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.

Targets
Literature
Receptor Data

Literature for 5-HT1 Receptors

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Neurodegeneration

Neurodegeneration Product Guide

A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

  • Alzheimer's disease
  • Parkinson's disease
  • Huntington's disease
5-HT Receptors

5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

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.