Neurotransmitter G Protein-Coupled Receptors

Neurotransmitter G Protein-Coupled Receptors Background

About Neurotransmitter G Protein-Coupled Receptors

Neurotransmitters GPCRs are a large family of receptors activated by a variety of neurotransmitters, including dopamine, serotonin, acetylcholine, and gamma-aminobutyric acid (GABA). They are integral to the regulation of synaptic transmission and are involved in the regulation of neuronal excitability, synaptic plasticity, and other cellular processes in the central and peripheral nervous system.

Depending on the localization of individual GPCRs in neurons, these receptors can function as autoreceptors to reduce neurotransmitter release, forming extrasynaptic or intersynaptic negative feedback loops to regulate neurotransmission at presynaptic terminals. Neurotransmitters released from presynaptic terminals bind to postsynaptic GPCRs and activate various distinct G protein-signaling pathways. Activation of G protein-signaling, directly or indirectly, has been shown to modulate cytoplasmic Ca2+ levels, which leads to membrane hyperpolarization and depolarization and contributes to synaptic excitation or inhibition. GPCR signaling also induces cAMP response element-binding protein (CREB) activation, leading to gene transcription and changes in synaptic plasticity.

Mechanism of Action of Neurotransmitter G Protein-Coupled Receptors

The mechanism of action of the neurotransmitter GPCR involves the following key steps:

  1. Ligand Binding and Receptor Activation: Neurotransmitter GPCRs are activated by specific neurotransmitters (e.g., dopamine, 5-hydroxytryptamine, etc.) bound to their extracellular domains. This binding induces a conformational change in the receptor, which activates intracellular signaling pathways.
  2. G Protein Coupling and Signaling: The activated neurotransmitter GPCR interacts with heterotrimeric G proteins composed of α, β, and γ subunits. This interaction promotes the exchange of GDP for GTP on the Gα subunit, leading to dissociation of the Gα subunit from the βγ subunit. The Gα subunit and/or βγ subunit can then modulate the activity of downstream effector molecules such as adenylate cyclase, phospholipase C, or ion channels.
  3. Second Messenger Production and Cellular Responses: Activation of the neurotransmitter GPCR leads to the production of second messengers such as cyclic adenosine monophosphate (cAMP), inositol triphosphate (IP3) and diacylglycerol (DAG). These second messengers can trigger a variety of intracellular signaling cascades that lead to changes in cellular processes, including gene expression, ion channel activity, neurotransmitter release, and synaptic plasticity.

Neurotransmitter G Protein-Coupled Receptors - Creative BioMart

Functions of Neurotransmitter G Protein-Coupled Receptors

Neurotransmitter G protein-coupled receptors are involved in the regulation of a variety of physiological and pathological processes, including but not limited to:

Neurotransmission: neurotransmitter GPCRs are key regulators of synaptic transmission. They regulate the release, synthesis, and reuptake of neurotransmitters, thereby affecting the strength and duration of neural signals.

Neuronal Excitability and Synaptic Plasticity: Neurotransmitter GPCRs play a crucial role in regulating neuronal excitability and synaptic plasticity, which are essential for learning, memory, and cognitive function. They modulate the strength of synaptic connections and contribute to long-term potentiation (LTP) or long-term depression (LTD) processes.

Neurological and Psychiatric Disorders: Dysfunction of the neurotransmitter GPCRs has been linked to a variety of neurological and psychiatric disorders, including Parkinson's disease, schizophrenia, depression, and anxiety disorders. Targeting these receptors with selective ligands offers potential therapeutic opportunities for the treatment of these disorders.

Mood Regulation and Cognitive Function: They are important in the study of mood disorders such as depression and anxiety.

Motor Coordination: They play a key role in the pathogenesis of movement disorders such as Parkinson's disease.

Drug Target: The target of many neurological drugs is the neurotransmitter G protein-coupled receptor, such as antipsychotics and antidepressants.

Available Resources for Neurotransmitter G Protein-Coupled Receptors

Neurotransmitter G protein-coupled receptors are important components of neural signaling and neurotransmission. They have multiple functions in the regulation of synaptic transmission, neuronal excitability, and synaptic plasticity. Creative BioMart offers a wide range of products and services related to neurotransmitter GPCR, including recombinant proteins, cell and tissue lysates, protein pre-coupled magnetic beads, assay kits, and customized services to support researchers in the study of these receptors and their involvement in various biological processes. These resources provide valuable tools for understanding the mechanism of action and function of neurotransmitter GPCRs and their potential impact on neurological and psychiatric disorders. The following neurotransmitter G protein-coupled receptors are displayed, click to view all related molecules/targets and research reagents. Please feel free to contact us with any questions or requests.


  1. Betke KM, Wells CA, Hamm HE. GPCR mediated regulation of synaptic transmission. Prog Neurobiol. 2012;96(3):304-321.
  2. Huang Y, Thathiah A. Regulation of neuronal communication by G protein-coupled receptors[J]. FEBS Letters, 2016, 589(14):1607-1619.
  3. Boczek T, Mackiewicz J, Sobolczyk M, et al. The Role of G Protein-Coupled Receptors (GPCRs) and Calcium Signaling in Schizophrenia. Focus on GPCRs Activated by Neurotransmitters and Chemokines[J]. Cells, 2021, 10(5):1228. DOI:10.3390/cells10051228.


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