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. Localization and function of the individual receptor subtypes are summarized in the table below.

5-HT1 Receptor Target Files

Related Categories
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)
Tandospirone (2854)*
CGS 12066B (0638)
CP 93129 (1032)
CP 94253 (1317)
5-Nonyloxy-tryptamine (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-Carboxamindo-tryptamine (0458)
Eltoprazine (1860)
5-Carboxamindo-tryptamine (0458)
Eltoprazine (1860)
5-Carboxamindo-tryptamine (0458)
Eltoprazine (1860)
5-Carboxamindo-tryptamine (0458)
Eltoprazine (1860)
5-Carboxamindo-tryptamine (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)
LY 310762 (3078)
- -
Non-subtype Selective Antagonists Pindolol (0994)
SDZ 21009 (1516)
Pindolol (0994)
GR 127935 (1054)
SDZ 21009 (1516)
GR 127935 (1054) - -

*partial agonist

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