G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentration
Definition
Target type: molecularfunction
A G protein-coupled neurotransmitter receptor activity occurring in the postsynaptic membrane, that is involved in regulating the cytosolic concentration of calcium ions in the postsynapse. [GOC:dos]
G protein-coupled neurotransmitter receptors play a crucial role in regulating postsynaptic cytosolic calcium ion concentration, a critical signaling process in neuronal communication. These receptors, embedded in the plasma membrane of postsynaptic neurons, bind to neurotransmitters released from presynaptic neurons. This binding triggers a cascade of events that ultimately lead to changes in intracellular calcium levels.
The process begins with the activation of the G protein-coupled receptor, which is coupled to a heterotrimeric G protein. Upon neurotransmitter binding, the receptor undergoes a conformational change, promoting the exchange of GDP for GTP on the alpha subunit of the G protein. This activation releases the alpha subunit from the beta-gamma dimer, allowing it to interact with downstream effector proteins.
In the context of calcium regulation, the activated alpha subunit often interacts with phospholipase C (PLC), a key enzyme involved in the hydrolysis of phosphatidylinositol 4,5-bisphosphate (PIP2). This hydrolysis generates two second messengers: diacylglycerol (DAG) and inositol trisphosphate (IP3). IP3 binds to receptors on the endoplasmic reticulum (ER), triggering the release of calcium ions from intracellular stores. This release elevates cytosolic calcium concentration, initiating a range of cellular responses.
DAG, on the other hand, activates protein kinase C (PKC), which can phosphorylate various substrates involved in calcium signaling pathways. This phosphorylation can modulate the activity of calcium channels, calcium pumps, and other proteins involved in calcium homeostasis.
The interplay between these signaling components allows G protein-coupled neurotransmitter receptors to exert precise control over postsynaptic calcium levels. These changes in calcium concentration can activate various calcium-dependent signaling pathways, such as the calmodulin-dependent protein kinase (CaMK) pathway, leading to alterations in gene expression, synaptic plasticity, and neuronal excitability.
In summary, G protein-coupled neurotransmitter receptors contribute to the regulation of postsynaptic cytosolic calcium ion concentration by activating a signaling cascade that involves the activation of G proteins, the hydrolysis of PIP2, the release of calcium from intracellular stores, and the modulation of calcium-related proteins. This intricate signaling network plays a vital role in mediating neuronal communication and shaping neuronal function.'
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Proteins (1)
| Protein | Definition | Taxonomy |
|---|---|---|
| Metabotropic glutamate receptor 1 | A metabotropic glutamate receptor 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13255] | Homo sapiens (human) |
Compounds (49)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| alpha-methyl-4-carboxyphenylglycine | |||
| ibotenic acid | Ibotenic Acid: A neurotoxic isoxazole (similar to KAINIC ACID and MUSCIMOL) found in AMANITA mushrooms. It causes motor depression, ataxia, and changes in mood, perceptions and feelings, and is a potent excitatory amino acid agonist. | non-proteinogenic alpha-amino acid | neurotoxin |
| 4-carboxy-3-hydroxyphenylglycine | 4-carboxy-3-hydroxyphenylglycine: weak agonist at metabotropic glutamate receptors; occludes the action of 1-aminocyclopentyl-1,3-dicarboxylate in hippocampus | hydroxybenzoic acid | |
| 1-aminoindan-1,5-dicarboxylic acid | 1-aminoindan-1,5-dicarboxylic acid: structure given in first source | ||
| 4-carboxyphenylglycine | 4-carboxyphenylglycine: RN given for (+-)-isomer; RN for cpd without isomeric designation not available 3/93; glutamate receptor antagonist | alpha-amino acid | |
| aspartic acid | aspartic acid : An alpha-amino acid that consists of succinic acid bearing a single alpha-amino substituent Aspartic Acid: One of the non-essential amino acids commonly occurring in the L-form. It is found in animals and plants, especially in sugar cane and sugar beets. It may be a neurotransmitter. L-aspartic acid : The L-enantiomer of aspartic acid. | aspartate family amino acid; aspartic acid; L-alpha-amino acid; proteinogenic amino acid | Escherichia coli metabolite; mouse metabolite; neurotransmitter |
| d-glutamate | D-alpha-amino acid; glutamic acid | Escherichia coli metabolite; mouse metabolite | |
| glutamic acid | glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2. Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM. | glutamic acid; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | Escherichia coli metabolite; ferroptosis inducer; micronutrient; mouse metabolite; neurotransmitter; nutraceutical |
| quisqualic acid | Quisqualic Acid: An agonist at two subsets of excitatory amino acid receptors, ionotropic receptors that directly control membrane channels and metabotropic receptors that indirectly mediate calcium mobilization from intracellular stores. The compound is obtained from the seeds and fruit of Quisqualis chinensis. | non-proteinogenic alpha-amino acid | |
| 1-amino-1,3-dicarboxycyclopentane, (trans)-isomer | |||
| d-aspartic acid | aspartic acid; D-alpha-amino acid | mouse metabolite | |
| L-2-aminoadipic acid | L-2-aminoadipic acid : The L-enantiomer of 2-aminoadipic acid. | 2-aminoadipic acid | Escherichia coli metabolite; human metabolite |
| alpha-aminopimelic acid | 2-aminopimelic acid : An amino dicarboxylic acid that is heptanedioic acid in which a hydrogen at position 2 is replaced by an amino group. It is a component of the cell wall peptidoglycan of bacteria. alpha-aminopimelic acid: antagonizes glutamate-induced inhibitions of Helix neurones | amino dicarboxylic acid; non-proteinogenic alpha-amino acid | bacterial metabolite |
| 1-amino-1,3-dicarboxycyclopentane | 1-amino-1,3-dicarboxycyclopentane: RN given refers to (cis)-isomer | ||
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | |||
| philanthotoxin 343 | philanthotoxin 343: structure given in first source (see article's footnote); identical to philanthotoxin 433 except that the number of methylene groups between the respective amine moieties is 3,4,3 instead of 4,3,3 | N-acyl-amino acid | |
| alpha-amino-3-(hydroxy)-5-methyl-4-isoxazoleacetic acid | alpha-amino-3-(hydroxy)-5-methyl-4-isoxazoleacetic acid: RN given refers to cpd without isomeric designation; structure given in first source | ||
| homocysteic acid | homocysteic acid : A non-proteinogenic alpha-amino acid that is homocysteine in which the thiol group has benn oxidised to the corresponding sulfonic acid. homocysteic acid: promotes growth in hypophysectomized rats; RN given refers to parent cpd L-homocysteic acid : A homocysteic acid with L-configuration. | homocysteic acid | NMDA receptor agonist |
| 2-amino-4-phosphonobutyric acid | (2S)-2-amino-4-phosphonobutanoic acid : A non-proteinogenc L-alpha-amino acid that is L-alpha-aminobutyric acid in which one of the hydrogens of the terminal methyl group has been replaced by a dihydroxy(oxido)-lambda(5)-phosphanyl group. It is a potent and selective agonist for the group III metabotropic glutamate receptors (mGluR4/6/7/8). | non-proteinogenic L-alpha-amino acid; phosphonic acids | metabotropic glutamate receptor agonist |
| eglumetad | eglumetad: LY-354740 is the active isomer, LY-366563 is the inactive isomer, and LY 314582 is the racemate; structure given in first source | L-alpha-amino acid | |
| 3,5-dihydroxyphenylglycine | (S)-3,5-dihydroxyphenylglycine : A glycine derivative that is L-alpha-phenylglycine substituted at positions 3 and 5 on the phenyl ring by hydroxy groups. | amino acid zwitterion; non-proteinogenic L-alpha-amino acid; resorcinols | |
| alpha-methyl-4-carboxyphenylglycine | (S)-alpha-methyl-4-carboxyphenylglycine : A non-proteinogenic alpha-amino acid that is alanine in which the alpha-hydrogen is replaced by a 4-carboxyphenyl group (the S-enantiomer). It is a non-selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. alpha-methyl-4-carboxyphenylglycine: glutamate receptor antagonist | non-proteinogenic alpha-amino acid | metabotropic glutamate receptor antagonist |
| 9-(dimethylamino)-3-(4-methoxyphenyl)-4-pyrido[1,2]thieno[3,4-d]pyrimidinone | organic heterobicyclic compound; organonitrogen heterocyclic compound; organosulfur heterocyclic compound | ||
| 4-bromohomoibotenic acid, (rs)-isomer | |||
| 6-methyl-2-(phenylethynyl)pyridine | 2-methyl-6-(phenylethynyl)pyridine : A methylpyridine that coinsists of 2-methylp[yridine bearing an additional phenylethynyl group at position 6. Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw. 6-methyl-2-(phenylethynyl)pyridine: an mGlu5 antagonist | acetylenic compound; methylpyridines | anxiolytic drug; metabotropic glutamate receptor antagonist |
| 4-methylglutamic acid, threo-(l)-isomer | |||
| sib 1757 | SIB 1757: a selective mGluR5 antagonist; structure in first source | ||
| l-2-(carboxypropyl)glycine | |||
| 2-(2,3-dicarboxycyclopropyl)glycine | |||
| 2r,4r-4-aminopyrrolidine-2,4-dicarboxylate | pyrrolidinedicarboxylic acid | ||
| upf 596 | UPF 596: structure in first source | ||
| ly-367385 | |||
| sib 1893 | SIB 1893: a selective mGluR5 antagonist; structure in first source | ||
| 4-carboxy-3-hydroxyphenylglycine | |||
| 1-amino-1,3-dicarboxycyclopentane, cis-(1s,3s)-isomer | |||
| ampa, (r)-isomer | |||
| 1-aminocyclopentane-1,3,4-tricarboxylic acid | 1-aminocyclopentane-1,3,4-tricarboxylic acid: metabolic glutamate receptor (mGluR) antagonist; structure in first source | ||
| 3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidine | 3-((2-methyl-1,3-thiazol-4-yl)ethynyl)piperidine: an excitatory amino acid antagonist | ||
| ly 341495 | xanthenes | ||
| mgs 0028 | MGS 0028: a group II mGluR agonist; structure in first source | ||
| bay36-7620 | BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity. ; structure in first source | ||
| ly 389795 | LY 389795: a group II metabotropic glutamate receptor agonist; structure in first source | ||
| ly 379268 | LY 379268 : An organic heterobicyclic compound that is (1R,5S)-2-oxabicyclo[3.1.0]hexane carrying amino, carboxy, and carboxy groups at positions 4R, 4R and 6R, respectively. It is a potent agonist of group II metabotropic glutamate receptors mGluR2 and mGluR3 (EC50 = 2.69 nM and 4.48 nM, respectively) that exhibits antipsychotic-like action in animal models of schizophrenia. LY 379268: group II metabotropic glutamate receptor agonist; structure in first source | amino dicarboxylic acid; bridged compound; organic heterobicyclic compound | antipsychotic agent; anxiolytic drug; metabotropic glutamate receptor agonist; neuroprotective agent |
| r 214127 | R 214127: an mGlu1 receptor ligand; structure in first source | ||
| jnj16259685 | organic heterotricyclic compound; organonitrogen heterocyclic compound; oxacycle | ||
| a 794282 | |||
| a-841720 | A-841720: structure in first source | ||
| sp 203 | 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile: a radioligand for mGlu5 receptor; structure in first source | ||
| fenobam | fenobam: in USAN fenobam refers to monohydrate | ureas |