| 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) |
MM 77 (0933) |
| S 14506
(1771) |
NAN-190 (0553) |
| Ipsapirone
(1869) |
Spiroxatrine (0631) |
| BP 554
(0556) |
(S)-WAY 100135 (1253) |
| Tandospirone
(2854)* |
|
| 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) |
GR 55562
(1054) |
| CP 93129
(1032) |
Isamoltane (0992) |
| CP 94253
(1317) |
SB 224289 (1221) |
| 5-Nonyloxytryptamine
(0901) |
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) |
BRL 15572
(1207) |
| GR 46611
(0864) |
Cyanopindolol (0993) |
| PNU 109291
(2556) |
LY 310762 (3078) |
| PNU 142633
(1985) |
|
| 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) |
N-Desmethylclozapine
(1007) |
| Ro 60-0175
(1854) |
RS 102221 (1050) |
| WAY 161503
(1801) |
SB 242084 (2901) |
| CP 809101
(3041) |
|
| 1-Methylpsilocin
(3017) |
|
| 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) |
MDL 72222
(0640) |
| Quipazine
(0629) |
Tropisetron (2459) |
| 1-phenylbiguanide
(0969) |
Y-25130 (0380) |
| m-chlorophenylbiguanide
(0440) |
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) |
GR 113808
(1322) |
| RS 67333
(0989)* |
GR 125487 (1658) |
| RS 67506
(0990)* |
RS 39604 (0991) |
| CJ 033466
(3089)* |
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) |
SB 258585
(1961) |
| EMD 386088
(2382) |
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) |
Pimozide
(0937) |
| LP 44 (2534) |
SB 269970 (1612) |
| LP 12 (2925) |
SB 259719 (2726) |
| * partial agonist |
|
|
|
|