5-HT1F receptor explained
5-hydroxytryptamine (serotonin) receptor 1F, also known as HTR1F is a 5-HT1 receptor protein and also denotes the human gene encoding it.[1] [2] [3] [4] [5]
Agonists
- 5-n-Butyryloxy-DMT:[6] >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[7] - as well as related benzamides[8]
- 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
MLS000756415[9]
See also
Further reading
- Hoyer D, Hannon JP, Martin GR . Molecular, pharmacological and functional diversity of 5-HT receptors . Pharmacology Biochemistry and Behavior . 71 . 4 . 533–54 . Apr 2002 . 11888546 . 10.1016/S0091-3057(01)00746-8 . 25543069 .
- Raymond JR, Mukhin YV, Gelasco A, Turner J, Collinsworth G, Gettys TW, Grewal JS, Garnovskaya MN . Multiplicity of mechanisms of serotonin receptor signal transduction . Pharmacology & Therapeutics . 92 . 2–3 . 179–212 . 2002 . 11916537 . 10.1016/S0163-7258(01)00169-3 .
- Amlaiky N, Ramboz S, Boschert U, Plassat JL, Hen R . Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus . The Journal of Biological Chemistry . 267 . 28 . 19761–4 . Oct 1992 . 10.1016/S0021-9258(19)88617-9 . 1328180 . free .
- Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA . 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 . Jan 1993 . 8380639 . 45671 . 10.1073/pnas.90.2.408 . 1993PNAS...90..408A . free .
- Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG . 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 . Mar 1993 . 8384716 . 46050 . 10.1073/pnas.90.6.2184 . 1993PNAS...90.2184L . free .
- Maassen VanDenBrink A, Vergouwe MN, Ophoff RA, Naylor SL, Dauwerse HG, Saxena PR, Ferrari MD, Frants RR . 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 . Jun 1998 . 9632173 . 10.1002/(SICI)1096-8628(19980605)77:5<415::AID-AJMG12>3.0.CO;2-L .
- Bhatnagar A, Sheffler DJ, Kroeze WK, Compton-Toth B, Roth BL. Bryan Roth . 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 . Aug 2004 . 15190056 . 10.1074/jbc.M404673200 . free .
- Hannula-Jouppi K, Kaminen-Ahola N, Taipale M, Eklund R, Nopola-Hemmi J, Kääriäinen H, Kere J . The axon guidance receptor gene ROBO1 is a candidate gene for developmental dyslexia . PLOS Genetics . 1 . 4 . e50 . Oct 2005 . 16254601 . 1270007 . 10.1371/journal.pgen.0010050 . free .
External links
- Web site: 5-HT1F . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology .
Notes and References
- Web site: 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 . 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 . Jan 1993 . 8380639 . 45671 . 10.1073/pnas.90.2.408 . 1993PNAS...90..408A . free .
- Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG . 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 . Mar 1993 . 8384716 . 46050 . 10.1073/pnas.90.6.2184 . 1993PNAS...90.2184L . free .
- Erdmann J, Shimron-Abarbanell D, Shridhar V, Smith DI, Propping P, Nöthen MM . 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 . 1997 . 9394293 . 10.3109/09687689709048173 .
- Maassen VanDenBrink A, Vergouwe MN, Ophoff RA, Naylor SL, Dauwerse HG, Saxena PR, Ferrari MD, Frants RR . 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 . Jun 1998 . 9632173 . 10.1002/(SICI)1096-8628(19980605)77:5<415::AID-AJMG12>3.0.CO;2-L .
- Klein MT, Dukat M, Glennon RA, 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 . The Journal of Pharmacology and Experimental Therapeutics . 337 . 3 . 860–7 . Jun 2011 . 21422162 . 3101003 . 10.1124/jpet.111.179606 .
- Wainscott DB, Krushinski JH, Audia JE, Schaus JM, Zgombick JM, Lucaites VL, Nelson DL . [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 . Mar 2005 . 15900510 . 10.1007/s00210-005-1035-9 . 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 . Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists . Bioorganic & Medicinal Chemistry Letters . 14 . 24 . 6011–6 . Dec 2004 . 15546719 . 10.1016/j.bmcl.2004.09.079 .
- https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4140 PudChem: MLS000756415
