Table 1.

Summary of the main characteristics of 5-HT₁ receptors

Receptor subtype	Distribution	Effector mechanism	Physiological action	Agonists used as antimigraine therapy
5-HT1A	CNS Raphe nuclei, hippocampus, amygdala, septum, entorhinal cortex, hypothalamus PNS Cholinergic heteroceptor in myenteric plexus	- Inhibition of adenylyl cyclase - Opening of K+ channels - Inhibition of voltage gated Ca2+ channels	- Serotonergic auto receptor - Neuronal inhibition - Facilitate ACh and NA release - Cholinergic nerve terminal in myenteric plexus - Hyperphagia	None
5-HT1B	CNS Subiculum, substantia nigra PNS Vascular smooth muscle	Inhibition of adenylyl cyclase	- Serotonergic auto receptor - Control release of ACh and NA - Contraction of vascular smooth muscle	Ergot alkaloids Triptans
5-HT1D	CNS Cranial blood vessel PNS Vascular smooth muscle	Inhibition of adenylyl cyclase	- Serotonergic auto receptor - GABAergic and cholinergic heteroreceptor - Vasoconstriction of intracranial blood vessel	Ergot alkaloids Triptans
5-HT1e	CNS Cortex striatum PNS mRNA in vascular tissue	Inhibition of adenylyl cyclase	Unknown	None
5-HT1F	CNS Cortex, spinal cord, hippocampus, locus coeruleus, hypothalamus, amygdala, cerebellum, dorsal raphe nucleus, pineal gland PNS Uterus, mesentery, vascular smooth muscle	Inhibition of adenylyl cyclase	Trigeminal neuroinhibition in guinea pig and rat	Lasmiditan

5-HT_1C was reclassified as 5-HT_2C, thereafter it is not included in this table. Data taken from [4–7]

ACh acetylcholine, CNS central nervous system, PNS peripheral nervous system, NA noradrenaline