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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 |
Xaliproden (2491) S 14506 (1771) Ipsapirone (1869) BP 554 (0556) |
CGS 12066B (0638) CP 93129 (1032) CP 94253 (1317) 5-Nonyloxytryptamine (0901) |
L-694,247 (0781) GR 46611 (0864) PNU 142633 (1985) PNU 109291 (2556) |
BRL 54443 (1129) |
BRL 54443 (1129) LY 344864 (2451) LY 334370 (3079) |
| Non-subtype Selective Agonists |
Eltoprazine (1860) 5-Carboxamindotrypt-amine (0458) |
Eltoprazine (1860) 5-Carboxamindotrypt-amine (0458) |
Eltoprazine (1860) 5-Carboxamindotrypt-amine (0458) |
Eltoprazine (1860) 5-Carboxamindotrypt-amine (0458) |
Eltoprazine (1860) 5-Carboxamindotrypt-amine (0458) |
| Selective Antagonists |
MM 77 (0933) NAN-190 (0553) Spiroxatrine (0631) (S)-WAY 100135 (1253) |
GR 55562 (1054) Isamoltane (0992) SB 224289 (1221) NAS-181 (1413) |
BRL 15572 (1207) Cyanopindolol (0993) |
- | - |
| Non-subtype Selective Antagonists |
Pindolol (0994) SDZ 21009 (1516) |
Pindolol (0994) GR 127935 (1054) SDZ 21009 (1516) |
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.