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5-HT receptor

From Wikipedia, the free encyclopedia
Class of transmembrane proteins
The5-HT1B receptor as an example of ametabotropic serotonin receptor. Itscrystallographic structure inribbon representation

5-HT receptors,5-hydroxytryptamine receptors, orserotonin receptors, are a group ofG protein-coupled receptor andligand-gated ion channels found in multiple tissues including thecentral andperipheral nervous systems.[1][2][3] They mediate bothexcitatory and inhibitoryneurotransmission. Theserotonin (i.e., 5-hydroxytryptamine, hence "5-HT") receptors are activated by theneurotransmitterserotonin, which acts as their naturalligand.

The serotonin receptors modulate the release of many neurotransmitters, includingglutamate,GABA,dopamine,epinephrine /norepinephrine, andacetylcholine, as well as many hormones, includingoxytocin,prolactin,vasopressin,cortisol,corticotropin, andsubstance P, among others. Serotonin receptors influence various biological and neurological processes such as aggression,anxiety, appetite,cognition, learning, memory,mood, nausea, sleep, andthermoregulation. They are the target of a variety of pharmaceutical and recreational drugs, including manyantidepressants,antipsychotics,anorectics,antiemetics,gastroprokinetic agents,antimigraine agents,psychedelics (hallucinogens), andentactogens.[4]

Serotonin receptors are found in almost all animals and are even known to regulate longevity and behavioural aging in the primitivenematode,Caenorhabditis elegans.[5][6]

Classification

[edit]

5-hydroxytryptamine receptors or 5-HT receptors, or serotonin receptors are found in thecentral andperipheral nervous systems.[1][2] They can be divided into 7 families ofG protein-coupled receptors which activate anintracellularsecond messenger cascade to produce an excitatory or inhibitory response. The exception to this is the5-HT3 receptor which is aligand-gated ion channel. In 2014, a novel 5-HT receptor was isolated from the small white butterfly,Pieris rapae, and named pr5-HT8. It does not occur in mammals and shares relatively low similarity to the known 5-HT receptor classes.[7]

Families

[edit]
FamilyTypeMechanismPotential
5-HT1Gi/Go-protein coupled.Decreasing cellular levels ofcAMP.Inhibitory
5-HT2Gq/G11-protein coupled.Increasing cellular levels ofIP3 andDAG.Excitatory
5-HT3Ligand-gatedNa+ andK+cation channel.Depolarizingplasma membrane.Excitatory
5-HT4Gs-protein coupled.Increasing cellular levels ofcAMP.Excitatory
5-HT5Gi/Go-protein coupled.[8]Decreasing cellular levels ofcAMP.Inhibitory
5-HT6Gs-protein coupled.Increasing cellular levels ofcAMP.Excitatory
5-HT7Gs-protein coupled.Increasing cellular levels ofcAMP.Excitatory

Subtypes

[edit]

The 7 general serotonin receptor classes include a total of 14 known serotonin receptors.[9] The 15th receptor 5-HT1P has been distinguished on the basis of functional and radioligand binding studies, its existence has never been definitely affirmed or refuted.[10][11] The specific types have been characterized as follows:[12][13][14]

Information on serotonin receptors (human isoforms if nothing else is stated)
ReceptorFirstcloned –PDB entriesGene(s)DistributionFunctionAgonistsAntagonistsUses of drugs that act on this receptor
Blood vesselsCNSGI TractPlateletsPNSSmooth Muscle
5-HT1A1987 –
  • 7e2x
  • 7e2y
  • 7e2z

YesYesNoNoNoNo

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

Nonselective

5-HT1B1992 –
  • 6g79
YesYesNoNoNoNo
5-HT1D1991 –
  • 7e32

YesYesNoNoNoNo
5-HT1E1992 –
  • 7e33

YesYesNoNoNoNo
  • None known
5-HT1F1993 –
  • 7exd

NoYesNoNoNoNo
  • Migraine
  • None known
5-HT1PNot clonedNoNoYesNoNoNo
  • None known
5-HT2A1988YesYesYesYesYesYes
  • Addiction (potentially modulating)[54]
  • Anxiety[55]
  • Appetite
  • Cognition
  • Imagination
  • Learning
  • Memory
  • Mood
  • Perception
  • Sexual Behavior[56]
  • Sleep[57]
  • Thermoregulation[58]
  • Vasoconstriction[59]
5-HT2B1992YesYesYesYesYesYes
5-HT2C1988YesYesYesYesYesYes
5-HT31993NoYesYesNoYesNo
  • Addiction
  • Anxiety
  • Emesis
  • GI Motility[77]
  • Learning[78]
  • Memory[78]
  • Nausea
5-HT41995NoYesYesNoYesNo
5-HT5A1994NoYesNoNoNoNo
  • None thus far
5-HT5B1993NoNoNoNoNoNo

Functions in rodents,
pseudogene in humans

  • None thus far
5-HT61993NoYesNoNoNoNo
5-HT71993YesYesYesNoNoNo

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.[107]

Very nonselective agonists of 5-HT receptor subtypes includeergotamine (anantimigraine), which activates 5-HT1A, 5-HT1D, 5-HT1B, D2 andnorepinephrine receptors.[38] LSD (apsychedelic) is a 5-HT1A, 5-HT2A, 5-HT2C, 5-HT5A and 5-HT6 agonist.[38]

Expression patterns

[edit]

The genes coding for serotonin receptors are expressed across the mammalian brain. Genes coding for different receptors types follow different developmental curves. Specifically, there is a developmental increase of HTR5A expression in several subregions of the human cortex, paralleled by a decreased expression of HTR1A from the embryonic period to the post-natal one.[108]

5-HT1-like

[edit]

A number of receptors were classed as "5-HT1-like" - by 1998 it was being argued that, since these receptors were "a heterogeneous population of 5-HT1B, 5-HT1D and 5-HT7" receptors the classification was redundant.[109]

References

[edit]
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