Table 1.
The family of 5-HT receptors [120].
| Receptor | Selective agonists | Potential | Type | G protein effector | Mechanism of action | CNS distribution |
|---|---|---|---|---|---|---|
| 5-HT1 (5-HT1A, 1B, 1D–F) | 1A=8-OH-DPAT, 1B=sumatriptan, 1C=sumatriptan, 1F=LY 334370 | Inhibitory | Gi/G0-protein coupled | Gi/o | Decrease in intracellular cAMP levels and inhibition of AC | Cerebral and frontal cortex, hippocampus |
|
| ||||||
| 5-HT2 (5-HT2A–C) | DOId, BW 723C86, Ro 600175 | Excitatory | Gq11-protein coupled | Gq/11 | Activation of PLC, enhancing in IP3 and DAG intracellular concentration, and rise in intracellular calcium | Nucleus accumbens, basal ganglia, cerebellum |
|
| ||||||
| 5-HT3 (5-HT3A, 3B) | DOId, BW 723C86, Ro 600175 | Excitatory | Ligand-gated Na+/K+ channel | — | Depolarization of cell plasma membrane | Hippocampus, amygdala, nucleus accumbens |
|
| ||||||
| 5-HT4 (5-HT4A–H) | DOId, BW 723C86, Ro 600175 | Excitatory | Gs-protein coupled | Gs | Increased intracellular cAMP concentration and activation of AC | Hippocampal membranes |
|
| ||||||
| 5-HT5 (5-HT5A) | — | Inhibitory | Gi/G0-protein coupled | Gi/o | Decrease in intracellular cAMP levels and inhibition of AC | Olfactory bulb, neocortex, hippocampus |