5-HT receptor

5-HT Receptor

Structure of a 5-HT receptor

The 5-HT receptors, also known as serotonin receptors, are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels found in the central nervous system and peripheral nervous system. They mediate the effects of the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT) and are involved in various physiological processes, including mood regulation, anxiety, and the modulation of neurotransmitter release.

Classification

5-HT receptors are classified into seven families, designated 5-HT₁ to 5-HT₇. Each family contains multiple subtypes, which are further distinguished by their pharmacological properties, molecular structure, and signaling mechanisms.

5-HT₁ Receptors

The 5-HT₁ receptor family includes several subtypes, such as 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT_1E, and 5-HT_1F. These receptors are primarily coupled to Gi/Go proteins, which inhibit adenylate cyclase activity, leading to decreased levels of cyclic AMP (cAMP).

• 5-HT_1A Receptor: This subtype is involved in the regulation of mood and anxiety. It is a target for several antidepressant and anxiolytic drugs.

• 5-HT_1D Receptor: This receptor is implicated in the modulation of migraine headaches and is a target for certain triptan medications.

• 5-HT_1E Receptor: The function of this receptor is less well understood, but it is believed to play a role in the central nervous system.

• 5-HT_1F Receptor: This receptor is also involved in the treatment of migraines and is a target for newer triptan drugs.

5-HT₂ Receptors

The 5-HT₂ receptor family includes 5-HT_2A, 5-HT_2B, and 5-HT_2C receptors. These receptors are coupled to Gq proteins, which activate phospholipase C, leading to increased levels of inositol trisphosphate (IP3) and diacylglycerol (DAG).

5-HT₃ Receptors

The 5-HT₃ receptor is unique among serotonin receptors as it is a ligand-gated ion channel. It is involved in the modulation of nausea and vomiting, particularly in response to chemotherapy.

5-HT₄ to 5-HT₇ Receptors

These receptors are involved in various functions, including gastrointestinal motility, cognition, and circadian rhythm regulation. They are coupled to different G proteins, leading to diverse signaling pathways.

Function

5-HT receptors play a crucial role in the modulation of neurotransmitter release, influencing the activity of dopamine, norepinephrine, and acetylcholine. They are involved in the regulation of mood, anxiety, appetite, and sleep, and are targets for a variety of pharmacological agents used in the treatment of depression, anxiety disorders, and schizophrenia.

Pharmacology

Many drugs target 5-HT receptors, including antidepressants, antipsychotics, and antiemetics. The selective targeting of specific 5-HT receptor subtypes allows for the modulation of specific physiological responses, minimizing side effects.

Related Pages

• Serotonin
• G protein-coupled receptor
• Neurotransmitter
• Antidepressant

Gallery

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  5-HT_1A receptor structure

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  5-HT_1D receptor structure

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  5-HT_1E receptor structure

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  5-HT_1F receptor structure

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  5-HT receptor

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  5-HT1A receptor bound to serotonin

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  5-HT1D receptor

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  5-HT1E receptor

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  5-HT1F receptor