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{{ | {{DISPLAYTITLE:5-HT<sub>1F</sub> receptor}} | ||
< | {{Infobox_gene}} | ||
{{ | '''5-hydroxytryptamine (serotonin) receptor 1F''', also known as '''HTR1F''' is a [[5-HT1 receptor|5-HT<sub>1</sub> receptor]] [[protein]] and also denotes the human [[gene]] encoding it.<ref name="entrez">{{cite web | title = Entrez Gene: HTR1F 5-hydroxytryptamine (serotonin) receptor 1F| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3355| accessdate = }}</ref><ref name="pmid8380639">{{cite journal | vauthors = Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA | title = Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 90 | issue = 2 | pages = 408–12 | date = Jan 1993 | pmid = 8380639 | pmc = 45671 | doi = 10.1073/pnas.90.2.408 | url = http://www.pnas.org/cgi/pmidlookup?view=long&pmid=8380639 }}</ref><ref name="pmid8384716">{{cite journal | vauthors = Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG | title = Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 90 | issue = 6 | pages = 2184–8 | date = Mar 1993 | pmid = 8384716 | pmc = 46050 | doi = 10.1073/pnas.90.6.2184 | url = http://www.pnas.org/cgi/pmidlookup?view=long&pmid=8384716 }}</ref><ref name="pmid9394293">{{cite journal | vauthors = Erdmann J, Shimron-Abarbanell D, Shridhar V, Smith DI, Propping P, Nöthen MM | title = Assignment of the human serotonin 1F receptor gene (HTR1F) to the short arm of chromosome 3 (3p13-p14.1) | journal = Molecular Membrane Biology | volume = 14 | issue = 3 | pages = 133–5 | year = 1997 | pmid = 9394293 | doi = 10.3109/09687689709048173 }}</ref><ref name="pmid9632173">{{cite journal | vauthors = Maassen VanDenBrink A, Vergouwe MN, Ophoff RA, Naylor SL, Dauwerse HG, Saxena PR, Ferrari MD, Frants RR | title = Chromosomal localization of the 5-HT1F receptor gene: no evidence for involvement in response to sumatriptan in migraine patients | journal = American Journal of Medical Genetics | volume = 77 | issue = 5 | pages = 415–20 | date = Jun 1998 | pmid = 9632173 | doi = 10.1002/(SICI)1096-8628(19980605)77:5<415::AID-AJMG12>3.0.CO;2-L }}</ref> | ||
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==Agonists== | |||
< | * 5-''n''-Butyryloxy-DMT:<ref>{{cite journal | vauthors = Klein MT, Dukat M, Glennon RA, Teitler M | title = Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 337 | issue = 3 | pages = 860–7 | date = Jun 2011 | pmid = 21422162 | pmc = 3101003 | doi = 10.1124/jpet.111.179606 }}</ref> >60-fold selectivity versus 5-HT<sub>1E</sub> receptor | ||
{{ | * [[BRL-54443]] - mixed 5-HT<sub>1E/1F</sub> agonist | ||
| | * [[Eletriptan]] - mixed 5-HT<sub>1B/1D/1E/1F/2B/7</sub> agonist | ||
| | * [[LY334370|LY-334,370]]<ref name="pmid15900510">{{cite journal | vauthors = Wainscott DB, Krushinski JH, Audia JE, Schaus JM, Zgombick JM, Lucaites VL, Nelson DL | title = [3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties | journal = Naunyn-Schmiedeberg's Archives of Pharmacology | volume = 371 | issue = 3 | pages = 169–77 | date = Mar 2005 | pmid = 15900510 | doi = 10.1007/s00210-005-1035-9 }}</ref> - as well as related [[benzamide]]s<ref name="pmid15546719">{{cite journal | vauthors = 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 | title = Design, synthesis and evaluation of bicyclic benzamides as novel 5-HT1F receptor agonists | journal = Bioorganic & Medicinal Chemistry Letters | volume = 14 | issue = 24 | pages = 6011–6 | date = Dec 2004 | pmid = 15546719 | doi = 10.1016/j.bmcl.2004.09.079 }}</ref> | ||
}} | * LY-344,864 (N-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluorobenzamide) | ||
* [[Naratriptan]] - mixed 5-HT<sub>1B/1D/1F</sub> agonist | |||
* [[Lasmiditan]] - selective 5-HT<sub>1F</sub> agonist, a first-in-class [[ditan]] molecule | |||
== | ==Antagonists== | ||
==See also== | ''MLS000756415''<ref>[https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4140 PudChem: MLS000756415]</ref> | ||
== See also == | |||
* [[5-HT1 receptor|5-HT<sub>1</sub> receptor]] | * [[5-HT1 receptor|5-HT<sub>1</sub> receptor]] | ||
* [[5-HT receptor]] | * [[5-HT receptor]] | ||
{{clear}} | |||
== References == | |||
{{reflist|33em}} | |||
== | == Further reading == | ||
{{ | {{refbegin |33em}} | ||
* {{cite journal | vauthors = Hoyer D, Hannon JP, Martin GR | title = Molecular, pharmacological and functional diversity of 5-HT receptors | journal = Pharmacology, Biochemistry, and Behavior | volume = 71 | issue = 4 | pages = 533–54 | date = Apr 2002 | pmid = 11888546 | doi = 10.1016/S0091-3057(01)00746-8 }} | |||
* {{cite journal | vauthors = Raymond JR, Mukhin YV, Gelasco A, Turner J, Collinsworth G, Gettys TW, Grewal JS, Garnovskaya MN | title = Multiplicity of mechanisms of serotonin receptor signal transduction | journal = Pharmacology & Therapeutics | volume = 92 | issue = 2-3 | pages = 179–212 | year = 2002 | pmid = 11916537 | doi = 10.1016/S0163-7258(01)00169-3 }} | |||
* {{cite journal | vauthors = Amlaiky N, Ramboz S, Boschert U, Plassat JL, Hen R | title = Isolation of a mouse "5HT1E-like" serotonin receptor expressed predominantly in hippocampus | journal = The Journal of Biological Chemistry | volume = 267 | issue = 28 | pages = 19761–4 | date = Oct 1992 | pmid = 1328180 | doi = }} | |||
* {{cite journal | vauthors = Adham N, Kao HT, Schecter LE, Bard J, Olsen M, Urquhart D, Durkin M, Hartig PR, Weinshank RL, Branchek TA | title = Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 90 | issue = 2 | pages = 408–12 | date = Jan 1993 | pmid = 8380639 | pmc = 45671 | doi = 10.1073/pnas.90.2.408 }} | |||
* {{cite journal | vauthors = Lovenberg TW, Erlander MG, Baron BM, Racke M, Slone AL, Siegel BW, Craft CM, Burns JE, Danielson PE, Sutcliffe JG | title = Molecular cloning and functional expression of 5-HT1E-like rat and human 5-hydroxytryptamine receptor genes | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 90 | issue = 6 | pages = 2184–8 | date = Mar 1993 | pmid = 8384716 | pmc = 46050 | doi = 10.1073/pnas.90.6.2184 }} | |||
* {{cite journal | vauthors = Maassen VanDenBrink A, Vergouwe MN, Ophoff RA, Naylor SL, Dauwerse HG, Saxena PR, Ferrari MD, Frants RR | title = Chromosomal localization of the 5-HT1F receptor gene: no evidence for involvement in response to sumatriptan in migraine patients | journal = American Journal of Medical Genetics | volume = 77 | issue = 5 | pages = 415–20 | date = Jun 1998 | pmid = 9632173 | doi = 10.1002/(SICI)1096-8628(19980605)77:5<415::AID-AJMG12>3.0.CO;2-L }} | |||
* {{cite journal | vauthors = Bhatnagar A, Sheffler DJ, Kroeze WK, Compton-Toth B, Roth BL | title = Caveolin-1 interacts with 5-HT2A serotonin receptors and profoundly modulates the signaling of selected Galphaq-coupled protein receptors | journal = The Journal of Biological Chemistry | volume = 279 | issue = 33 | pages = 34614–23 | date = Aug 2004 | pmid = 15190056 | doi = 10.1074/jbc.M404673200 }} | |||
* {{cite journal | vauthors = Hannula-Jouppi K, Kaminen-Ahola N, Taipale M, Eklund R, Nopola-Hemmi J, Kääriäinen H, Kere J | title = The axon guidance receptor gene ROBO1 is a candidate gene for developmental dyslexia | journal = PLoS Genetics | volume = 1 | issue = 4 | pages = e50 | date = Oct 2005 | pmid = 16254601 | pmc = 1270007 | doi = 10.1371/journal.pgen.0010050 }} | |||
{{refend}} | |||
== | == External links == | ||
* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2318 | title = 5-HT<sub>1F</sub> | accessdate = | authorlink = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | archiveurl = | archivedate = | quote = }} | |||
* {{UCSC gene info|HTR1F}} | |||
*{{cite | |||
*{{ | |||
{{NLM content}} | {{NLM content}} | ||
{{G protein-coupled receptors}} | {{G protein-coupled receptors}} | ||
[[Category: | {{Serotonergics}} | ||
{{DEFAULTSORT:5-Ht1f Receptor}} | |||
[[Category:Serotonin receptors]] | |||
{{transmembranereceptor-stub}} |
Revision as of 17:13, 29 August 2017
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External IDs | GeneCards: [1] | ||||||
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Species | Human | Mouse | |||||
Entrez |
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Ensembl |
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UniProt |
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RefSeq (mRNA) |
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RefSeq (protein) |
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Location (UCSC) | n/a | n/a | |||||
PubMed search | n/a | n/a | |||||
Wikidata | |||||||
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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.[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
References
- ↑ "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. 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. 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.
- ↑ 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
- 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.
- 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. 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. 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. 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
- "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.
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