5-HT receptor

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The 5-HT1B receptor as an example of a metabotropic serotonin receptor. Its crystallographic structure in ribbon representation

The serotonin receptors, also known as 5-hydroxytryptamine receptors or 5-HT receptors, are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems.[1][2] They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand.

The serotonin receptors modulate the release of many neurotransmitters, including glutamate, GABA, dopamine, epinephrine / norepinephrine, and acetylcholine, as well as many hormones, including oxytocin, prolactin, vasopressin, cortisol, corticotropin, and substance P, among others. The serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, and thermoregulation. The serotonin receptors are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.[3]

Serotonin receptors are found in almost all animals and humans and are even known to regulate longevity and behavioral aging in the primitive nematode, Caenorhabditis elegans.[4][5]

Classification

With the exception of the 5-HT3 receptor, a ligand-gated ion channel, all other serotonin receptors are G protein-coupled receptors that activate an intracellular second messenger cascade to produce an excitatory or inhibitory response. In 2014 a novel 5-HT receptor was described that was isolated from the small white butterfly, Pieris rapae, and named pr5-HT8. It shares relatively low similarity to the known 5-HT receptor classes and does not occur in mammals.[6]

Families

Family Type Mechanism Potential
5-HT1 Gi/Go-protein coupled. Decreasing cellular levels of cAMP. Inhibitory
5-HT2 Gq/G11-protein coupled. Increasing cellular levels of IP3 and DAG. Excitatory
5-HT3 Ligand-gated Na+ and K+ cation channel. Depolarizing plasma membrane. Excitatory
5-HT4 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory
5-HT5 Gi/Go-protein coupled.[7] Decreasing cellular levels of cAMP. Inhibitory
5-HT6 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory
5-HT7 Gs-protein coupled. Increasing cellular levels of cAMP. Excitatory

Subtypes

The 7 general serotonin receptor classes include a total of 14 known serotonin receptors.[8] The specific types have been characterized as follows:[9][10][11]

Overview of Serotonin Receptors

Receptor
(first cloned)		 Gene(s) Distribution Function Agonists Antagonists Uses of drugs that act on this receptor
5-HT1A
(1987)
  • Blood Vessels
  • CNS

Selective (for 5-HT1A over other 5-HT receptors)

Nonselective
5-HT1B
(1992)
  • Blood Vessels
  • CNS
5-HT1D
(1991)
  • Blood Vessels
  • CNS
5-HT1E
(1992)
  • Blood Vessels
  • CNS
  • None known
5-HT1F
(1993)
  • CNS
  • Migraine
  • None known
5-HT2A
(1988)
  • Blood Vessels
  • CNS
  • GI Tract
  • Platelets
  • PNS
  • Smooth Muscle
  • Addiction (potentially modulating) [47]
  • Anxiety[48]
  • Appetite
  • Cognition
  • Imagination
  • Learning
  • Memory
  • Mood
  • Perception
  • Sexual Behavior[49]
  • Sleep[50]
  • Thermoregulation[51]
  • Vasoconstriction[52]
5-HT2B
(1992)
  • Blood Vessels
  • CNS
  • GI Tract
  • Platelets
  • PNS
  • Smooth Muscle
5-HT2C
(1988)
  • Blood Vessels
  • CNS
  • GI Tract
  • Platelets
  • PNS
  • Smooth Muscle
5-HT3
(1993)
  • CNS
  • GI Tract
  • PNS
  • Addiction
  • Anxiety
  • Emesis
  • GI Motility[69]
  • Learning[70]
  • Memory[70]
  • Nausea
5-HT4
(1995)
  • CNS
  • GI Tract
  • PNS
5-HT5A
(1994)
  • CNS
  • None thus far
5-HT5B
(1993)

functions in rodents,
pseudogene in humans
  • None thus far
5-HT6
(1993)
  • CNS
5-HT7
(1993)
  • Blood Vessels
  • CNS
  • GI Tract

Note that there is no 5-HT1C receptor since, after the receptor was cloned and further characterized, it was found to have more in common with the 5-HT2 family of receptors and was redesignated as the 5-HT2C receptor.

Very nonselective agonists of 5-HT receptor subtypes include ergotamine (an antimigraine), which activates 5-HT1A, 5-HT1D, 5-HT1B, D2 and norepinephrine receptors.[35] LSD (a psychedelic) is a 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A, 5-HT5, 5-HT6 agonist.[35]

References

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  35. ↑ 35.00 35.01 35.02 35.03 35.04 35.05 35.06 35.07 35.08 35.09 35.10 35.11 35.12 35.13 35.14 35.15 35.16 35.17 35.18 35.19 35.20 Pharmacology Corner > Serotonin (5-HT): receptors, agonists and antagonists By Flavio Guzmán, M.D. on 9/08/09
  36. ↑ 36.0 36.1 36.2 36.3 36.4 "BRINTELLIX™ (vortioxetine) tablets for oral use. Full Prescribing Information, Section 12.2 (Pharmacodynamics)." Takeda Pharmaceuticals America Inc. and Lundbeck, 2013. Revised September 2013. [1]
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  47. ↑ 47.0 47.1 [2] Bubar MJ, Cunningham KA. Serotonin 5-HT2A and 5-HT2C receptors as potential targets for modulation of psychostimulant use and dependence. Curr Top Med Chem. 2006;6(18):1971-85.
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  95. ↑ Davies MA, Sheffler DJ, Roth BL. Aripiprazole: A Novel Atypical Antipsychotic Drug With a Uniquely Robust Pharmacology. CNS Drug Reviews [Internet]. 2004 [cited 2013 Aug 4];10(4):317–36. Available from: http://onlinelibrary.wiley.com/doi/10.1111/j.1527-3458.2004.tb00030.x/pdf

External links

  • Serotonin Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
  • Lua error in package.lua at line 80: module 'strict' not found.
  • Lua error in package.lua at line 80: module 'strict' not found.
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