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5-HT1D

Previous and Unofficial Names
Names References
5-HT1Dα 86
Structural Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Name Reference
Human 7 377 1p36.3-p34.3 HTR1D 86
Rat 7 374 5q36 Htr1d 137
Mouse 7 374 4 D3 Htr1d 138
Contents:
Previous and Unofficial Names
Structural Information
Database Links
Agonists
Antagonists
Allosteric Regulators
Transduction Mechanisms
Tissue Distribution
Functional Assays
Physiological Functions
Biologically Significant Variants
Database Links
ChEMBL Target 105 (Hs), 18065 (Mm), 10578 (Rn)
Ensembl ENSG00000179546 (Hs), ENSMUSG00000070687 (Mm), ENSRNOG00000012038 (Rn)
Entrez Gene 3352 (Hs), 15552 (Mm), 25323 (Rn)
GeneCards HTR1D (Hs)
HomoloGene 20240 (Hs)
OMIM 182133 (Hs)
PharmGKB Gene PA29550 (Hs)
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)
UniGene Hs. 121482 (Hs)
UniProt P28221 (Hs), Q61224 (Mm), P28565 (Rn)
Wikipedia 5-HT1D
Search for 3D structures on the PDB
Search using keywords: 5-Hydroxytryptamine receptors 5-HT1D Search using accession numbers: P28565 || P28221 || Q61224
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]8-OH-DPAT Hs Full agonist 9.1 pKd 48
[3H]eletriptan Hs Full agonist 9.0 pKd 72
[3H]alniditan Hs Full agonist 8.8 – 8.9 pKd 133
5-HT Hs Full agonist 8.2 – 8.6 pKd 86,128,133
[3H]sumatriptan Hs Full agonist 8.2 pKd 72
donitriptan Rn Full agonist 9.6 pKi 71
dihydroergotamine Hs Full agonist 9.2 – 9.9 pKi 133-134,139
oxymetazoline Hs Partial agonist 9.4 pKi 135
donitriptan Hs Full agonist 9.3 pKi 71
7-methoxy-1-naphthylpiperazine Hs Full agonist 9.2 pKi 49
lysergol Hs Full agonist 9.2 pKi 86
alniditan Hs Full agonist 8.7 – 9.4 pKi 133-134
lisuride Hs Partial agonist 9.0 pKi 69
ziprasidone Hs Full agonist 9.0 pKi 65
5-CT Hs Full agonist 8.6 – 9.2 pKi 86,134,139
eletriptan Hs Full agonist 8.9 pKi 72
(+)-lysergic acid Hs Full agonist 8.8 – 9.0 pKi 134
zolmitriptan Hs Full agonist 8.9 pKi 72
GR-127935 Hs Partial agonist 8.6 – 9.1 pKi 49,58,128,130,132
naratriptan Hs Full agonist 8.4 – 9.0 pKi 72,131,146
CGS-12066 Hs Full agonist 8.5 – 8.6 pKi 86,139
5-HT Hs Full agonist 8.0 – 9.0 pKi 48,86,127-128,130,134,139
ORG-5222 Hs Full agonist 8.4 pKi 65
sumatriptan Hs Full agonist 8.0 – 8.7 pKi 54,72,86,134,139
xanomeline Hs Full agonist 8.2 pKi 73
1-naphthylpiperazine Hs Full agonist 8.1 – 8.2 pKi 49,86
cabergoline Hs Partial agonist 8.1 pKi 69
5-MeOT Hs Full agonist 7.4 – 8.7 pKi 86,134,139
bromocriptine Hs Partial agonist 8.0 pKi 69
BRL-15572 Hs Partial agonist 7.9 pKi 58
pergolide Hs Partial agonist 7.9 pKi 69
rizatriptan Hs Full agonist 7.9 pKi 72
terguride Hs Partial agonist 7.8 pKi 69
RU 24969 Hs Full agonist 7.7 pKi 139
SB 216641 Hs Partial agonist 7.6 pKi 58
aripiprazole Hs Full agonist 7.2 pKi 70
dimethyltryptamine Hs Full agonist 7.0 – 7.3 pKi 134
TFMPP Hs Full agonist 7.1 – 7.2 pKi 86,139
8-OH-DPAT Hs Full agonist 6.9 – 7.3 pKi 72,131,134
tryptamine Hs Full agonist 6.8 – 7.4 pKi 86,134
roxindole Hs Partial agonist 7.0 – 7.2 pKi 48,69
EMDT Hs Full agonist 6.5 pKi 59
clozapine Hs Full agonist 6.4 pKi 65
α-methyl-5-HT Hs Full agonist 6.1 – 6.6 pKi 134
LY344864 Hs Full agonist 6.2 pKi 64
olanzapine Hs Full agonist 6.2 pKi 65
2-methyl-5-HT Hs Full agonist 5.7 – 6.2 pKi 86,134
quetiapine Hs Full agonist 5.7 pKi 65
SL65.0155 Hs Partial agonist 5.1 pKi 67
dipropyl-5-CT Hs Full agonist 7.9 pIC50 86
CP-122288 Hs Full agonist 7.7 pIC50 131
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
zotepine Hs Antagonist 9.3 pKi 65
SB 714786 Hs Antagonist 9.1 pKi 79
metergoline Hs Antagonist 8.6 – 9.2 pKi 131,134,139
SB 649915 Hs Antagonist 8.8 pKi 79
ocaperidone Hs Antagonist 8.7 – 8.8 pKi 134
SB 272183 Hs Antagonist 8.7 pKi 78
methysergide Hs Antagonist 8.4 – 8.9 pKi 86,134
GR-127935 Hs Antagonist 8.3 – 8.6 pKi 134
9-OH-risperidone Hs Antagonist 7.9 pKi 65
risperidone Hs Antagonist 7.8 – 8.0 pKi 65,134
bufotenine Hs Antagonist 7.7 – 8.0 pKi 134
rauwolscine Hs Antagonist 7.8 pKi 86
methiothepin Hs Inverse agonist 7.3 – 8.2 pKi 130-131,134,139
ritanserin Hs Antagonist 7.6 pKi 134
(+)-WAY 100135 Hs Antagonist 7.6 pKi 127
ketanserin Hs Antagonist 7.4 – 7.5 pKi 131,134
yohimbine Hs Antagonist 7.2 – 7.7 pKi 54,86,134,139
sertindole Hs Antagonist 7.2 pKi 65
cyanopindolol Hs Antagonist 7.1 pKi 139
S33084 Hs Antagonist 6.9 pKi 75
pipamperone Hs Antagonist 6.8 pKi 65
m-CPP Hs Antagonist 6.7 pKi 139
haloperidol Hs Antagonist 6.6 pKi 65
SB 224289 Hs Antagonist 6.3 pKi 128,132
fluspirilene Hs Antagonist 6.0 pKi 65
SB 277011-A Hs Antagonist 5.8 pKi 147
spiperone Hs Antagonist 5.5 – 6.0 pKi 86,139
MPDT Hs Antagonist 5.2 pKi 59
L-772,405 Hs Antagonist 9.0 pIC50 60
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 136

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

Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
References:  7,139
Tissue Distribution
Benign and malignant prostate tissue.
Species:  Human
Technique:  Western blotting.
References:  25
Trigeminal ganglion.
Species:  Rat
Technique:  Immunohistochemistry.
References:  109
Dorsal root ganglion and trigeminal ganglion.
Species:  Rat
Technique:  immunocytochemistry.
References:  141
Globus pallidus > frontal cortex > putamen.
Species:  Human
Technique:  Radioligand binding.
References:  142
Spinal cord: dorsal horn > ventral horn.
Species:  Human
Technique:  Radioligand binding.
References:  30
Lumbar dorsal root ganglia, superior cervical ganglia, lumbar sympathetic ganglia.
Species:  Rat
Technique:  RT-PCR.
References:  33
Poorly expressed in coronary arteries, atrium, ventricle and epicardium.
Species:  Human
Technique:  RT-PCR.
References:  29
Trigeminal ganglion.
Species:  Human
Technique:  immunocytochemistry.
References:  108
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:  86
Physiological Functions
Growth hormone release.
Species:  Human
Tissue:  In vivo.
References:  143-144
Inhibition of 5-HT release.
Species:  Rat
Tissue:  in vivo and mesencephalic raphe slices.
References:  145
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:  140

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-HT1D. Last modified on 2010-06-28. Accessed on 2010-09-03. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=3.


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