5-HT receptor: Difference between revisions
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! [[5-HT1D receptor|5-HT<sub>1D</sub>]] |
! [[5-HT1D receptor|5-HT<sub>1D</sub>]] |
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| {{Gene|HTR1D}} |
| {{Gene|HTR1D}} |
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| CNS: locomotion; vascular: cerebral [[vasoconstriction]] |
| CNS: locomotion, anxiety; vascular: cerebral [[vasoconstriction]] |
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| 5-(Nonyloxy)tryptamine <ref name="Glennon_et_al_94">{{cite journal | author=Glennon RA, Hong SS, Dukat M, Teitler M, Davis K.| title=5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist. | journal=Journal of Medicinal Chemistry | year=1994 | pages=2828–30 | volume=37 | issue=18 | id=PMID 8071931}}</ref>, sumatriptan |
| 5-(Nonyloxy)tryptamine <ref name="Glennon_et_al_94">{{cite journal | author=Glennon RA, Hong SS, Dukat M, Teitler M, Davis K.| title=5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist. | journal=Journal of Medicinal Chemistry | year=1994 | pages=2828–30 | volume=37 | issue=18 | id=PMID 8071931}}</ref>, sumatriptan |
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| methiothepin, yohimbine, metergoline, ergotamine |
| methiothepin, yohimbine, metergoline, ergotamine |
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! [[5-HT2A receptor|5-HT<sub>2A</sub>]] |
! [[5-HT2A receptor|5-HT<sub>2A</sub>]] |
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| {{Gene|HTR2A}} |
| {{Gene|HTR2A}} |
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| CNS: neuronal excitation, behavioural effects, learning; smooth muscle: contraction, vasoconstriction / dilatation; platelets: aggregation |
| CNS: neuronal excitation, behavioural effects, learning, anxiety; smooth muscle: contraction, vasoconstriction / dilatation; platelets: aggregation |
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| [[α-methyl-5-HT]], [[LSD]] (CNS), [[psilocin]], [[2,5-Dimethoxy-4-iodoamphetamine|DOI]] |
| [[α-methyl-5-HT]], [[LSD]] (CNS), [[psilocin]], [[2,5-Dimethoxy-4-iodoamphetamine|DOI]] |
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| [[Nefazodone]], [[trazodone]], [[mirtazapine]], [[ketanserin]], [[cyproheptadine]], [[pizotifen]], [[LSD]], [[atypical antipsychotics]] ([[Peripheral nervous system|PNS]]) |
| [[Nefazodone]], [[trazodone]], [[mirtazapine]], [[ketanserin]], [[cyproheptadine]], [[pizotifen]], [[LSD]], [[atypical antipsychotics]] ([[Peripheral nervous system|PNS]]) |
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! [[5-HT2C receptor|5-HT<sub>2C</sub>]] |
! [[5-HT2C receptor|5-HT<sub>2C</sub>]] |
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| {{Gene|HTR2C}} |
| {{Gene|HTR2C}} |
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| CNS, [[choroid plexus]]: [[cerebrospinal fluid]] (CSF) secretion |
| CNS: anxiety, [[choroid plexus]]: [[cerebrospinal fluid]] (CSF) secretion |
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| α-methyl-5-HT, [[agomelatine]], [[LSD]] (CNS), [[psilocin]], [[2,5-Dimethoxy-4-iodoamphetamine|DOI]] |
| α-methyl-5-HT, [[agomelatine]], [[LSD]] (CNS), [[psilocin]], [[2,5-Dimethoxy-4-iodoamphetamine|DOI]] |
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| [[mesulergine]], [[agomelatine]], [[LSD]] (PNS), [[fluoxetine]] |
| [[mesulergine]], [[agomelatine]], [[LSD]] (PNS), [[fluoxetine]] |
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Revision as of 02:05, 21 September 2007
In the field of neurochemistry, 5-HT receptors are receptors for the neurotransmitter and peripheral signal mediator serotonin, also known as 5-hydroxytryptamine or 5-HT. 5-HT receptors are located on the cell membrane of nerve cells and other cell types including smooth muscle in animals, and mediate the effects of serotonin as the endogenous ligand and of a broad range of pharmaceutical and hallucinogenic drugs. All 5-HT receptors reduce cyclic adenosine monophosphate (cAMP).
Classification
With the exception of the 5-HT3 receptor, a ligand gated ion channel, all other 5-HT receptors are G protein coupled seven transmembrane (or heptahelical) receptors that activate an intracellular second messenger cascade.
Families
| Family | Type | Mechanism |
| 5-HT1 | Gi/Go coupled | decreasing cellular levels of cAMP |
| 5-HT2 | Gq/G11 coupled | increasing cellular levels of inositol trisphosphate (IP3) and diacylglycerol (DAG) |
| 5-HT3 | ligand-gated Na+ and K+ cation channel | depolarizing plasma membrane |
| 5-HT4 | Gs coupled | increasing cellular levels of cAMP |
| 5-HT5A | G protein coupled; the primary coupling appears to be through Gi/o | inhibiting adenylate cyclase activity.[1] |
| 5-HT7 | Gs coupled | increasing cellular levels of cAMP |
Specific proteins/genes
Within these general classes of 5-HT receptors, a number of specific types have been characterized:
| Receptor | Gene | Actions | Agonists | Antagonists |
|---|---|---|---|---|
| 5-HT1A | HTR1A | CNS: neuronal inhibition, behavioural effects (sleep, feeding, thermoregulation, aggression, anxiety) | buspirone, psilocin | spiperone, methiothepin, ergotamine, yohimbine |
| 5-HT1B | HTR1B | CNS: presynaptic inhibition, behavioural effects; vascular: pulmonary vasoconstriction | ergotamine, sumatriptan | methiothepin, yohimbine, metergoline |
| 5-HT1D | HTR1D | CNS: locomotion, anxiety; vascular: cerebral vasoconstriction | 5-(Nonyloxy)tryptamine [2], sumatriptan | methiothepin, yohimbine, metergoline, ergotamine |
| 5-HT1E | HTR1E | |||
| 5-HT1F | HTR1F | |||
| 5-HT2A | HTR2A | CNS: neuronal excitation, behavioural effects, learning, anxiety; smooth muscle: contraction, vasoconstriction / dilatation; platelets: aggregation | α-methyl-5-HT, LSD (CNS), psilocin, DOI | Nefazodone, trazodone, mirtazapine, ketanserin, cyproheptadine, pizotifen, LSD, atypical antipsychotics (PNS) |
| 5-HT2B | HTR2B | stomach: contraction | α-methyl-5-HT, LSD (CNS), DOI | yohimbine, LSD (PNS) |
| 5-HT2C | HTR2C | CNS: anxiety, choroid plexus: cerebrospinal fluid (CSF) secretion | α-methyl-5-HT, agomelatine, LSD (CNS), psilocin, DOI | mesulergine, agomelatine, LSD (PNS), fluoxetine |
| 5-HT3 | HTR3A, HTR3B | CNS, PNS: neuronal excitation, anxiety, emesis | 2-methyl-5-HT | metoclopramide (high doses), renzapride, ondansetron, alosetron, mirtazapine, memantine |
| 5-HT4 | HTR4 | GIT, CNS: neuronal excitation, gastrointestinal motility | 5-methoxytryptamine, metoclopramide, renzapride, tegaserod | GR113808 |
| 5-HT5A | HTR5A | CNS (cortex, hippocampus, cerebellum): unknown | 5-carboxytryptamine; LSD (partial agonist)[1] |
unknown |
| 5-HT6 | HTR6 | CNS: unknown | LSD | SB271046 [3] |
| 5-HT7 | HTR7 | CNS, GIT, blood vessels: unknown | 5-carboxytryptamine, LSD | methiothepin, risperidone |
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.
Therapeutic modulation
Various drugs are used to modulate the 5-HT system including some antidepressants, anxiolytics, antiemetics, antipsychotics and anti-migraine agents.
References
- ^ a b D.L. Nelson (2004). "5-HT5 receptors". Curr. Drug Targets CNS Neurol. Disord. 3 (1): 53–58. PMID 14965244.
- ^ Glennon RA, Hong SS, Dukat M, Teitler M, Davis K. (1994). "5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist". Journal of Medicinal Chemistry. 37 (18): 2828–30. PMID 8071931.
{{cite journal}}: CS1 maint: multiple names: authors list (link) - ^ "Target Schizophrenia - Possible future developments". Retrieved 2007-07-06.
External links
- IUPHAR GPCR Database - 5-HT Receptors
- Serotonin Receptor Subtypes and Ligands by R.A. Glennon, 2000
- G Protein-Coupled Receptor Activation of 5-HT2A and other GPCRs. A hypothetical model of how these receptors work by L.A. Rubenstein, 1997
- Basic Neurochemistry - Serotonin Receptors (published 1999)
- Wesołowska A (2002). "In the search for selective ligands of 5-HT5, 5-HT6 and 5-HT7 serotonin receptors" (PDF). Polish journal of pharmacology. 54 (4): 327–41. PMID 12523486.
- Serotonin+Receptors at the U.S. National Library of Medicine Medical Subject Headings (MeSH)