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5-HT1F

Previous and Unofficial Names
Names References
5-HT6
5-HT1Eβ 157
Structural Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Name Reference
Human 7 366 3p12 HTR1F 154
Rat 7 366 11p12 Htr1f 157
Mouse 7 366 16 C1.3 Htr1f 158
Contents:
Previous and Unofficial Names
Structural Information
Database Links
Agonists
Antagonists
Transduction Mechanisms
Tissue Distribution
Functional Assays
Receptor Comments
Database Links
ChEMBL Target 279 (Hs), 17109 (Mm), 10619 (Rn)
Ensembl ENSG00000179097 (Hs), ENSMUSG00000050783 (Mm), ENSRNOG00000000716 (Rn)
Entrez Gene 3355 (Hs), 15557 (Mm), 60448 (Rn)
GeneCards HTR1F (Hs)
HomoloGene 37361 (Hs)
OMIM 182134 (Hs)
PharmGKB Gene PA29553 (Hs)
Protein Ontology (PRO) PRO:000001165 (Hs)
RefSeq Nucleotide NM_000866 (Hs), NM_008310 (Mm), NM_021857 (Rn)
RefSeq Protein NP_000857 (Hs), NP_032336 (Mm), NP_068629 (Rn)
UniGene Hs. 248136 (Hs)
UniProt P30939 (Hs), Q02284 (Mm), P30940 (Rn)
Wikipedia 5-HT1F
Search for 3D structures on the PDB
Search using keywords: 5-Hydroxytryptamine receptors 5-HT1F Search using accession numbers: P30940 || P30939 || Q02284
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]LY334370 Hs Full agonist 9.4 pKd 63
5-HT Hs Full agonist 8.0 pKd 154
LY334370 Hs Full agonist 8.7 pKi 63
LY344864 Hs Full agonist 8.2 pKi 64
naratriptan Hs Full agonist 8.2 pKi 63,72
eletriptan Hs Full agonist 8.0 pKi 72
5-HT Hs Full agonist 7.7 – 8.0 pKi 63,154,160
sumatriptan Hs Full agonist 7.2 – 7.9 pKi 63,72,154,160
zolmitriptan Hs Full agonist 7.4 – 7.5 pKi 63,72
5-MeO-DMT Hs Full agonist 7.4 pKi 154
clozapine Hs Full agonist 6.9 pKi 65
dihydroergotamine Hs Full agonist 6.6 – 7.1 pKi 63,160
ergotamine Hs Full agonist 6.8 pKi 154
GR-127935 Hs Partial agonist 6.4 – 7.2 pKi 58,63
α-methyl-5-HT Hs Full agonist 6.7 pKi 154
NAN 190 Hs Partial agonist 6.7 pKi 154
rizatriptan Hs Full agonist 6.4 – 6.8 pKi 63,72
olanzapine Hs Full agonist 6.5 pKi 65
xanomeline Hs Full agonist 6.5 pKi 73
2-methyl-5-HT Hs Full agonist 6.4 pKi 154
5-CT Hs Full agonist 6.1 pKi 154,160
BRL-15572 Hs Partial agonist 6.0 pKi 58
TFMPP Hs Full agonist 6.0 pKi 154
5-MeOT Hs Full agonist 5.9 pKi 154
8-OH-DPAT Hs Full agonist 5.8 pKi 154
dipropyl-5-CT Hs Full agonist 5.8 pKi 154
DOI Hs Full agonist 5.8 pKi 154
quetiapine Hs Full agonist 5.6 pKi 65
tryptamine Hs Full agonist 5.6 pKi 154
donitriptan Hs Full agonist 5.5 pKi 71
ergotamine Rn Full agonist 7.3 pIC50 157
5-HT Rn Full agonist 7.2 pIC50 157
sumatriptan Hs Full agonist 7.2 pIC50 157
5-CT Rn Full agonist 5.6 pIC50 157
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
methysergide Hs Antagonist 8.2 pKi 63,154
methylergonovine Hs Antagonist 7.5 pKi 154
1-naphthylpiperazine Hs Antagonist 7.3 pKi 154,160
yohimbine Hs Antagonist 7.0 pKi 154
metergoline Hs Antagonist 6.5 pKi 154,160
sertindole Hs Antagonist 6.4 pKi 65
methiothepin Hs Antagonist 6.2 pKi 154,160
risperidone Hs Antagonist 5.9 pKi 65
methysergide Rn Antagonist 7.8 pIC50 157
metergoline Rn Antagonist 6.3 pIC50 157
yohimbine Rn Antagonist 6.2 pIC50 157
View species-specific antagonist tables

Explore drug-target interactions for this set of compounds using iPHACE

Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  159
Tissue Distribution
Brain, uterus (endometrium and myometrium), mesentery.
Species:  Human
Technique:  PCR.
References:  154
Ventricle wall > atrium, epicardium, coronary artery.
Species:  Human
Technique:  RT-PCR.
References:  29
Trigeminal ganglion.
Species:  Rat
Technique:  Immunohistochemistry.
References:  109
Thymus, peripheral blood lymphocytes, spleen, mitogen-activated spleen cells.
Species:  Rat
Technique:  RT-PCR.
References:  116
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:  154
Brain: cortex, striatum, hippocampus > thalamus, pons > hypothalamus > cerebellum.
Species:  Rat
Technique:  RT-PCR.
References:  157
Functional Assays
Measurement of cAMP levels in LM(tk-) cells
Species:  Human
Tissue:  LM(tk-) cells.
Response measured:  Weak inhibition of cAMP accumulation.
References:  154
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:  157
Receptor Comments
Physiological role remains unknown.

To cite this receptor data page, please use the following:

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. Last modified on 2010-06-28. Accessed on 2010-09-03. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=5.


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