志文章,随机对照试验
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更新日期：2018-12-01 00:00:00
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journal_title：Neuropharmacology
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更新日期：2009-01-01 00:00:00
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journal_title：Neuropharmacology
pub_type： 杂志文章
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更新日期：1985-11-01 00:00:00
