Nomenclature: 5-HT1D receptor

Family: 5-Hydroxytryptamine receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates. 

Contents

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 9
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
DrugBank Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligands
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
pKd 9.1 (Kd 9x10-10 M) [49]
[3H]eletriptan Hs Full agonist 9.1 pKd 26
pKd 9.1 (Kd 9x10-10 M) [26]
[3H]8-OH-DPAT Hs Full agonist 9.0 pKd 27
pKd 9.0 (Kd 1x10-9 M) [27]
[125I]GTI Rn Agonist 8.9 pKd 2
pKd 8.9 (Kd 1.3x10-9 M) [2]
[3H]alniditan Hs Full agonist 8.85 – 8.92 pKd 16
pKd 8.85 – 8.92 (Kd 1.2x10-9 – 1.4x10-9 M) [16]
[3H]5-HT Hs Full agonist 8.2 – 8.6 pKd 16,39,45
pKd 8.2 – 8.6 [16,39,45]
[3H]sumatriptan Hs Full agonist 8.2 pKd 26
pKd 8.2 (Kd 7x10-9 M) [26]
donitriptan Rn Full agonist 9.6 pKi 12
pKi 9.6 [12]
dihydroergotamine Hs Full agonist 9.2 – 9.9 pKi 10,16-17
pKi 9.2 – 9.9 [10,16-17]
oxymetazoline Hs Partial agonist 9.4 pKi 15
pKi 9.4 [15]
donitriptan Hs Full agonist 9.3 pKi 12
pKi 9.3 [12]
7-methoxy-1-naphthylpiperazine Hs Full agonist 9.2 pKi 13
pKi 9.2 [13]
lysergol Hs Full agonist 9.2 pKi 45
pKi 9.2 [45]
ergotamine Hs Agonist 9.1 pKi 8
pKi 9.1 (Ki 8x10-10 M) [8]
PNU109291 Gg Agonist 9.1 pKi 6
pKi 9.1 (Ki 9x10-10 M) [6]
alniditan Hs Full agonist 8.7 – 9.4 pKi 16-17
pKi 8.7 – 9.4 [16-17]
lisuride Hs Partial agonist 9.0 pKi 21
pKi 9.0 [21]
L-694,247 Hs Agonist 9.0 pKi 48
pKi 9.0 (Ki 1x10-9 M) [48]
ziprasidone Hs Full agonist 9.0 pKi 38
pKi 9.0 [38]
5-CT Hs Full agonist 8.6 – 9.2 pKi 10,17,45
pKi 8.6 – 9.2 [10,17,45]
zolmitriptan Hs Full agonist 8.9 pKi 26
pKi 8.9 [26]
eletriptan Hs Full agonist 8.9 pKi 26
pKi 8.9 [26]
lysergic acid Hs Full agonist 8.8 – 9.0 pKi 17
pKi 8.8 – 9.0 [17]
GR-127935 Hs Partial agonist 8.6 – 9.1 pKi 7,13,33,39,44
pKi 8.6 – 9.1 [7,13,33,39,44]
naratriptan Hs Full agonist 8.4 – 9.0 pKi 5,26,35
pKi 8.4 – 9.0 [5,26,35]
CGS-12066 Hs Full agonist 8.5 – 8.6 pKi 10,45
pKi 8.5 – 8.6 [10,45]
5-HT Hs Full agonist 8.0 – 9.0 pKi 3,10,17,27,39,44-45
pKi 8.0 – 9.0 [3,10,17,27,39,44-45]
asenapine Hs Full agonist 8.4 pKi 38
pKi 8.4 [38]
frovatriptan Hs Agonist 8.36 pKi 50
pKi 8.36 (Ki 4.4x10-9 M) [50]
sumatriptan Hs Full agonist 8.0 – 8.7 pKi 10,17,22,26,45
pKi 8.0 – 8.7 [10,17,22,26,45]
xanomeline Hs Full agonist 8.2 pKi 42
pKi 8.2 [42]
1-naphthylpiperazine Hs Full agonist 8.1 – 8.2 pKi 13,45
pKi 8.1 – 8.2 [13,45]
cabergoline Hs Partial agonist 8.1 pKi 21
pKi 8.1 [21]
5-MeOT Hs Full agonist 7.4 – 8.7 pKi 10,17,45
pKi 7.4 – 8.7 [10,17,45]
bromocriptine Hs Partial agonist 8.0 pKi 21
pKi 8.0 [21]
pergolide Hs Partial agonist 7.9 pKi 21
pKi 7.9 [21]
rizatriptan Hs Full agonist 7.9 pKi 26
pKi 7.9 [26]
BRL-15572 Hs Partial agonist 7.9 pKi 33
pKi 7.9 [33]
terguride Hs Partial agonist 7.8 pKi 21
pKi 7.8 [21]
RU 24969 Hs Full agonist 7.7 pKi 10
pKi 7.7 [10]
SB 216641 Hs Partial agonist 7.6 pKi 33
pKi 7.6 [33]
aripiprazole Hs Full agonist 7.2 pKi 40
pKi 7.2 [40]
dimethyltryptamine Hs Full agonist 7.0 – 7.3 pKi 17
pKi 7.0 – 7.3 [17]
TFMPP Hs Full agonist 7.1 – 7.2 pKi 10,45
pKi 7.1 – 7.2 [10,45]
tryptamine Hs Full agonist 6.8 – 7.4 pKi 17,45
pKi 6.8 – 7.4 [17,45]
8-OH-DPAT Hs Full agonist 6.9 – 7.3 pKi 5,17,26
pKi 6.9 – 7.3 [5,17,26]
roxindole Hs Partial agonist 7.0 – 7.2 pKi 21,27
pKi 7.0 – 7.2 [21,27]
EMDT Hs Full agonist 6.5 pKi 8
pKi 6.5 [8]
clozapine Hs Full agonist 6.4 pKi 38
pKi 6.4 [38]
α-methyl-5-HT Hs Full agonist 6.1 – 6.6 pKi 17
pKi 6.1 – 6.6 [17]
olanzapine Hs Full agonist 6.2 pKi 38
pKi 6.2 [38]
LY344864 Hs Full agonist 6.2 pKi 29
pKi 6.2 [29]
2-methyl-5-HT Hs Full agonist 5.7 – 6.2 pKi 17,45
pKi 5.7 – 6.2 [17,45]
quetiapine Hs Full agonist 5.7 pKi 38
pKi 5.7 [38]
SL65.0155 Hs Partial agonist 5.1 pKi 24
pKi 5.1 [24]
dipropyl-5-CT Hs Full agonist 7.9 pIC50 45
pIC50 7.9 [45]
CP-122288 Hs Full agonist 7.7 pIC50 5
pIC50 7.7 [5]
View species-specific agonist tables
Agonist Comments
Frovatriptan is selective for 1B and 1D 5-HT receptor subtypes over the 1A subtype [50].
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
pKd 8.6 (Kd 2.8x10-9 M) [49]
zotepine Hs Antagonist 9.3 pKi 38
pKi 9.3 [38]
SB 714786 Hs Antagonist 9.1 pKi 41
pKi 9.1 [41]
metergoline Hs Antagonist 8.6 – 9.2 pKi 5,10,17
pKi 8.6 – 9.2 [5,10,17]
SB 649915 Hs Antagonist 8.8 pKi 41
pKi 8.8 [41]
ocaperidone Hs Antagonist 8.7 – 8.8 pKi 17
pKi 8.7 – 8.8 [17]
SB 272183 Hs Antagonist 8.7 pKi 43
pKi 8.7 [43]
methysergide Hs Antagonist 8.4 – 8.9 pKi 17,45
pKi 8.4 – 8.9 [17,45]
GR-127935 Hs Antagonist 8.3 – 8.6 pKi 17
pKi 8.3 – 8.6 [17]
risperidone Hs Antagonist 7.8 – 8.0 pKi 17,38
pKi 7.8 – 8.0 [17,38]
9-OH-risperidone Hs Antagonist 7.9 pKi 38
pKi 7.9 [38]
BRL-15572 Hs Antagonist 7.9 pKi 33
pKi 7.9 [33]
bufotenine Hs Antagonist 7.7 – 8.0 pKi 17
pKi 7.7 – 8.0 [17]
rauwolscine Hs Antagonist 7.8 pKi 45
pKi 7.8 [45]
methiothepin Hs Inverse agonist 7.3 – 8.2 pKi 5,10,17,44
pKi 7.3 – 8.2 [5,10,17,44]
(+)-WAY 100135 Hs Antagonist 7.6 pKi 3
pKi 7.6 [3]
ritanserin Hs Antagonist 7.6 pKi 17
pKi 7.6 [17]
ketanserin Hs Antagonist 7.4 – 7.5 pKi 5,17
pKi 7.4 – 7.5 [5,17]
yohimbine Hs Antagonist 7.2 – 7.7 pKi 10,17,22,45
pKi 7.2 – 7.7 [10,17,22,45]
sertindole Hs Antagonist 7.2 pKi 38
pKi 7.2 [38]
cyanopindolol Hs Antagonist 7.1 pKi 10
pKi 7.1 [10]
S33084 Hs Antagonist 6.9 pKi 20
pKi 6.9 [20]
pipamperone Hs Antagonist 6.8 pKi 38
pKi 6.8 [38]
m-CPP Hs Antagonist 6.7 pKi 10
pKi 6.7 [10]
haloperidol Hs Antagonist 6.6 pKi 38
pKi 6.6 [38]
SB 224289 Hs Antagonist 6.3 pKi 7,39
pKi 6.3 [7,39]
fluspirilene Hs Antagonist 6.0 pKi 38
pKi 6.0 [38]
SB 277011-A Hs Antagonist 5.8 pKi 34
pKi 5.8 [34]
spiperone Hs Antagonist 5.5 – 6.0 pKi 10,45
pKi 5.5 – 6.0 [10,45]
MPDT Hs Antagonist 5.2 pKi 8
pKi 5.2 [8]
L-772,405 Hs Antagonist 9.0 pIC50 37
pIC50 9.0 [37]
Allosteric Modulators
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
pIC50 12.0 [36]
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  10,18
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

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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
Type:  Single nucletide polymorphisms.
Species:  Human
Description:  Three polymorphisms, 1123 T -> G, 628 T-> C and 2190 A -> G have a possible association with anorexia nervosa.
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 24/04/2014. Accessed on 24/07/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=3.

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