5-HT<sub>1F</sub> receptor | 5-Hydroxytryptamine receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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5-HT1F receptor

Target not currently curated in GtoImmuPdb

Target id: 5

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.  » Email us

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 receptor 1F 3
Mouse 7 366 16 C1.3 Htr1f 5-hydroxytryptamine (serotonin) receptor 1F 6
Rat 7 366 11p12 Htr1f 5-hydroxytryptamine receptor 1F 9
Previous and Unofficial Names
5-HT1Eβ [9] | 5-HT6 | 5-HT1F | HTR1EL | serotonin receptor 1F | 5-hydroxytryptamine (serotonin) receptor 1F, G protein-coupled
Database Links
Specialist databases
GPCRDB 5ht1f_human (Hs), 5ht1f_mouse (Mm), 5ht1f_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein
Natural/Endogenous Ligands

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]LY334370 Hs Full agonist 9.4 pKd 18
pKd 9.4 (Kd 3.98x10-10 M) [18]
[125I]LSD Mm Agonist 9.0 pKd 4
pKd 9.0 (Kd 9.8x10-10 M) [4]
5-hydroxytryptamine Hs Full agonist 8.0 pKd 3
pKd 8.0 [3]
BRL-54443 Hs Full agonist 8.9 pKi 5
pKi 8.9 [5]
LY334370 Hs Full agonist 8.7 pKi 18
pKi 8.7 (Ki 1.99x10-9 M) [18]
lasmiditan Hs Full agonist 8.7 pKi 12
pKi 8.7 [12]
5-BODMT Hs Agonist 8.4 pKi 8
pKi 8.4 (Ki 3.6x10-9 M) [8]
LY344864 Hs Full agonist 8.2 pKi 14
pKi 8.2 (Ki 6.31x10-9 M) [14]
naratriptan Hs Full agonist 8.2 pKi 11,18
pKi 8.2 [11,18]
eletriptan Hs Full agonist 8.0 pKi 11
pKi 8.0 (Ki 1x10-8 M) [11]
5-hydroxytryptamine Hs Full agonist 7.7 – 8.0 pKi 1,3,18
pKi 7.7 – 8.0 [1,3,18]
sumatriptan Hs Full agonist 7.2 – 7.9 pKi 1,3,11,18
pKi 7.2 – 7.9 [1,3,11,18]
zolmitriptan Hs Full agonist 7.4 – 7.5 pKi 11,18
pKi 7.4 – 7.5 [11,18]
5-MeO-DMT Hs Full agonist 7.4 pKi 3
pKi 7.4 [3]
clozapine Hs Full agonist 6.9 pKi 16
pKi 6.9 [16]
dihydroergotamine Hs Full agonist 6.6 – 7.1 pKi 1,18
pKi 6.6 – 7.1 [1,18]
GR 127935 Hs Partial agonist 6.4 – 7.2 pKi 15,18
pKi 6.4 – 7.2 [15,18]
ergotamine Hs Full agonist 6.8 pKi 3
pKi 6.8 [3]
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 11,18
pKi 6.4 – 6.8 [11,18]
olanzapine Hs Full agonist 6.5 pKi 16
pKi 6.5 [16]
xanomeline Hs Full agonist 6.5 pKi 19
pKi 6.5 [19]
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 15
pKi 6.0 [15]
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]
8-OH-DPAT 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]
DOI Hs Full agonist 5.8 pKi 3
pKi 5.8 [3]
quetiapine Hs Full agonist 5.6 pKi 16
pKi 5.6 [16]
tryptamine Hs Full agonist 5.6 pKi 3
pKi 5.6 [3]
donitriptan Hs Full agonist 5.5 pKi 7
pKi 5.5 [7]
ergotamine Rn Full agonist 7.3 pIC50 9
pIC50 7.3 [9]
5-hydroxytryptamine Rn Full agonist 7.2 pIC50 9
pIC50 7.2 [9]
sumatriptan Hs Full agonist 7.2 pIC50 9
pIC50 7.2 [9]
5-CT Rn Full agonist 5.6 pIC50 9
pIC50 5.6 [9]
View species-specific agonist tables
Agonist Comments
Compared to other family members, BRL-54443 is selective for 5-HT1e and 5-HT1F receptors [5].
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
methysergide Hs Antagonist 8.2 pKi 3,18
pKi 8.2 [3,18]
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 16
pKi 6.4 [16]
methiothepin Hs Antagonist 6.2 pKi 1,3
pKi 6.2 [1,3]
risperidone Hs Antagonist 5.9 pKi 16
pKi 5.9 [16]
methysergide Rn Antagonist 7.8 pIC50 9
pIC50 7.8 [9]
metergoline Rn Antagonist 6.3 pIC50 9
pIC50 6.3 [9]
yohimbine Rn Antagonist 6.2 pIC50 9
pIC50 6.2 [9]
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:  13
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:  10
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  17
Brain: cortex, striatum, hippocampus > thalamus, pons > hypothalamus > cerebellum.
Species:  Rat
Technique:  RT-PCR.
References:  9
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]

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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:  9
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.


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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. Neuropharmacology, 36: 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 Pharmacol, 348: 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 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 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 Pharmacology, 123 (1): 233.

6. Guptan P, Dhingra A, Panicker MM. (1997) Multiple transcripts encode the 5-HT1F receptor in rodent brain. Neuroreport, 8: 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 Ther, 290: 83-95. [PMID:10381763]

8. Klein MT, Dukat M, Glennon RA, Teitler M. (2011) Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J. Pharmacol. Exp. Ther., 337 (3): 860-7. [PMID:21422162]

9. 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 A, 90: 2184-2188. [PMID:8384716]

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

11. 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 Pharmacol, 368: 259-268. [PMID:10193663]

12. 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]

13. 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 Pharmacol, 372: 49-56. [PMID:10374714]

14. 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 Sci, 61: 2117-212. [PMID:9395253]

15. 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]

16. 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]

17. 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 Immun, 14: 219-224. [PMID:10970681]

18. 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 Pharmacol, 371: 169-177. [PMID:15900510]

19. 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 Pharmacol, 125: 1413-1420. [PMID:9884068]


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How to cite this page

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 16/02/2018. Accessed on 16/09/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=5.