Main 5-HT receptor subtypes

Receptor

Location

Main effects

Second
messenger

1A

CNS

Neuronal inhibition
cAMP
Behavioural effects: sleep,
feeding, thermoregulation, anxiety

1B

CNS
Vascular smooth muscle

Presynaptic inhibition
Behavioural effects
Pulmonary vasoconstriction

1D

CNS
Blood vessels

2A

Agonists

Antagonists

5-CT
8-OH-DPAT
Buspirone (partial
agonist)

Spirperone
Methiothepin
Ergotamine (partial
agonist)

cAMP

5-CT
Ergotamine (partial
agonist)

Methiothepin

Cerebral vasoconstriction
Behavioural effects: locomotion

cAMP

5-CT
Sumatriptan

Methiothepin
Ergotamine (partial
agonist)

CNS
PNS
Smooth muscle
Platelets

Neuronal excitation
Behavioural effects
Smooth muscle contraction (gut,
bronchi etc)
Platelet aggregation
Vasoconstriction/vasodilatation

IP3/DAG

-Me-5-HT
LSD (CNS)
LSD (periphery)

Ketanserin
Cyproheptadine
Pizotifen (nonselective)
Methylsergide

2B

Gastric Fundus

Contraction

IP3/DAG

-Me-5-HT

2C

CNS
Choroid plexus

Cerebrospinal fluid secretion

IP3/DAG

-Me-5-HT
LSD

Methylsergide

PNS
CNS

Neuronal excitation (autonomic,

nociceptive neurons)
Emesis
Behavioural effects: anxiety

Nil - ligand
gated cation
channel

2-Me-5-HT
Chlorophenylbiguanide

Ondansetron
Tropistetron
Granisetron

Receptor

Location

Main effects

Second
messenger

Agonists

Antagonists

PNS (GI tract)

CNS

Neuronal excitation
GIT motility

cAMP

5-Methoxytryptamine
Metoclopramide
Tegaserod

Various
experimental
compounds

CNS

Not known

Not known

Not known

Not known

CNS

Not known

Not known

Not known

Not known

CNS
GI Tract
Blood vessels

Not known

cAMP

5-CT
LSD
No selective agonists

Various 5-HT2
antagonists
No selective
antagonists