Target intelligence / Profile preview

Serotonin and Dopamine Receptors

Molecular classification
G protein-coupled receptor (majority of both families; see below for exception), Ligand-gated ion channel (for serotonin 5-HT3 receptor only)
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Overview

Serotonin and dopamine receptors are two major classes of neurotransmitter receptors in the central and peripheral nervous systems, primarily responsible for mediating the actions of the monoamines serotonin and dopamine. The serotonin receptor family (5-HT receptors) consists of at least 14 different subtypes, most of which are G protein-coupled receptors except for the 5-HT3 receptor, which is a ligand-gated ion channel. The dopamine receptor family comprises five well-characterized subtypes (D1–D5), all belonging to the G protein-coupled receptor superfamily. Both receptor systems are involved in mood regulation, cognition, behavior, reward, motor activity, and neuroendocrine signaling. These receptors are key therapeutic targets for drugs used in psychiatry and neurology, as well as for drugs of abuse. The close interaction between these systems underlies the pharmacology of many current antipsychotics and antidepressants, and dysregulation of these receptors has been strongly linked to psychiatric and neurological conditions.

Other names
5-HT and dopamine receptorsSerotonin (5-HT) receptors and Dopamine receptorsMonoaminergic receptors
02

Mechanism of action

Agonism or antagonism of G protein-coupled receptors (signal modulation through cAMP, IP3, DAG, second messengers) Blockade or stimulation of postsynaptic or presynaptic receptors affecting neuronal firing and neurotransmitter release Inhibition or activation of ligand-gated ion channel (for 5-HT3) Modulation of dopaminergic or serotonergic tone to impact neural circuits associated with mood, cognition, and behavior

03

Biological functions

Signal transductionNeurotransmissionModulation of mood, cognition, reward, and motor functions
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Disease associations

Neuropsychiatric disorders (including depression, schizophrenia, anxiety)Neurodegenerative diseases (Parkinson's disease)Addiction and substance use disordersOther CNS disorders
05

Safety considerations

Extrapyramidal symptoms and movement disorders (dopamine antagonists)Serotonin syndrome (serotonin agonists/SSRIs)Cardiac arrhythmias (some 5-HT2B, 5-HT3 modulators)Metabolic syndrome/weight gain (some antipsychotics)Potential for abuse (psychostimulants, dopamine agonists)
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Interacting drugs

Antipsychotics (e.g., haloperidol, clozapine, risperidone)

5 more in the full profile.

07

Biomarkers

5-HIAA (serotonin metabolite) in CSF or urine (serotonin function)DAT, SERT PET imaging (dopamine/serotonin transporter density)D2 receptor occupancy for antipsychotic efficacy

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