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5-HT1F receptor

Family: 5-Hydroxytryptamine receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Phenotypes, Alleles and Disease Models
General Comments
References
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-HT6
5-HT1Eβ 8
5-HT1Eb
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 279 (Hs), 17109 (Mm), 10619 (Rn)
DrugBank Target 511 (Hs)
Ensembl ENSG00000179097 (Hs), ENSMUSG00000050783 (Mm), ENSRNOG00000000716 (Rn)
Entrez Gene 3355 (Hs), 15557 (Mm), 60448 (Rn)
GeneCards HTR1F (Hs)
GenitoUrinary Development Molecular Anatomy Project Htr1f (Mm)
HomoloGene 37361 (Hs)
Human Protein Reference Database 01637 (Hs)
InterPro P30939 (Hs), Q02284 (Mm), P30940 (Rn)
KEGG Gene hsa:3355 (Hs), mmu:15557 (Mm), rno:60448 (Rn)
OMIM 182134 (Hs)
PharmGKB Gene PA29553 (Hs)
PhosphoSitePlus P30939 (Hs), Q02284 (Mm), P30940 (Rn)
Protein Ontology (PRO) PRO:000001165 (Hs)
RefSeq Nucleotide NM_000866 (Hs), NM_008310 (Mm), NM_021857 (Rn)
RefSeq Protein NP_000857 (Hs), NP_032336 (Mm), NP_068629 (Rn)
TreeFam ENSG00000179097 (Hs), ENSMUSG00000050783 (Mm), ENSRNOG00000000716 (Rn)
UniGene Hs. 248136 (Hs)
UniProt P30939 (Hs), Q02284 (Mm), P30940 (Rn)
Wikipedia 5-HT1F receptor
5-Hydroxytryptamine receptors
Search for 3D structures on the PDB
Search by keyword: 5-Hydroxytryptamine receptors 5-HT1F receptor Search by accession number: P30940, P30939, Q02284
Natural/Endogenous Ligand(s)
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
[125I]LSD Mm Agonist 9.0 pKd 4
5-HT Hs Full agonist 8.0 pKd 3
BRL-54443 Hs Full agonist 8.9 pKi 5
LY334370 Hs Full agonist 8.7 pKi 17
LY573144 Hs Full agonist 8.7 pKi 11
LY344864 Hs Full agonist 8.2 pKi 13
naratriptan Hs Full agonist 8.2 pKi 10,17
eletriptan Hs Full agonist 8.0 pKi 10
5-HT Hs Full agonist 7.7 – 8.0 pKi 1,3,17
10-OBn-7α-F-gingkolide B Hs Full agonist 7.2 – 7.9 pKi
sumatriptan Hs Full agonist 7.2 – 7.9 pKi 1,3,10,17
zolmitriptan Hs Full agonist 7.4 – 7.5 pKi 10,17
5-MeO-DMT Hs Full agonist 7.4 pKi 3
clozapine Hs Full agonist 6.9 pKi 15
dihydroergotamine Hs Full agonist 6.6 – 7.1 pKi 1,17
ergotamine Hs Full agonist 6.8 pKi 3
GR-127935 Hs Partial agonist 6.4 – 7.2 pKi 14,17
α-methyl-5-HT Hs Full agonist 6.7 pKi 3
NAN 190 Hs Partial agonist 6.7 pKi 3
rizatriptan Hs Full agonist 6.4 – 6.8 pKi 10,17
olanzapine Hs Full agonist 6.5 pKi 15
xanomeline Hs Full agonist 6.5 pKi 18
2-methyl-5-HT Hs Full agonist 6.4 pKi 3
5-CT Hs Full agonist 6.1 pKi 1,3
BRL-15572 Hs Partial agonist 6.0 pKi 14
TFMPP Hs Full agonist 6.0 pKi 3
5-MeOT Hs Full agonist 5.9 pKi 3
8-OH-DPAT Hs Full agonist 5.8 pKi 3
dipropyl-5-CT Hs Full agonist 5.8 pKi 3
DOI Hs Full agonist 5.8 pKi 3
quetiapine Hs Full agonist 5.6 pKi 15
tryptamine Hs Full agonist 5.6 pKi 3
donitriptan Hs Full agonist 5.5 pKi 7
ergotamine Rn Full agonist 7.3 pIC50 8
5-HT Rn Full agonist 7.2 pIC50 8
sumatriptan Hs Full agonist 7.2 pIC50 8
5-CT Rn Full agonist 5.6 pIC50 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
methylergonovine Hs Antagonist 7.5 pKi 3
1-naphthylpiperazine Hs Antagonist 7.3 pKi 1,3
yohimbine Hs Antagonist 7.0 pKi 3
metergoline Hs Antagonist 6.5 pKi 1,3
sertindole Hs Antagonist 6.4 pKi 15
methiothepin Hs Antagonist 6.2 pKi 1,3
risperidone Hs Antagonist 5.9 pKi 15
methysergide Rn Antagonist 7.8 pIC50 8
metergoline Rn Antagonist 6.3 pIC50 8
yohimbine Rn Antagonist 6.2 pIC50 8
View species-specific antagonist tables

Explore drug-target interactions for this set of compounds using iPHACE

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

Click here to show/hide data

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]

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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

Click here to show/hide data

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.

REFERENCES

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1. Adham, N., Bard, J. A., Zgombick, J. M., Durkin, M. M., Kucharewicz, S., Weinshank, R. L. and Branchek, T. A. (1997) Cloning and characterization of the guinea pig 5-HT1F receptor subtype: a comparison of the pharmacological profile to the human species homolog. Neuropharmacology, 36: 569-576. [PMID:9225282]

2. Adham, N., Borden, L. A., Schechter, L. E., Gustafson, E. L., Cochran, T. L., Vaysse, P. J., Weinshank, R. L. and Branchek, T. A. (1993) Cell-specific coupling of the cloned human 5-HT1F receptor to multiple signal transduction pathways. Naunyn Schmiedebergs Arch Pharmacol, 348: 566-575. [PMID:8133900]

3. Adham, N., Kao, H. T., Schecter, L. E., Bard, J., Olsen, M., Urquhart, D., Durkin, M., Hartig, P. R., Weinshank, R. L. and Branchek, T. A. (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 A, 90: 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, A.M., Avenell, K., Young, T.J., Ho, M., Porter, R.A., Vimal, M and Middlemiss, D.N. (1998) BRL 54443, a potent agonist with selectivity for human cloned 5-HT1E and 5-HT1F receptors. British Journal of Pharmacology, 123 (1): 233.

6. Guptan, P., Dhingra, A. and Panicker, M. M. (1997) Multiple transcripts encode the 5-HT1F receptor in rodent brain. Neuroreport, 8: 3317-3321. [PMID:9351664]

7. John, G. W., Pauwels, P. J., Perez, M., Halazy, S., Le Grand, B., Verscheure, Y., Valentin, J. P., Palmier, C., Wurch, T., Chopin, P., Marien, M., Kleven, M. S., Koek, W., Assie, M. B., Carilla-Durand, E., Tarayre, J. P. and Colpaert, F. C. (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 Ther, 290: 83-95. [PMID:10381763]

8. Lovenberg, T. W., Erlander, M. G., Baron, B. M., Racke, M., Slone, A. L., Siegel, B. W., Craft, C. M., Burns, J. E., Danielson, P. E. and Sutcliffe, J. G. (1993) Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes. Proc Natl Acad Sci U S A, 90: 2184-2188. [PMID:8384716]

9. Ma, Q. P. (2001) Co-localization of 5-HT(1B/1D/1F) receptors and glutamate in trigeminal ganglia in rats. Neuroreport, 12: 1589-1591. [PMID:11409721]

10. Napier, C., Stewart, M., Melrose, H., Hopkins, B., McHarg, A. and 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 Pharmacol, 368: 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. Cephalalgia, 30 (10): 1159-69. [PMID:20855361]

12. Nilsson, T., Longmore, J., Shaw, D., Pantev, E., Bard, J. A., Branchek, T. and Edvinsson, L. (1999) Characterisation of 5-HT receptors in human coronary arteries by molecular and pharmacological techniques. Eur J Pharmacol, 372: 49-56. [PMID:10374714]

13. Phebus, L. A., Johnson, K. W., Zgombick, J. M., Gilbert, P. J., Van Belle, K., Mancuso, V., Nelson, D. L., Calligaro, D. O., Kiefer, A. D., Branchek, T. A. and Flaugh, M. E. (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 Sci, 61: 2117-212. [PMID:9395253]

14. Price, G. W., Burton, M. J., Collin, L. J., Duckworth, M., Gaster, L., Gothert, M., Jones, B. J., Roberts, C., Watson, J. M. and Middlemiss, D. N. (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, P. F., Gommeren, W., Luyten, W. H., Van Gompel, P., Lesage, A. S., De Loore, K. and Leysen, J. E. (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. and Schauenstein, K. (2000) mRNA expression of serotonin receptors in cells of the immune tissues of the rat. Brain Behav Immun, 14: 219-224. [PMID:10970681]

17. Wainscott, D. B., Krushinski, J. H., Audia, J. E., Schaus, J. M., Zgombick, J. M., Lucaites, V. L. and Nelson, D. L. (2005) [3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties. Naunyn Schmiedebergs Arch Pharmacol, 371: 169-177. [PMID:15900510]

18. Watson, J., Brough, S., Coldwell, M. C., Gager, T., Ho, M., Hunter, A. J., Jerman, J., Middlemiss, D. N., Riley, G. J. and Brown, A. M. (1998) Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors. Br J Pharmacol, 125: 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 25/02/2013. Accessed on 21/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=5.


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