5-HT1B receptor

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5-HT1B receptor is a subtype of 5-HT receptor that binds the neurotransmitter serotonin, also known as 5-hydroxytryptamine (5-HT). It is a G protein-coupled receptor (GPCR) that is coupled to Gi/Go proteins and is expressed in various regions of the human brain, including the basal ganglia, hippocampus, and cerebral cortex.

Function[edit | edit source]

The 5-HT1B receptor plays a crucial role in the modulation of serotonin release. It acts as an autoreceptor on the presynaptic neuron, inhibiting the release of serotonin, and as a heteroreceptor, modulating the release of other neurotransmitters such as dopamine and GABA. This receptor is involved in a variety of physiological and neurological processes, including aggression, anxiety, appetite, cognition, learning, memory, and thermoregulation.

Pharmacology[edit | edit source]

Several drugs target the 5-HT1B receptor to treat various conditions. Agonists of this receptor, such as sumatriptan and zolmitriptan, are used in the treatment of migraine and cluster headache. Antagonists of the 5-HT1B receptor, such as SB-216641 and NAS-181, are being investigated for their potential use in the treatment of depression and anxiety disorders.

Genetics[edit | edit source]

The 5-HT1B receptor is encoded by the HTR1B gene located on chromosome 6 in humans. Variations in this gene have been associated with various psychiatric disorders, including major depressive disorder, bipolar disorder, schizophrenia, and substance use disorder.

See also[edit | edit source]

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Contributors: Prab R. Tumpati, MD