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Molecular Pharmacology of Promiscuous Seven Transmembrane Receptors Sensing Organic Nutrients
A number of highly promiscuous seven transmembrane (7TM) receptors have been cloned and characterized within the last few years. It is noteworthy that many of these receptors are activated broadly byExpand
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Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors.
Family C of G-protein coupled receptors (GPCRs) from humans is constituted by eight metabotropic glutamate (mGlu(1-8)) receptors, two heterodimeric gamma-aminobutyric acid(B) (GABA(B)) receptors, aExpand
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Molecular cloning, expression, and sequence analysis of GPRC6A, a novel family C G-protein-coupled receptor.
By similarity searching of the human genome sequence using known family C G-protein-coupled receptors (GPCRs) as query sequences, we have identified a putative novel human gene product of unknownExpand
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Molecular basis for amino acid sensing by family C G‐protein‐coupled receptors
Family C of human G‐protein‐coupled receptors (GPCRs) is constituted by eight metabotropic glutamate receptors, two γ‐aminobutyric acid type B (GABAB1–2) subunits forming the heterodimeric GABABExpand
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Deorphanization of GPRC6A: A Promiscuous l-α-Amino Acid Receptor with Preference for Basic Amino Acids
One of the most important tasks of molecular pharmacology is the deorphanization of the large number of G-protein-coupled receptors with unidentified endogenous agonists. We recently reported theExpand
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Potency of GABA at human recombinant GABAA receptors expressed in Xenopus oocytes: a mini review
GABAA receptors are members of the ligand-gated ion channel superfamily that mediate inhibitory neurotransmission in the central nervous system. They are thought to be composed of 2 alpha (α), 2 betaExpand
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GHB receptor targets in the CNS: focus on high-affinity binding sites.
γ-Hydroxybutyric acid (GHB) is an endogenous compound in the mammalian brain with both low- and high-affinity receptor targets. GHB is used clinically in the treatment of symptoms of narcolepsy andExpand
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Delineation of the GPRC6A Receptor Signaling Pathways Using a Mammalian Cell Line Stably Expressing the Receptor
The GPRC6A receptor is a recently “deorphanized” class C G protein–coupled receptor. We and others have shown that this receptor is coactivated by basic l-α-amino acids and divalent cations, whereasExpand
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The rat GPRC6A: cloning and characterization.
GPRC6A is a novel member of family C of G protein-coupled receptors with so far elusive biological function. GPRC6A has been described in human and mouse as a promiscuous l-alpha-amino acid receptor.Expand
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Low nanomolar GABA effects at extrasynaptic α4β1/β3δ GABA(A) receptor subtypes indicate a different binding mode for GABA at these receptors.
Ionotropic GABA(A) receptors are a highly heterogenous population of receptors assembled from a combination of multiple subunits. The aims of this study were to characterize the potency of GABA atExpand
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