Table 1.
Receptor | Structural Family | Signal Transduction | Localization | Function | Comments |
---|---|---|---|---|---|
5-HT1A | GPCR | Inhibition of AC | Hippocampus, Septum, Amygdala, Cortical limbic areas, Raphe nuclei | Autoreceptor | Cloned and pharmacological 5-HT1A sites. |
5-HT1B | GPCR | Inhibition of AC | Basal and Trigeminal ganglia, Striatum, Frontal cortex Cerebral arteries and other vascular tissues |
Autoreceptor | Rodent homologue of human 5-HT1Dβ receptors. |
5-HT1D | GPCR | Inhibition of AC | Basal and Trigeminal ganglia | Unknown | Newer name: 5-HT1Bβ; a mouse homologue of human 5-HT1Dβ receptors; sites identified in binding studies using brains homogenates; 5-HT1Dα and 5-HT1Dβ (cloned human 5-HT1D subpopulations). |
Cranial blood vessels | Vasoconstriction | ||||
5-ht1E | GPCR | Inhibition of AC | Cerebral cortex, Striatum | Unknown | Newer name: 5-ht1Eβ; sites identified in binding studies using brain homogenates; 5-ht1Ea (an alternate name for cloned human 5-ht1E receptors). |
5-ht1F | GPCR | Inhibition of AC | Dorsal raphe, Hippocampus, Striatum, Cerebral cortex, Thalamus, Hypothalamus | Unknown | A cloned human 5-HT1-like receptor population. |
Uterus, Mesentery | Vasoconstriction | ||||
5-HT2A (D receptor) | GPCR | Activation of PLC | Cerebral cortex, Claustrum, Basal ganglia | Neuronal excitation | Newer name: 5-HT2A; original "5-HT2" (5-HT2α) receptors |
Smooth muscle | Contraction | ||||
Platelets | Platelet aggregation | ||||
5-HT2B | GPCR | Activation of PLC (Other unknown) | Cerebellum, Lateral septum, Hypothalamus, Medial amygdala | Unknown | Newer name: 5-HT2B; 5-HT2-like receptors in rat fundus |
Stomach fundus | Contraction | ||||
Blood vessels | Vasodilatation | ||||
5-HT2C | GPCR | Activation of PLC | Choroid plexus | Vasodilatation | Newer name: 5-HT2C; original "5-HT1C" (5-HT2β) receptors. |
5-HT3 (M receptor) | 5-HT-GIC | Ligand-gated ion channel | Area postrema, Enthorinal and Frontal cortex, Hippocampus, Solitary Tract, Amygdala Peripheral pre- and post-ganglionic autonomic neurons, Sensory nervous system, Gastrointestinal tract | Neuronal excitation | An ion channel receptor. |
5-HT4 | GPCR | Activation of AC | Hippocampus, Colliculi, Nucleus accumbens Gastrointestinal tract, Vascular smooth muscle | Neuronal excitation | 5-HT4 population originally described in functional studies; 5-HT4s (short form of cloned rat 5-HT4 receptors); 5-HT4L (long form of cloned rat 5-HT4 receptors). |
5-ht5A | GPCR | Inhibition of AC | Hypothalamus, Hippocampus, Corpus callosum, Fimbria, Cerebral ventricles, Glia | Unknown | Cloned mouse, rat and human 5-ht5 or 5-ht5A-like receptors. |
5-ht5B | Unknown | Unknown | |||
5-ht6 | GPCR | Activation of AC | Caudate nucleus, Striatum, Amygdala, Nucleus accumbens, Hippocampus, Cerebral cortex and Olfactory tubercle | Unknown | Cloned rat and human 5-HT receptors. |
5-HT7 | GPCR | Activation of AC | Cerebral cortex, Thalamic nuclei, Sensory nuclei, Substantia nigra, Hypothalamus, Raphe nuclei Vascular tissues, Smooth muscle (ileum) |
Unknown | Cloned rat, mouse, guinea pig and human 5-HT receptors; original "5-HT1-like" receptors. |
Legend: GPCR, G protein-coupled Receptor; 5-HT-GIC, 5-HT-gated ion channel; AC, adenylate cyclase; PLC, phospholipase C.