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5-HT Receptors

5-Hydroxytryptamine (5-HT, serotonin) is a monoamine neurotransmitter synthesized from L-tryptophan in serotonergic neurons and enterochromaffin cells of the gastrointestinal tract. 5-HT acts at serotonin receptors, which have been classified into seven groups (5-HT1-7) based on their pharmacological profiles, cDNA-deduced primary sequences and signal transduction mechanisms.

5-HT Receptor Target Files

Related Categories

Except for the 5-HT3 receptor, which is a ligand-gated ion channel, 5-HT receptors belong to the G-protein-coupled receptor (GPCR) superfamily. The 5-HT1, 5-HT2, 5-HT3 and 5-ht5 receptor groups have been further subdivided. In the CNS, serotonin has an important role in the regulation of mood, emesis, sexuality, sleep and appetite. Abnormalities in serotonergic function have been implicated in many disease states such as depression, anxiety, schizophrenia and migraine.

The table below summarizes the properties of 5-HT receptors.

Receptor Subtype Transduction Mechanism Localization Function Specific Agonists Specific Antagonists
5-HT1A ↓AC (Gi/o) Limbic system (hippocampus, lateral septum, cortical areas), mesencephalic raphe nuclei Hyperpolarization, modulation of neurotransmitter release, anxiolysis, hypothermia, hyperphagia Xaliprofen (2491)
S 14506 (1771)
Ipsapirone (1869)
BP 554 (0556)
U 92016A (2739)
Tandospirone (2854)*
MM 77 (0933)
NAN-190 (0553)
Spiroxatrine (0631)
(S)-WAY 100135 (1253)
5-HT1B ↓AC (Gi/o) Basal ganglia, striatum, amygdala, trigeminal ganglion, vascular smooth muscle Autoreceptor, locomotion, hypophagia, hypothermia, modulation of neurotransmitter release, vasoconstriction CGS 12066B (0638)
CP 93129 (1032)
CP 94253 (1317)
5-Nonyloxytryptamine (0901)
GR 55562 (1054)
Isamoltane (0992)
SB 224289 (1221)
NAS-181 (1413)
5-HT1D ↓AC (Gi/o) Basal ganglia, hippocampus, cortex, spinal cord, vascular smooth muscle Autoreceptor, modulation of neurotransmitter release L-694,247 (0781)
GR 46611 (0864)
PNU 109291 (2556)
PNU 142633 (1985)
BRL 15572 (1207)
Cyanopindolol (0993)
LY 310762 (3078)
5-ht1E ↓AC (Gi/o) Cortex, caudate putamen, claustrum, hippocampus, amygdala Unknown BRL 54443 (1129) -
5-HT1F ↓AC (Gi/o) Hippocampus, cortex, dorsal raphe nucleus, uterus Speculative role in visual and cognitive function BRL 5443 (1129)
LY 344864 (2451)
LY 334370 (3079)
-
5-HT2A ↑ PLC Forebrain, caudate nucleus, nucleus accumbens, hippocampus, olfactory tubercle, vascular smooth muscle, blood platelets Neuronal depolarization, head twitch, hyperthermia, modulation of neurotransmitter release smooth muscle contraction, platelet activation TBC-2 (2592) R- 96544 (1742)
Spiperone (0995)
MDL 11,939 (0870)
4F 4PP (0523)
Risperidone (2865)
5-HT2B ↑ PLC Brain, stomach fundus (rat), gut, heart, kidney, lung Contraction of the stomach fundus, anxiety BW 723C86 (1059) SB 204741 (1372)
LY 272015 (3077)
5-HT2C ↑ PLC Choroid plexus, cortex, limbic system, basal ganglia Hypolocomotion, hypophagia, penile erection, hyperthermia, anxiety, ↓ noradrenalin and dopamine release MK 212 (0941)
Ro 60-0175 (1854)
WAY 161503 (1801)
CP 809101 (3041)
1-Methylpsilocin (3017)
N-Desmethylclozapine (1007)
RS 102221 (1050)
SB 242084 (2901)
5-HT3 Ion channel
(Na+, K+, Ca2+)
Dorsal vagal complex, hippocampus, amygdala, caudate, cerebral cortex, heart, intestines Anxiety, cognition, pain , reward/withdrawal, vomiting reflex, vasodilation, intestinal tone and secretion SR 57227 (1205)
Quipazine (0629)
1-phenylbiguanide (0969)
m-chlorophenylbiguanide (0440)
MDL 72222 (0640)
Tropisetron (2459)
Y-25130 (0380)
Ondansetron (2891) Granisetron (2903)
5-HT4 ↑ AC (Gs) Cerebral cortex, limbic areas, hippocampus, colliculus, intestines Learning and memory, visual perception, anxiety, motor coordination, arousal, smooth muscle relaxation, modulation of neurotransmitter release Cisapride (1695)
RS 67333 (0989)*
RS 67506 (0990)*
CJ 033466 (3089)*
GR 113808 (1322)
GR 125487 (1658)
RS 39604 (0991)
RS 23597-190 (0728)
5-ht5A ↓ AC (Gi/o) Amygdala, hippocampus, caudate nucleus, cerebellum, hypothalamus, thalamus, substantia nigra, spinal cord Modulation of exploratory behavior and locomotion - SB 699551 (3188)
5-HT6 ↑ AC (Gs) Striatum, olfactory tubercles, nucleus accumbens, hippocampus, stomach, adrenal glands Memory and learning, modulation of neurotransmitter release 5-Methyl-5-hydroxytryptamine (0558)
EMD 386088 (2382)
SB 258585 (1961)
Ro 47-1816/001 (2911)
SB 399885 (3189)
NPS ALX Compound 4a (3285)
5-HT7 ↑ AC (Gs) Thalamus, hypothalamus, hippocampus, cerebral cortex, amygdala, GI and vascular smooth muscle, heart Circadian rhythms, smooth muscle relaxation, nociception, hypotension, modulation of REM sleep, learning and memory, LH release AS 19 (1968)
LP 44 (2534)
LP 12 (2925)
Pimozide (0937)
SB 269970 (1612)
SB 259719 (2726)

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