5-HT1 Receptors
Serotonin 5-HT1 receptors are a subfamily of 5-HT receptors which bind the neurotransmitter serotonin, also known as 5-hydroxytryptamine. Five subtypes have been identified (5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E and 5-HT1F), all of which are G-protein-coupled receptors that couple to Gi/o causing a decrease in cAMP levels.
Related Targets
5-HT Transporters | Non-selective 5-HT1 |
5-HT3 Receptors (5-HT3 Receptors) |
Receptor Data
5-HT1 Receptor Data
| Receptor Subtype | 5-HT1A | 5-HT1B | 5-HT1D | 5-ht1E | 5-HT1F |
|---|---|---|---|---|---|
| Transduction Mechanism | ↓Adenylyl Cyclase (Gi/o) | ↓ Adenylyl Cyclase (Gi/o) | ↓ Adenylyl Cyclase (Gi/o) | ↓ Adenylyl Cyclase (Gi/o) | ↓ Adenylyl Cyclase (Gi/o) |
| Primary Distribution | Limbic system (hippocampus, lateral septum, cortical areas), mesencephalic raphe nuclei | Basal ganglia, striatum, amygdala, trigeminal ganglion, vascular smooth muscle | Basal ganglia, hippocampus, cortex, spinal cord, vascular smooth muscle | Cortex, caudate putamen, claustrum, hippocampus, amygdala | Hippocampus, cortex, dorsal raphe nucleus, uterus |
| Function | Hyperpolarization, modulation of neurotransmitter release, anxiolysis, hypothermia, hyperphagia | Autoreceptor, locomotion, hypophagia, hypothermia, modulation of neurotransmitter release, vasoconstriction | Autoreceptor, modulation of neurotransmitter release | Unknown | Speculative role in visual and cognitive function |
| Selective Agonists | Ipsapirone (1869) | CGS 12066B (0638) CP 93129 (1032) CP 94253 (1317) 5-Nonyloxytryptamine | L-694,247 PNU 142633 (1985) PNU 109291 | - | LY 344864 (2451) |
| Non-subtype Selective Agonists | 5-Carboxamindotrypt-amine (0458) | 5-Carboxamindotrypt-amine (0458) | 5-Carboxamindotrypt-amine (0458) | 5-Carboxamindotrypt-amine (0458) | 5-Carboxamindotrypt-amine (0458) |
| Selective Antagonists | NAN-190 (0553) (S)-WAY 100135 (1253) | GR 55562 (1054) SB 224289 (1221) | BRL 15572 Cyanopindolol (0993) | - | - |
| Non-subtype Selective Antagonists | Pindolol | Pindolol GR 127935 (1054) | GR 127935 (1054) | - | - |
References
Hoyer et al (1994) VII. International union of pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacol. Rev. 46 157. Barnes and Sharp (1999) A review of central 5-HT receptors and their function. Neuropharmacol. 38 1083. Pauwels (2003) 5-HT receptors and their ligands. Tocris Reviews No. 25.