Nomenclature: 5-HT1F receptor

Family: 5-Hydroxytryptamine receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates. 

Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 366 3p12 HTR1F 5-hydroxytryptamine (serotonin) receptor 1F, G protein-coupled 3
Mouse 7 366 16 C1.3 Htr1f 5-hydroxytryptamine (serotonin) receptor 1F 6
Rat 7 366 11p12 Htr1f 5-hydroxytryptamine (serotonin) receptor 1F, G protein-coupled 8
Previous and Unofficial Names
Names References
5-HT1Eβ 8
5-HT1Eb
5-HT6
HTR1EL
5-HT1F
5-hydroxytryptamine (serotonin) receptor 1F
Htr1eb
5-HT-1F
5-hydroxytryptamine receptor 1F
serotonin receptor 1F
serotonin receptor gene (similar to Mm Htr1eb)
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligands
5-HT
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]LY334370 Hs Full agonist 9.4 pKd 17
pKd 9.4 (Kd 3.98x10-10 M) [17]
[125I]LSD Mm Agonist 9.0 pKd 4
pKd 9.0 (Kd 9.8x10-10 M) [4]
5-HT Hs Full agonist 8.0 pKd 3
pKd 8.0 [3]
BRL-54443 Hs Full agonist 8.9 pKi 5
pKi 8.9 [5]
lasmiditan Hs Full agonist 8.7 pKi 11
pKi 8.7 [11]
LY334370 Hs Full agonist 8.7 pKi 17
pKi 8.7 [17]
LY344864 Hs Full agonist 8.2 pKi 13
pKi 8.2 [13]
naratriptan Hs Full agonist 8.2 pKi 10,17
pKi 8.2 [10,17]
eletriptan Hs Full agonist 8.0 pKi 10
pKi 8.0 [10]
5-HT Hs Full agonist 7.7 – 8.0 pKi 1,3,17
pKi 7.7 – 8.0 [1,3,17]
sumatriptan Hs Full agonist 7.2 – 7.9 pKi 1,3,10,17
pKi 7.2 – 7.9 [1,3,10,17]
zolmitriptan Hs Full agonist 7.4 – 7.5 pKi 10,17
pKi 7.4 – 7.5 [10,17]
5-MeO-DMT Hs Full agonist 7.4 pKi 3
pKi 7.4 [3]
clozapine Hs Full agonist 6.9 pKi 15
pKi 6.9 [15]
dihydroergotamine Hs Full agonist 6.6 – 7.1 pKi 1,17
pKi 6.6 – 7.1 [1,17]
ergotamine Hs Full agonist 6.8 pKi 3
pKi 6.8 [3]
GR-127935 Hs Partial agonist 6.4 – 7.2 pKi 14,17
pKi 6.4 – 7.2 [14,17]
NAN 190 Hs Partial agonist 6.7 pKi 3
pKi 6.7 [3]
α-methyl-5-HT Hs Full agonist 6.7 pKi 3
pKi 6.7 [3]
rizatriptan Hs Full agonist 6.4 – 6.8 pKi 10,17
pKi 6.4 – 6.8 [10,17]
xanomeline Hs Full agonist 6.5 pKi 18
pKi 6.5 [18]
olanzapine Hs Full agonist 6.5 pKi 15
pKi 6.5 [15]
2-methyl-5-HT Hs Full agonist 6.4 pKi 3
pKi 6.4 [3]
5-CT Hs Full agonist 6.1 pKi 1,3
pKi 6.1 [1,3]
BRL-15572 Hs Partial agonist 6.0 pKi 14
pKi 6.0 [14]
TFMPP Hs Full agonist 6.0 pKi 3
pKi 6.0 [3]
5-MeOT Hs Full agonist 5.9 pKi 3
pKi 5.9 [3]
DOI Hs Full agonist 5.8 pKi 3
pKi 5.8 [3]
dipropyl-5-CT Hs Full agonist 5.8 pKi 3
pKi 5.8 [3]
8-OH-DPAT Hs Full agonist 5.8 pKi 3
pKi 5.8 [3]
tryptamine Hs Full agonist 5.6 pKi 3
pKi 5.6 [3]
quetiapine Hs Full agonist 5.6 pKi 15
pKi 5.6 [15]
donitriptan Hs Full agonist 5.5 pKi 7
pKi 5.5 [7]
ergotamine Rn Full agonist 7.3 pIC50 8
pIC50 7.3 [8]
sumatriptan Hs Full agonist 7.2 pIC50 8
pIC50 7.2 [8]
5-HT Rn Full agonist 7.2 pIC50 8
pIC50 7.2 [8]
5-CT Rn Full agonist 5.6 pIC50 8
pIC50 5.6 [8]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
methysergide Hs Antagonist 8.2 pKi 3,17
pKi 8.2 [3,17]
methylergonovine Hs Antagonist 7.5 pKi 3
pKi 7.5 [3]
1-naphthylpiperazine Hs Antagonist 7.3 pKi 1,3
pKi 7.3 [1,3]
yohimbine Hs Antagonist 7.0 pKi 3
pKi 7.0 [3]
metergoline Hs Antagonist 6.5 pKi 1,3
pKi 6.5 [1,3]
sertindole Hs Antagonist 6.4 pKi 15
pKi 6.4 [15]
methiothepin Hs Antagonist 6.2 pKi 1,3
pKi 6.2 [1,3]
risperidone Hs Antagonist 5.9 pKi 15
pKi 5.9 [15]
methysergide Rn Antagonist 7.8 pIC50 8
pIC50 7.8 [8]
metergoline Rn Antagonist 6.3 pIC50 8
pIC50 6.3 [8]
yohimbine Rn Antagonist 6.2 pIC50 8
pIC50 6.2 [8]
View species-specific antagonist tables
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  2
Tissue Distribution
Brain, uterus (endometrium and myometrium), mesentery.
Species:  Human
Technique:  PCR.
References:  3
Ventricle wall > atrium, epicardium, coronary artery.
Species:  Human
Technique:  RT-PCR.
References:  12
Brain: lamina V of the frontal cortex in large pyramidal cells, hippocampal pyramidal cells, thalamic nuclei and dorsal raphe.
Species:  Human
Technique:  in situ hybridisation.
References:  3
Trigeminal ganglion.
Species:  Rat
Technique:  Immunohistochemistry.
References:  9
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  16
Brain: cortex, striatum, hippocampus > thalamus, pons > hypothalamus > cerebellum.
Species:  Rat
Technique:  RT-PCR.
References:  8
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

There should be a chart of expression data here, you may need to enable JavaScript!
Functional Assays
Measurement of cAMP levels in LM(tk-) cells
Species:  Human
Tissue:  LM(tk-) cells.
Response measured:  Weak inhibition of cAMP accumulation.
References:  3
Measurement of cAMP levels in HeLa cells transfected with the rat 5-HT1f receptor.
Species:  Rat
Tissue:  HeLa cells.
Response measured:  Inhibition of cAMP accumulation.
References:  8
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Htr1ftm1Dgen Htr1ftm1Dgen/Htr1ftm1Dgen
involves: 129P2/OlaHsd * C57BL/6
MGI:99842  MP:0009141 increased prepulse inhibition
Htr1ftm1Dgen Htr1ftm1Dgen/Htr1ftm1Dgen
involves: 129P2/OlaHsd * C57BL/6
MGI:99842  MP:0001973 increased thermal nociceptive threshold
General Comments
Physiological role remains unknown.
Available Assays
DiscoveRx PathHunter® eXpress HTR1F U2OS β-Arrestin GPCR Assay (Cat no. 93-0699E3CP0M)
PathHunter® U2OS HTR1F β-Arrestin Cell Line (Cat no. 93-0699C3)
more info

REFERENCES

1. Adham N, Bard JA, Zgombick JM, Durkin MM, Kucharewicz S, Weinshank RL, Branchek TA. (1997) Cloning and characterization of the guinea pig 5-HT1F receptor subtype: a comparison of the pharmacological profile to the human species homolog. Neuropharmacology36: 569-576. [PMID:9225282]

2. Adham N, Borden LA, Schechter LE, Gustafson EL, Cochran TL, Vaysse PJ, Weinshank RL, Branchek TA. (1993) Cell-specific coupling of the cloned human 5-HT1F receptor to multiple signal transduction pathways. Naunyn Schmiedebergs Arch Pharmacol348: 566-575. [PMID:8133900]

3. Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA. (1993) Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. Proc Natl Acad Sci U S A90: 408-412. [PMID:8380639]

4. Amlaiky N, Ramboz S, Boschert U, Plassat JL, Hen R. (1992) Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus. J. Biol. Chem.267 (28): 19761-4. [PMID:1328180]

5. Brown AM, Avenell K, Young TJ, Ho M, Porter RA, Vimal M, Middlemiss DN. (1998) BRL 54443, a potent agonist with selectivity for human cloned 5-HT1E and 5-HT1F receptors. British Journal of Pharmacology123 (1): 233.

6. Guptan P, Dhingra A, Panicker MM. (1997) Multiple transcripts encode the 5-HT1F receptor in rodent brain. Neuroreport8: 3317-3321. [PMID:9351664]

7. John GW, Pauwels PJ, Perez M, Halazy S, Le Grand B, Verscheure Y, Valentin JP, Palmier C, Wurch T, Chopin P, Marien M, Kleven MS, Koek W, Assie MB, Carilla-Durand E, Tarayre JP, Colpaert FC. (1999) F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine. J Pharmacol Exp Ther290: 83-95. [PMID:10381763]

8. Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG. (1993) Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes. Proc Natl Acad Sci U S A90: 2184-2188. [PMID:8384716]

9. Ma QP. (2001) Co-localization of 5-HT(1B/1D/1F) receptors and glutamate in trigeminal ganglia in rats. Neuroreport12: 1589-1591. [PMID:11409721]

10. Napier C, Stewart M, Melrose H, Hopkins B, McHarg A, Wallis R. (1999) Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol368: 259-268. [PMID:10193663]

11. Nelson DL, Phebus LA, Johnson KW, Wainscott DB, Cohen ML, Calligaro DO, Xu YC. (2010) Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan. Cephalalgia30 (10): 1159-69. [PMID:20855361]

12. Nilsson T, Longmore J, Shaw D, Pantev E, Bard JA, Branchek T, Edvinsson L. (1999) Characterisation of 5-HT receptors in human coronary arteries by molecular and pharmacological techniques. Eur J Pharmacol372: 49-56. [PMID:10374714]

13. Phebus LA, Johnson KW, Zgombick JM, Gilbert PJ, Van Belle K, Mancuso V, Nelson DL, Calligaro DO, Kiefer AD, Branchek TA, Flaugh ME. (1997) Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci61: 2117-212. [PMID:9395253]

14. Price GW, Burton MJ, Collin LJ, Duckworth M, Gaster L, Gothert M, Jones BJ, Roberts C, Watson JM, Middlemiss DN. (1997) SB-216641 and BRL-15572 compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch. Pharmacol.356: 312-320. [PMID:9303567]

15. Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE. (1996) Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl)124: 57-73. [PMID:8935801]

16. Stefulj J, Jernej B, Cicin-Sain L, Rinner I, Schauenstein K. (2000) mRNA expression of serotonin receptors in cells of the immune tissues of the rat. Brain Behav Immun14: 219-224. [PMID:10970681]

17. Wainscott DB, Krushinski JH, Audia JE, Schaus JM, Zgombick JM, Lucaites VL, Nelson DL. (2005) [3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties. Naunyn Schmiedebergs Arch Pharmacol371: 169-177. [PMID:15900510]

18. Watson J, Brough S, Coldwell MC, Gager T, Ho M, Hunter AJ, Jerman J, Middlemiss DN, Riley GJ, Brown AM. (1998) Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors. Br J Pharmacol125: 1413-1420. [PMID:9884068]

To cite this database page, please use the following:

Rodrigo Andrade, Nicholas M. Barnes, Gordon Baxter, Joel Bockaert, Theresa Branchek, Marlene L. Cohen, Aline Dumuis, Richard M. Eglen, Manfred Göthert, Mark Hamblin, Michel Hamon, Paul R. Hartig, René Hen, Katharine Herrick-Davis, Rebecca Hills, Daniel Hoyer, Patrick P. A. Humphrey, Klaus Peter Latté, Luc Maroteaux, Graeme R. Martin, Derek N. Middlemiss, Ewan Mylecharane, Stephen J. Peroutka, Pramod R. Saxena, Andrew Sleight, Carlos M. Villalon, Frank Yocca.
5-Hydroxytryptamine receptors: 5-HT1F receptor. Last modified on 10/02/2014. Accessed on 31/10/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=5.

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