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5-HT1D receptor

Family: 5-Hydroxytryptamine receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Antagonists
Allosteric Regulators
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Functional Assays
Physiological Functions
Phenotypes, Alleles and Disease Models
Biologically Significant Variants
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 377 1p36.3-p34.3 HTR1D 5-hydroxytryptamine (serotonin) receptor 1D, G protein-coupled 45
Mouse 7 374 4 D3 Htr1d 5-hydroxytryptamine (serotonin) receptor 1D 46
Rat 7 374 5q36 Htr1d 5-hydroxytryptamine (serotonin) receptor 1D, G protein-coupled 10
Previous and Unofficial Names
Names References
5-HT1Dα 45
5-HT 1Dα
HTRL
RDC4
HT1DA
5-HT1D
5-hydroxytryptamine (serotonin) receptor 1D
5HT1D
5-HT-1D
5-hydroxytryptamine receptor 1D
serotonin receptor 1D
Gpcr14
Htr1db
AI853647
Database Links
ChEMBL Target 105 (Hs), 18065 (Mm), 10578 (Rn)
DrugBank Target 725 (Hs)
Ensembl ENSG00000179546 (Hs), ENSMUSG00000070687 (Mm), ENSRNOG00000012038 (Rn)
Entrez Gene 3352 (Hs), 15552 (Mm), 25323 (Rn)
GeneCards HTR1D (Hs)
GenitoUrinary Development Molecular Anatomy Project Htr1d (Mm)
HomoloGene 20240 (Hs)
Human Protein Reference Database 01636 (Hs)
InterPro P28221 (Hs), Q61224 (Mm), P28565 (Rn)
KEGG Gene hsa:3352 (Hs), mmu:15552 (Mm), rno:25323 (Rn)
OMIM 182133 (Hs)
PharmGKB Gene PA29550 (Hs)
PhosphoSitePlus P28221 (Hs), Q61224 (Mm), P28565 (Rn)
Protein Ontology (PRO) PRO:000001163 (Hs)
RefSeq Nucleotide NM_000864 (Hs), NM_008309 (Mm), NM_012852 (Rn)
RefSeq Protein NP_000855 (Hs), NP_032335 (Mm), NP_036984 (Rn)
TreeFam ENSG00000179546 (Hs), ENSMUSG00000070687 (Mm), ENSRNOG00000012038 (Rn)
UniGene Hs. 121482 (Hs)
UniProt P28221 (Hs), Q61224 (Mm), P28565 (Rn)
Wikipedia 5-HT1D receptor
5-Hydroxytryptamine receptors
Search for 3D structures on the PDB
Search by keyword: 5-Hydroxytryptamine receptors 5-HT1D receptor Search by accession number: P28565, P28221, Q61224
Natural/Endogenous Ligand(s)
5-HT
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]5-CT Hs Agonist 9.1 pKd 49
[3H]eletriptan Hs Full agonist 9.1 pKd 26
[3H]8-OH-DPAT Hs Full agonist 9.0 pKd 27
[125I]GTI Rn Agonist 8.9 pKd 2
[3H]alniditan Hs Full agonist 8.85 – 8.92 pKd 16
[3H]5-HT Hs Full agonist 8.2 – 8.6 pKd 16,39,45
[3H]sumatriptan Hs Full agonist 8.2 pKd 26
donitriptan Rn Full agonist 9.6 pKi 12
dihydroergotamine Hs Full agonist 9.2 – 9.9 pKi 9,16-17
oxymetazoline Hs Partial agonist 9.4 pKi 15
donitriptan Hs Full agonist 9.3 pKi 12
7-methoxy-1-naphthylpiperazine Hs Full agonist 9.2 pKi 13
lysergol Hs Full agonist 9.2 pKi 45
PNU109291 Gg Agonist 9.1 pKi 6
alniditan Hs Full agonist 8.7 – 9.4 pKi 16-17
L-694,247 Hs Agonist 9.0 pKi 48
lisuride Hs Partial agonist 9.0 pKi 21
ziprasidone Hs Full agonist 9.0 pKi 38
5-CT Hs Full agonist 8.6 – 9.2 pKi 9,17,45
eletriptan Hs Full agonist 8.9 pKi 26
(+)-lysergic acid Hs Full agonist 8.8 – 9.0 pKi 17
zolmitriptan Hs Full agonist 8.9 pKi 26
GR-127935 Hs Partial agonist 8.6 – 9.1 pKi 7,13,33,39,42
naratriptan Hs Full agonist 8.4 – 9.0 pKi 5,26,35
CGS-12066 Hs Full agonist 8.5 – 8.6 pKi 9,45
5-HT Hs Full agonist 8.0 – 9.0 pKi 3,9,17,27,39,42,45
asenapine Hs Full agonist 8.4 pKi 38
sumatriptan Hs Full agonist 8.0 – 8.7 pKi 9,17,22,26,45
xanomeline Hs Full agonist 8.2 pKi 43
1-naphthylpiperazine Hs Full agonist 8.1 – 8.2 pKi 13,45
cabergoline Hs Partial agonist 8.1 pKi 21
5-MeOT Hs Full agonist 7.4 – 8.7 pKi 9,17,45
bromocriptine Hs Partial agonist 8.0 pKi 21
BRL-15572 Hs Partial agonist 7.9 pKi 33
pergolide Hs Partial agonist 7.9 pKi 21
rizatriptan Hs Full agonist 7.9 pKi 26
terguride Hs Partial agonist 7.8 pKi 21
RU 24969 Hs Full agonist 7.7 pKi 9
SB 216641 Hs Partial agonist 7.6 pKi 33
aripiprazole Hs Full agonist 7.2 pKi 40
dimethyltryptamine Hs Full agonist 7.0 – 7.3 pKi 17
TFMPP Hs Full agonist 7.1 – 7.2 pKi 9,45
8-OH-DPAT Hs Full agonist 6.9 – 7.3 pKi 5,17,26
tryptamine Hs Full agonist 6.8 – 7.4 pKi 17,45
roxindole Hs Partial agonist 7.0 – 7.2 pKi 21,27
EMDT Hs Full agonist 6.5 pKi 8
clozapine Hs Full agonist 6.4 pKi 38
α-methyl-5-HT Hs Full agonist 6.1 – 6.6 pKi 17
LY344864 Hs Full agonist 6.2 pKi 29
olanzapine Hs Full agonist 6.2 pKi 38
2-methyl-5-HT Hs Full agonist 5.7 – 6.2 pKi 17,45
quetiapine Hs Full agonist 5.7 pKi 38
SL65.0155 Hs Partial agonist 5.1 pKi 24
dipropyl-5-CT Hs Full agonist 7.9 pIC50 45
CP-122288 Hs Full agonist 7.7 pIC50 5
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
[3H]GR 125,743 Hs Antagonist 8.6 pKd 49
zotepine Hs Antagonist 9.3 pKi 38
SB 714786 Hs Antagonist 9.1 pKi 41
metergoline Hs Antagonist 8.6 – 9.2 pKi 5,9,17
SB 649915 Hs Antagonist 8.8 pKi 41
ocaperidone Hs Antagonist 8.7 – 8.8 pKi 17
SB 272183 Hs Antagonist 8.7 pKi 44
methysergide Hs Antagonist 8.4 – 8.9 pKi 17,45
GR-127935 Hs Antagonist 8.3 – 8.6 pKi 17
9-OH-risperidone Hs Antagonist 7.9 pKi 38
BRL-15572 Hs Antagonist 7.9 pKi 33
risperidone Hs Antagonist 7.8 – 8.0 pKi 17,38
bufotenine Hs Antagonist 7.7 – 8.0 pKi 17
rauwolscine Hs Antagonist 7.8 pKi 45
methiothepin Hs Inverse agonist 7.3 – 8.2 pKi 5,9,17,42
ritanserin Hs Antagonist 7.6 pKi 17
(+)-WAY 100135 Hs Antagonist 7.6 pKi 3
ketanserin Hs Antagonist 7.4 – 7.5 pKi 5,17
yohimbine Hs Antagonist 7.2 – 7.7 pKi 9,17,22,45
sertindole Hs Antagonist 7.2 pKi 38
cyanopindolol Hs Antagonist 7.1 pKi 9
S33084 Hs Antagonist 6.9 pKi 20
pipamperone Hs Antagonist 6.8 pKi 38
m-CPP Hs Antagonist 6.7 pKi 9
haloperidol Hs Antagonist 6.6 pKi 38
SB 224289 Hs Antagonist 6.3 pKi 7,39
fluspirilene Hs Antagonist 6.0 pKi 38
SB 277011-A Hs Antagonist 5.8 pKi 34
spiperone Hs Antagonist 5.5 – 6.0 pKi 9,45
MPDT Hs Antagonist 5.2 pKi 8
L-772,405 Hs Antagonist 9.0 pIC50 37
Allosteric Regulators
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
5-HT-moduline Hs Negative 12.0 pIC50 36

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

Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  9,18
Tissue Distribution
Trigeminal ganglion.
Species:  Human
Technique:  immunocytochemistry.
References:  11
Spinal cord: dorsal horn > ventral horn.
Species:  Human
Technique:  Radioligand binding.
References:  14
Poorly expressed in coronary arteries, atrium, ventricle and epicardium.
Species:  Human
Technique:  RT-PCR.
References:  28
Benign and malignant prostate tissue.
Species:  Human
Technique:  Western blotting.
References:  4
Globus pallidus > frontal cortex > putamen.
Species:  Human
Technique:  Radioligand binding.
References:  23
Trigeminal ganglion.
Species:  Rat
Technique:  Immunohistochemistry.
References:  19
Dorsal root ganglion and trigeminal ganglion.
Species:  Rat
Technique:  immunocytochemistry.
References:  32
Lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  30
Expression Datasets

Click here to show/hide data

Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays
Measurement of cAMP levels in mouse adrenal Y-1 cells transfected with the 5-HT1D receptor.
Species:  Human
Tissue:  Y-1 cells.
Response measured:  Inhibition of cAMP accumulation.
References:  45
Physiological Functions
Growth hormone release.
Species:  Human
Tissue:  In vivo.
References:  25,47
Inhibition of 5-HT release.
Species:  Rat
Tissue:  in vivo and mesencephalic raphe slices.
References:  31
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Htr1dtm1Lex Htr1dtm1Lex/Htr1dtm1Lex
involves: 129S5/SvEvBrd * C57BL/6J		 MGI:96276  MP:0002169 no abnormal phenotype detected
Biologically Significant Variants
Three polymorphisms, 1123 T -> G, 628 T-> C and 2190 A -> G have a possible association with anorexia nervosa.
Type:  Single nucletide polymorphisms.
Species:  Human
References:  1

REFERENCES

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To cite this database 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-HT1D receptor. Last modified on 12/02/2013. Accessed on 22/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=3.


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