Gene Symbol: HTR1F
Description: 5-hydroxytryptamine receptor 1F
Alias: 5-HT-1F, 5-HT1F, 5HT6, HTR1EL, MR77, 5-hydroxytryptamine receptor 1F, 5-hydroxytryptamine (serotonin) receptor 1F, G protein-coupled, serotonin receptor 1F
Species: human
Products:     HTR1F

Top Publications

  1. Pan J, Deng F, Zeng B, Zheng P, Liang W, Yin B, et al. Absence of gut microbiota during early life affects anxiolytic Behaviors and monoamine neurotransmitters system in the hippocampal of mice. J Neurol Sci. 2019;400:160-168 pubmed publisher
    ..In total, 19 differential expressed genes (Htr7, Htr1f, Htr3b, Drd3, Ddc, Maob, Tdo2, Fos, Creb1, Akt1, Gsk3a, Pik3ca, Pla2g5, Cyp2d22, Grk6, Ephb1, Slc18a1, Nr4a1, Gdnf)..
  2. Tfelt Hansen P, Olesen J. The 5-HT1F receptor agonist lasmiditan as a potential treatment of migraine attacks: a review of two placebo-controlled phase II trials. J Headache Pain. 2012;13:271-5 pubmed publisher
    ..Larger studies including the parameters of patients' preferences are necessary to accurately position this new treatment principle in relation to the triptans. ..
  3. Cevoli S, Marzocchi N, Capellari S, Scapoli C, Pierangeli G, Grimaldi D, et al. Lack of association between five serotonin metabolism-related genes and medication overuse headache. J Headache Pain. 2010;11:53-8 pubmed publisher
    ..receptor 1A(5-HT1A), serotonin receptor 1B (5-HT1B), serotonin receptor 2A (5-HT2A) and serotonin receptor 6 (5HT6)genes...
  4. Martelletti P. The therapeutic armamentarium in migraine is quite elderly. Expert Opin Drug Metab Toxicol. 2015;11:175-7 pubmed publisher
  5. Shahidi S, Sadeghian R, Komaki A, Asl S. Intracerebroventricular microinjection of the 5-HT1F receptor agonist LY 344864 inhibits methamphetamine conditioned place preference reinstatement in rats. Pharmacol Biochem Behav. 2018;173:27-35 pubmed publisher
    ..These findings suggest that future studies should evaluate the therapeutic potential of 5-HT1F agonists for preventing relapse in individuals with METH addiction. ..
  6. Sawant Basak A, Obach R, Doran A, Lockwood P, Schildknegt K, Gao H, et al. Metabolism of a 5HT6 Antagonist, 2-Methyl-1-(Phenylsulfonyl)-4-(Piperazin-1-yl)-1H-Benzo[d]imidazole (SAM-760): Impact of Sulfonamide Metabolism on Diminution of a Ketoconazole-Mediated Clinical Drug-Drug Interaction. Drug Metab Dispos. 2018;46:934-942 pubmed publisher
    ..Thus, the disposition of [14C]SAM-760 in human hepatocytes via novel sulfonamide metabolism and CYP3A verified the lower than expected clinical DDI when SAM-760 was coadministered with ketoconazole. ..
  7. Liu K, Li J, Tan H, Du C, Xie W, Zhang Y, et al. Serotonin₆ receptors in the dorsal hippocampus regulate depressive-like behaviors in unilateral 6-hydroxydopamine-lesioned Parkinson's rats. Neuropharmacology. 2015;95:290-8 pubmed publisher
    ..In sham-operated rats, intra-DH injection of 5HT6 receptor agonist WAY208466 or antagonist SB258585 increased sucrose consumption and decreased immobility time, ..
  8. Andrews M, Tousi B, Sabbagh M. 5HT6 Antagonists in the Treatment of Alzheimer's Dementia: Current Progress. Neurol Ther. 2018;7:51-58 pubmed publisher
    ..The 5HT6 antagonists are a new class of medications to be offered...
  9. Yokoyama T, Nakamuta N, Kusakabe T, Yamamoto Y. Serotonin-mediated modulation of hypoxia-induced intracellular calcium responses in glomus cells isolated from rat carotid body. Neurosci Lett. 2015;597:149-53 pubmed publisher
    ..These results suggest that 5-HT increases hypoxia-induced [Ca(2+)]i responses in glomus cells. 5-HT may elevate hypoxic responses in glomus cells in order to increase chemosensory activity of the CB. ..

More Information


  1. LaPorta J, Hernandez L. Serotonin receptor expression is dynamic in the liver during the transition period in Holstein dairy cows. Domest Anim Endocrinol. 2015;51:65-73 pubmed publisher
    ..Additional research is needed to further explore the functional role of these receptors in the liver during the transition from pregnancy to lactation. ..
  2. Mitsikostas D, Tfelt Hansen P. Targeting to 5-HT1F receptor subtype for migraine treatment: lessons from the past, implications for the future. Cent Nerv Syst Agents Med Chem. 2012;12:241-9 pubmed
  3. Tso A, Goadsby P. New targets for migraine therapy. Curr Treat Options Neurol. 2014;16:318 pubmed publisher
    ..Hopefully in the coming years we will see a new era of migraine therapy, with multiple classes of better-tolerated, more effective agents targeting diverse yet specific migraine mechanisms. ..
  4. Dudek M, Marcinkowska M, Bucki A, Olczyk A, Kołaczkowski M. Idalopirdine - a small molecule antagonist of 5-HT6 with therapeutic potential against obesity. Metab Brain Dis. 2015;30:1487-94 pubmed publisher
    b>5HT6 receptor antagonists offer the potential for safe and effective drugs against obesity, because they can reduce weight without causing serious side effects in the cardiovascular system...
  5. Faulkner P, Mancinelli F, Lockwood P, Matarin M, Dolan R, Wood N, et al. Peripheral Serotonin 1B Receptor Transcription Predicts the Effect of Acute Tryptophan Depletion on Risky Decision-Making. Int J Neuropsychopharmacol. 2017;20:58-66 pubmed publisher
    ..Peripheral levels of serotonin markers may predict response to treatments that act upon the serotonin system, such as selective serotonin reuptake inhibitors. ..
  6. Vila Pueyo M. Targeted 5-HT1F Therapies for Migraine. Neurotherapeutics. 2018;15:291-303 pubmed publisher
    ..This review will focus on the characterisation of 5-HT1 receptor agonists and their effects as migraine therapies. ..
  7. Nagy R, Boutin T, Marten J, Huffman J, Kerr S, Campbell A, et al. Exploration of haplotype research consortium imputation for genome-wide association studies in 20,032 Generation Scotland participants. Genome Med. 2017;9:23 pubmed publisher
    ..near to Y_RNA and WDR4 and four new associations with heart rate at SNPs within CSMD1 and ASPH, upstream of HTR1F and between PROKR2 and GPCPD1. All were driven by rare variants (minor allele frequencies in the range of 0.08-1%)...
  8. Schuster N, Vollbracht S, Rapoport A. Emerging treatments for the primary headache disorders. Neurol Sci. 2015;36 Suppl 1:109-13 pubmed publisher
    ..Finally, we discuss patch, inhaled, and intranasal methods of triptan and dihydroergotamine delivery. ..
  9. Rubio Beltrán E, Labastida Ramírez A, Villalón C, Maassenvandenbrink A. Is selective 5-HT1F receptor agonism an entity apart from that of the triptans in antimigraine therapy?. Pharmacol Ther. 2018;186:88-97 pubmed publisher
    ..This review will be particularly focussed on the similarities and differences between the triptans and the ditans, their proposed sites of action, side effects and their cardiovascular risk profile. ..
  10. Parker C, Rabiner E, Gunn R, Searle G, Martarello L, Comley R, et al. Human Kinetic Modeling of the 5HT6 PET Radioligand 11C-GSK215083 and Its Utility for Determining Occupancy at Both 5HT6 and 5HT2A Receptors by SB742457 as a Potential Therapeutic Mechanism of Action in Alzheimer Disease. J Nucl Med. 2015;56:1901-9 pubmed publisher
    Antagonism of 5-hydroxytrypamine-6 (5HT6) receptors is associated with procognitive effects in preclinical species, suggesting a therapeutic potential for this mechanism in Alzheimer disease (AD) and other cognitive diseases...
  11. Diener H, Charles A, Goadsby P, Holle D. New therapeutic approaches for the prevention and treatment of migraine. Lancet Neurol. 2015;14:1010-22 pubmed publisher
  12. Naumovska Z, Nestorovska A, Filipce A, Sterjev Z, Brezovska K, Dimovski A, et al. Pharmacogenetics and antipsychotic treatment response. Pril (Makedon Akad Nauk Umet Odd Med Nauki). 2015;36:53-67 pubmed
    ..ABCB1 transporter gene, dopaminergic and serotonergic drug targets (DRD2, DRD3, DRD4, 5-HT1, 5HT-2A, 5HT-2C, 5HT6) as well as genes responsible for metabolism of neurotransmitters and G signalling pathways (5-HTTLPR, BDNF, COMT, ..
  13. Zhang D, Blanco M, Ying B, Kohlman D, Liang S, Victor F, et al. Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT₁ F receptor agonists: Evolution from bicyclic to monocyclic cores. Bioorg Med Chem Lett. 2015;25:4337-41 pubmed publisher
    ..Through this effort, the 2-F-phenyl and N-2-pyridyl series were also identified as potent and selective 5-HT1F receptor agonists. ..
  14. Gibbs W, Garrett S, Beeson C, Schnellmann R. Identification of Dual Mechanisms Mediating 5-hydroxytryptamine Receptor 1F Induced Mitochondrial Biogenesis. Am J Physiol Renal Physiol. 2017;:ajprenal.00324.2017 pubmed publisher
    ..Novel mechanisms of MB provide the foundation for new chemicals that induce MB to treat acute and chronic organ injuries...
  15. Raffaelli B, Israel H, Neeb L, Reuter U. The safety and efficacy of the 5-HT 1F receptor agonist lasmiditan in the acute treatment of migraine. Expert Opin Pharmacother. 2017;18:1409-1415 pubmed publisher
    ..The results of long-term Phase III studies will determine if these adverse events represent a limitation in clinical practice...
  16. Bhatnagar A, Sheffler D, Kroeze W, Compton Toth B, Roth B. Caveolin-1 interacts with 5-HT2A serotonin receptors and profoundly modulates the signaling of selected Galphaq-coupled protein receptors. J Biol Chem. 2004;279:34614-23 pubmed
    ..These studies provide compelling evidence for a prominent role of Cav-1 in regulating the functional activity of not only 5-HT(2A) serotonin receptors but also selected Galpha(q)-coupled receptors. ..
  17. Gong P, Zhang F, Ge W, Lei X, Chi W, Zhang K, et al. Association analysis of TPH2, 5-HT2A, and 5-HT6 with executive function in a young Chinese Han population. J Neurogenet. 2011;25:27-34 pubmed publisher
    ..05). The present study suggests that TPH2 contributes distinctively to the inhibition domain of executive function, whereas 5-HT2A and 5-HT6 show no striking effects on executive function in the Chinese Han population. ..
  18. Hoyer D, Hannon J, Martin G. Molecular, pharmacological and functional diversity of 5-HT receptors. Pharmacol Biochem Behav. 2002;71:533-54 pubmed
    ..The reward for unravelling this complex array of serotonin receptor--effector systems may be substantial, the ultimate prize being the development of important new drugs in a range of disease areas. ..
  19. Adham N, Kao H, Schecter L, Bard J, Olsen M, Urquhart D, et al. 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. 1993;90:408-12 pubmed
    ..9 nM) in transfected cells. These properties distinguish this receptor from any previously characterized and establish a fifth 5-HT1-like receptor subtype (5-HT1F) coupled to the inhibition of adenylate cyclase. ..
  20. Scholpa N, Lynn M, Corum D, Boger H, Schnellmann R. 5-HT1F Receptor-Mediated Mitochondrial Biogenesis for the Treatment of Parkinson's Disease. Br J Pharmacol. 2017;: pubmed publisher
  21. Maassen VanDenBrink A, Vergouwe M, Ophoff R, Naylor S, Dauwerse H, Saxena P, et al. Chromosomal localization of the 5-HT1F receptor gene: no evidence for involvement in response to sumatriptan in migraine patients. Am J Med Genet. 1998;77:415-20 pubmed
    ..No polymorphisms were detected in any of the patients. We therefore conclude that genetic diversity of the 5-HT1F receptor gene is most probably not responsible for the variable clinical response to sumatriptan. ..
  22. Almaca J, Molina J, Menegaz D, Pronin A, Tamayo A, Slepak V, et al. Human Beta Cells Produce and Release Serotonin to Inhibit Glucagon Secretion from Alpha Cells. Cell Rep. 2016;17:3281-3291 pubmed publisher
    ..Thus, modulation of serotonin signaling in the islet represents a drug intervention opportunity. ..
  23. Amlaiky N, Ramboz S, Boschert U, Plassat J, Hen R. Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus. J Biol Chem. 1992;267:19761-4 pubmed
    ..Our results therefore demonstrate that the 5HT1E receptors constitute a heterogeneous family of receptors. ..
  24. Turecki G, Sequeira A, Gingras Y, Seguin M, Lesage A, Tousignant M, et al. Suicide and serotonin: study of variation at seven serotonin receptor genes in suicide completers. Am J Med Genet B Neuropsychiatr Genet. 2003;118B:36-40 pubmed
    ..variation at genes that code for serotonin receptor 1B (5-HTR1B), 1Dalpha (5-HTR1Dalpha), 1E (5-HTR1E), 1F (5-HTR1F), 2C (5-HTR2C), 5A (5-HTR5A), and 6 (5-HTR6) in a total sample of 106 suicide completers and 120 normal controls...
  25. Klein M, Dukat M, Glennon R, Teitler M. 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. 2011;337:860-7 pubmed publisher
    ..The insights generated from this study will inform future drug development and molecular modeling studies for both 5-HT(1E) and 5-HT(1F) receptors. ..
  26. Videtic A, Pungercic G, Pajnic I, Zupanc T, Balazic J, Tomori M, et al. Association study of seven polymorphisms in four serotonin receptor genes on suicide victims. Am J Med Genet B Neuropsychiatr Genet. 2006;141B:669-72 pubmed
    ..067), but the correlation was not statistically significant. None of the tested genetic variants of serotonin receptors appears to be associated with suicidal behavior in the Slovenian population which has a relatively high suicide rate. ..
  27. Raymond J, Mukhin Y, Gelasco A, Turner J, Collinsworth G, Gettys T, et al. Multiplicity of mechanisms of serotonin receptor signal transduction. Pharmacol Ther. 2001;92:179-212 pubmed
    ..This review will focus on what is known about the signaling linkages of the G-protein-linked 5-HT receptors, and will highlight some fascinating new insights into 5-HT receptor signaling. ..
  28. Hannula Jouppi K, Kaminen Ahola N, Taipale M, Eklund R, Nopola Hemmi J, Kaariainen H, et al. The axon guidance receptor gene ROBO1 is a candidate gene for developmental dyslexia. PLoS Genet. 2005;1:e50 pubmed
    ..Thus, our data suggest that a slight disturbance in neuronal axon crossing across the midline between brain hemispheres, dendrite guidance, or another function of ROBO1 may manifest as a specific reading disability in humans. ..
  29. Lovenberg T, Erlander M, Baron B, Racke M, Slone A, Siegel B, et al. Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes. Proc Natl Acad Sci U S A. 1993;90:2184-8 pubmed
    ..The resulting product was subcloned and used to screen a rat genomic library to identify a full-length clone (MR77) containing an intronless open reading frame encoding a 366-amino acid seven-transmembrane domain protein...
  30. Corominas R, Sobrido M, Ribases M, Cuenca León E, Blanco Arias P, Narberhaus B, et al. Association study of the serotoninergic system in migraine in the Spanish population. Am J Med Genet B Neuropsychiatr Genet. 2010;153B:177-84 pubmed publisher
    ..These results suggest a differential involvement of serotonin-related genes in the genetic background of MO and MA. ..