Target intelligence / Profile preview

Monoaminergic neurotransmission

Molecular classification
G protein-coupled receptor, Ion channel, Enzyme, Transporter, Other
01

Overview

Monoaminergic neurotransmission is the physiological process governing the signaling of monoamine neurotransmitters, including dopamine, serotonin, norepinephrine, and histamine, across the central and peripheral nervous systems. Rather than a single target, it constitutes a complex regulatory network composed of metabolic enzymes, vesicular and plasma membrane transporters, and a wide variety of mostly G protein-coupled receptors. This system serves as a master modulator of diverse biological functions such as mood regulation, executive function, motor coordination, sleep-wake cycles, and the reward pathway. Imbalances in monoaminergic signaling are implicated in the etiology of numerous psychiatric and neurological disorders, most notably depression, Parkinson's disease, and schizophrenia. Because of its broad influence, the system is a central pillar of neuropharmacology, targeted by classes such as selective serotonin reuptake inhibitors (SSRIs), monoamine oxidase inhibitors (MAOIs), and antipsychotics. These therapeutic interventions typically aim to restore homeostasis by modulating the synthesis, synaptic concentration, or receptor-mediated effects of these biogenic amines.

Other names
Monoaminergic systemMonoamine neurotransmissionBiogenic amine neurotransmissionMonoaminergic signaling
02

Mechanism of action

Pharmacological modulation of monoaminergic neurotransmission occurs through the inhibition of neurotransmitter reuptake transporters (e.g., SERT, DAT, NET), the inhibition of degradative enzymes (e.g., MAO, COMT), the promotion of neurotransmitter release, or the direct agonism/antagonism of various postsynaptic and presynaptic receptors.

03

Biological functions

Signal transductionMood regulationMotor controlArousalCognitive processingReward processingNociceptionThermoregulationSleep-wake regulation
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Disease associations

Neurodegenerative diseaseInflammationDepressionAnxietySchizophreniaParkinson's diseaseAttention deficit hyperactivity disorder (ADHD)Alzheimer's disease
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Safety considerations

Serotonin syndromeHypertensive crisis (e.g., 'cheese effect' with MAOIs)Extrapyramidal symptomsTardive dyskinesiaAddiction and substance use disorderCardiovascular side effects
06

Interacting drugs

Fluoxetine

8 more in the full profile.

07

Biomarkers

5-Hydroxyindoleacetic acid (5-HIAA)Homovanillic acid (HVA)3-Methoxy-4-hydroxyphenylglycol (MHPG)Cerebrospinal fluid monoamine metabolite levelsPlatelet monoamine oxidase activityDopamine transporter imaging (DaTscan)

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