Serotonin GPCR Family Subtypes and Products

What Are Serotonin Receptors?

Serotonin (5-HT) receptors are a family of G protein-coupled receptors (GPCRs) comprised of seven subclasses of receptors: 5-HT1, with five subtypes, 5-HT2, with three subtypes, 5-HT3, 5-HT4, 5-HT5, with two subtypes, 5-HT6, and 5-HT7. Serotonin receptors play a large role in a variety of neurological processes, such as mood, appetite, learning, nausea, sleep, and memory, and are a major target for pharmaceutical and recreational drugs. 5-HT receptor agonists currently have pharmacological utility in treating anxiety, migraines, and constipation, while 5-HT receptor antagonists are used in the treatment of nausea, IBS, and psychotic disorders.

Click here to view more information about this particular family, including specific subtype information.

Serotonin Receptor Information

Clickable Text Interaction

5-HT1A

5-HT1B

5-HT2A

5-HT2B

5-HT2C

5-HT4A/B/D

5-HT6

5-HT7

The human serotonin receptor 5-HT1A is a G protein-coupled receptor. 5-HT1A receptors can be found mainly in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucelus, with lesser amounts in the basal ganglia and thalamus. 5-HT1A ligands may prove to be therapeutic in the treatment of various disorders such as depression, anxiety, and schizophrenia.

The human serotonin receptor 5-HT1B is a G protein-coupled receptor. 5-HT1B receptors are present in many parts of the central nervous system, but most notably, can be found in the basal ganglia, striatum, and frontal cortex. 5- HT1B receptors inhibit the release of many neurotransmitters, such as serotonin, GABA, acetylcholine, and glutamate. 5-HT1B ligands may prove to be therapeutic in the treatment of various disorders such as depression, anxiety, and aggression.

5-HT2A (5-hydroxytryptamine receptor 2A) is a receptor for serotonin. It is expressed throughout the central nervous system in the neocortex and olfactory tubercle. Additionally, it is expressed in platelets, fibroblasts and neurons of the peripheral nervous system. 5-HT2A receptor agonists may have important clinical value in the treatment of various disorders, such as depression, anxiety, bipolar disorder and schizophrenia. It is also a receptor for the human polyomavirus, JC virus.

5-HT2B (5-hydroxytryptamine receptor 2B) is a receptor for serotonin. It is expressed in many peripheral and central nervous system tissues, including stomach fundus, liver kidney, muscle, intestine and brain. 5-HT2B receptors are responsible for many cardiovascular and central nervous system functions, such as blood vessel contraction, platelet shape changes, neuronal sensitization to tactile stimuli, and mediation of the hallucinogenic effects of phenylisopropylamin hallucinogens. It has also been shown to be required for heart development.

5-HT2C (5-hydroxytryptamine receptor 2C) is a receptor for serotonin. It is expressed in the brain and spinal cord, especially the choroid plexus. 5-HT2C receptor agonists may have important clinical value in the treatment of mental and eating disorders, such as depression, panic anxiety, OCD, bulimia and obesity.

The human serotonin receptor 5-HT4 is a G protein-coupled receptor. 5-HT4 receptors can be found in the central nervous system and in peripheral tissues such as the alimentary tract, urinary bladder, heart and adrenal gland. 5-HT4 ligands may prove to be therapeutic in the treatment of disorders such as cardiac arrhythmias, irritable bowel syndrome and urinary incontinence.

Human 5-HT6 receptors are G protein-coupled receptors. The cDNA encodes a 440-amino-acid polypeptide. The 5-HT6 receptors are expressed exclusively in brain regions such as striatum, cortex, nucleus accumbens, olfactory tubercle, hippocampus, hypothalamus, amygdala and cerebellum. The 5-HT6 receptors appear to regulate GABAergic, glutamatergic and cholinergic neurotransmission and are involved in the regulation of cognition, feeding and sleep/wake regulation. They may also play a role in mediating the effects of some antipsychotic agents, and in modulating sensory gating which is often affected in schizophrenic patients.

The 5-HT7 receptor is a member of the GPCR superfamily of cell surface receptors and is activated by the neurotransmitter serotonin. The 5-HT7 receptor is expressed in a variety of tissues, particularly in the brain, the gastrointestinal tract, and various blood vessels. The 5-HT7 receptor plays a role in smooth muscle relaxation within the vasculature and in the gastrointestinal tract, and is involved in thermoregulation, circadian rhythm, learning and memory, and sleep. This receptor is also involved in mood regulation, suggesting that it may be a useful target in the treatment of depression.

Serotonin Cell Lines

Receptor Family	Receptor	Species	Parental	Stable Cell Lines	Division-Arrested Cells	Membranes
Serotonin	5-HT1A	human	HEK293T	C1319	DC1319	MC1319
	5-HT1A	human	HEK293T	C1319a	DC1319a	MC1319a
	5-HT1B	human	HEK293T	C1320	DC1320	MC1320
	5-HT1B	human	HEK293T	C1320a	DC1320a	MC1320a
	5-HT1B	human	HEK293T Gαqi5	CG1320	DCG1320	MCG1320
	5-HT2A	human	CHO-K1	C1324-1	DC1324-1	MC1324-1
	5-HT2A	mouse	HEK293T	Cm1324	DCm1324	MCm1324
	5-HT2A	mouse	CHO-K1	Cm1324-1	DCm1324-1	MCm1324-1
	5-HT2A	dog	HEK293T	Cd1324	DCd1324	MCd1324
	5-HT2B	human	CHO-K1	C1325-1	DC1325-1	MC1325-1
	5-HT2B	human	HEK293T	C1325	DC1325	MC1325
	5-HT2B	mouse	HEK293T	Cm1325	DCm1325	MCm1325
	5-HT2C	human	CHO-K1	C1326-1	DC1326-1	MC1326-1
	5-HT4A	human	CHO-K1	C1518-1	DC1518-1	MC1518-1
	5-HT4A	mouse	CHO-K1	Cm1518-1	DCm1518-1	MCm1518-1
	5-HT4B	human	CHO-K1	C1330-1	DC1330-1	MC1330-1
	5-HT4B	human	HEK293T	C1330	DC1330	MC1330
	5-HT4D	human	CHO-K1	C1520-1	DC1520-1	MC1520-1
	5-HT6	human	CHO-K1	C1331-1	DC1331-1	MC1331-1
	5-HT7	human	HEK293T	C1334	DC1334	MC1334