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5-HT2 Receptors
Serotonin 5-HT2 receptors are a subfamily of 5-HT receptors which bind the neurotransmitter serotonin (5-hydroxytryptamine). Three subtypes have been identified: 5-HT2A, 5-HT2B and 5-HT2C.
5-HT2 Receptor Target Files
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5-HT2A, 5-HT2B and 5-HT2C are are G-protein-coupled receptors that couple to Gq/11 causing activation of phospholipase C (PLC). PLC in turn hydrolyzes phosphatidylinositol (PIP2) to diacylglycerol (DAG) and inositol triphosphate (IP3). Localization and function of the individual receptor subtypes is summarized in the table below.
| Receptor Subtype | 5-HT2A | 5-HT2B | 5-HT2C |
|---|
| Transduction Mechanism | ↑ PLC (Gq/11) | ↑ PLC (Gq/11) | ↑ PLC (Gq/11) |
| Primary Distribution | Forebrain, caudate nucleus, nucleus accumbens, hippocampus, olfactory tubercle, vascular smooth muscle, blood platelets | Brain, stomach fundus (rat), gut, heart, kidney, lung | Choroid plexus, cortex, limbic system, basal ganglia |
| Function | Neuronal depolarization, head twitch, hyperthermia, modulation of neurotransmitter release smooth muscle contraction, platelet activation | Contraction of the stomach fundus, anxiety | Hypolocomotion, hypophagia, penile erection, hyperthermia, anxiety, ↓ noradrenalin and dopamine release |
| Selective Agonists | TCB-2 (2592) | BW 723C86 (1059) |
MK 212 (0941) Ro 60-0175 (1854) SCH 23390 (0925) WAY 161503 (1801) WAY 629 (2173) CP 809101 (3041) 1-Methylpsilocin (3017) |
| Non-subtype Selective Agonists |
PNU 22394 (2201)* α-methyl-5-hydroxytryptamine (0557) |
PNU 22394 (2201)* α-methyl-5-hydroxytryptamine (0557) m-CPP (0875) |
PNU 22394 (2201) α-methyl-5-hydroxytryptamine (0557) m-CPP (0875) |
| Selective Antagonists |
R-96544 (1742) Spiperone (0995) 4F 4PP (0523) Risperidone (2865) |
SB 204741 (1372) LY 272015 (3077) |
N-Desmethylclozapine (1007) RS 102221 (1050) SB 242084 (2901) |
| Non-subtype Selective Antagonists |
Altanserin (1809) Cyproheptadine (0996) MDL 11,939 (0870) Ritanserin (1955) Amperozide (2746) |
Altanserin (1809) Cyproheptadine (0996) MDL 11,939 (0870) Ritanserin (1955) Amperozide (2746) |
Altanserin (1809) Cyproheptadine (0996) MDL 11,939 (0870) Ritanserin (1955) Amperozide (2746) |
*partial agonist
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5-HT Review
Written by Nicholas Barnes and John Neumaier, leading experts. Request a copy or view PDF today.
7-TM Receptor Signaling
Written by T. Kenakin et al
'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy
Antidepressants - Current and Future Targets
Written by P. Skolnich et al
'Antidepressants - Current and Future Targets' provides an overview of the current and future targets for the treatment of major depressive disorder.
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