5-HT1F receptor
Appearance
HTR1F | |||||||||||||||||||||||||||||||||||||||||||||||||||
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Identifiers | |||||||||||||||||||||||||||||||||||||||||||||||||||
Aliases | HTR1F, 5-HT-1F, 5-HT1F, 5HT6, HTR1EL, MR77, 5-HT1F receptor, 5-hydroxytryptamine receptor 1F | ||||||||||||||||||||||||||||||||||||||||||||||||||
External IDs | OMIM: 182134; MGI: 99842; HomoloGene: 37361; GeneCards: HTR1F; OMA:HTR1F - orthologs | ||||||||||||||||||||||||||||||||||||||||||||||||||
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5-hydroxytryptamine (serotonin) receptor 1F, also known as HTR1F is a 5-HT1 receptor protein and also denotes the human gene encoding it.[5][6][7][8][9]
Agonists
[edit]- 5-n-Butyryloxy-DMT:[10] >60-fold selectivity versus 5-HT1E receptor
- BRL-54443 - mixed 5-HT1E/1F agonist
- Eletriptan - mixed 5-HT1B/1D/1E/1F/2B/7 agonist
- LY-334,370[11] - as well as related benzamides[12]
- LY-344,864 (N-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluorobenzamide)
- Naratriptan - mixed 5-HT1B/1D/1F agonist
- Lasmiditan - selective 5-HT1F agonist, a first-in-class ditan molecule
Antagonists
[edit]MLS000756415[13]
See also
[edit]References
[edit]- ^ a b c GRCh38: Ensembl release 89: ENSG00000179097 – Ensembl, May 2017
- ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000050783 – Ensembl, May 2017
- ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
- ^ "Entrez Gene: HTR1F 5-hydroxytryptamine (serotonin) receptor 1F".
- ^ Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA (Jan 1993). "Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase". Proceedings of the National Academy of Sciences of the United States of America. 90 (2): 408–12. Bibcode:1993PNAS...90..408A. doi:10.1073/pnas.90.2.408. PMC 45671. PMID 8380639.
- ^ Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG (Mar 1993). "Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes". Proceedings of the National Academy of Sciences of the United States of America. 90 (6): 2184–8. Bibcode:1993PNAS...90.2184L. doi:10.1073/pnas.90.6.2184. PMC 46050. PMID 8384716.
- ^ Erdmann J, Shimron-Abarbanell D, Shridhar V, Smith DI, Propping P, Nöthen MM (1997). "Assignment of the human serotonin 1F receptor gene (HTR1F) to the short arm of chromosome 3 (3p13-p14.1)". Molecular Membrane Biology. 14 (3): 133–5. doi:10.3109/09687689709048173. PMID 9394293.
- ^ Maassen VanDenBrink A, Vergouwe MN, Ophoff RA, Naylor SL, Dauwerse HG, Saxena PR, Ferrari MD, Frants RR (Jun 1998). "Chromosomal localization of the 5-HT1F receptor gene: no evidence for involvement in response to sumatriptan in migraine patients". American Journal of Medical Genetics. 77 (5): 415–20. doi:10.1002/(SICI)1096-8628(19980605)77:5<415::AID-AJMG12>3.0.CO;2-L. PMID 9632173.
- ^ Klein MT, Dukat M, Glennon RA, Teitler M (Jun 2011). "Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships". The Journal of Pharmacology and Experimental Therapeutics. 337 (3): 860–7. doi:10.1124/jpet.111.179606. PMC 3101003. PMID 21422162.
- ^ Wainscott DB, Krushinski JH, Audia JE, Schaus JM, Zgombick JM, Lucaites VL, Nelson DL (Mar 2005). "[3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties". Naunyn-Schmiedeberg's Archives of Pharmacology. 371 (3): 169–77. doi:10.1007/s00210-005-1035-9. PMID 15900510. S2CID 2230855.
- ^ Zhang D, Kohlman D, Krushinski J, Liang S, Ying BP, Reilly JE, Dinn SR, Wainscott DB, Nutter S, Gough W, Nelson DL, Schaus JM, Xu YC (Dec 2004). "Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists". Bioorganic & Medicinal Chemistry Letters. 14 (24): 6011–6. doi:10.1016/j.bmcl.2004.09.079. PMID 15546719.
- ^ PudChem: MLS000756415
Further reading
[edit]- Hoyer D, Hannon JP, Martin GR (Apr 2002). "Molecular, pharmacological and functional diversity of 5-HT receptors". Pharmacology Biochemistry and Behavior. 71 (4): 533–54. doi:10.1016/S0091-3057(01)00746-8. PMID 11888546. S2CID 25543069.
- Raymond JR, Mukhin YV, Gelasco A, Turner J, Collinsworth G, Gettys TW, Grewal JS, Garnovskaya MN (2002). "Multiplicity of mechanisms of serotonin receptor signal transduction". Pharmacology & Therapeutics. 92 (2–3): 179–212. doi:10.1016/S0163-7258(01)00169-3. PMID 11916537.
- Amlaiky N, Ramboz S, Boschert U, Plassat JL, Hen R (Oct 1992). "Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus". The Journal of Biological Chemistry. 267 (28): 19761–4. doi:10.1016/S0021-9258(19)88617-9. PMID 1328180.
- Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA (Jan 1993). "Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase". Proceedings of the National Academy of Sciences of the United States of America. 90 (2): 408–12. Bibcode:1993PNAS...90..408A. doi:10.1073/pnas.90.2.408. PMC 45671. PMID 8380639.
- Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG (Mar 1993). "Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes". Proceedings of the National Academy of Sciences of the United States of America. 90 (6): 2184–8. Bibcode:1993PNAS...90.2184L. doi:10.1073/pnas.90.6.2184. PMC 46050. PMID 8384716.
- Maassen VanDenBrink A, Vergouwe MN, Ophoff RA, Naylor SL, Dauwerse HG, Saxena PR, Ferrari MD, Frants RR (Jun 1998). "Chromosomal localization of the 5-HT1F receptor gene: no evidence for involvement in response to sumatriptan in migraine patients". American Journal of Medical Genetics. 77 (5): 415–20. doi:10.1002/(SICI)1096-8628(19980605)77:5<415::AID-AJMG12>3.0.CO;2-L. PMID 9632173.
- Bhatnagar A, Sheffler DJ, Kroeze WK, Compton-Toth B, Roth BL (Aug 2004). "Caveolin-1 interacts with 5-HT2A serotonin receptors and profoundly modulates the signaling of selected Galphaq-coupled protein receptors". The Journal of Biological Chemistry. 279 (33): 34614–23. doi:10.1074/jbc.M404673200. PMID 15190056.
- Hannula-Jouppi K, Kaminen-Ahola N, Taipale M, Eklund R, Nopola-Hemmi J, Kääriäinen H, Kere J (Oct 2005). "The axon guidance receptor gene ROBO1 is a candidate gene for developmental dyslexia". PLOS Genetics. 1 (4): e50. doi:10.1371/journal.pgen.0010050. PMC 1270007. PMID 16254601.
External links
[edit]- "5-HT1F". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- Human HTR1F genome location and HTR1F gene details page in the UCSC Genome Browser.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.