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. 


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
5-hydroxytryptamine (serotonin) receptor 1D
5-hydroxytryptamine receptor 1D
serotonin receptor 1D
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Reference Database
PharmGKB Gene
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
UniGene Hs.
Natural/Endogenous Ligands
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].
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

Show »

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]

There should be a chart of expression data here, you may need to enable JavaScript!
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

Show »

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


1. Bergen AW, van den Bree MB, Yeager M, Welch R, Ganjei JK, Haque K, Bacanu S, Berrettini WH, Grice DE, Goldman D, Bulik CM, Klump K, Fichter M, Halmi K, Kaplan A, Strober M, Treasure J, Woodside B, Kaye WH. (2003) Candidate genes for anorexia nervosa in the 1p33-36 linkage region: serotonin 1D and delta opioid receptor loci exhibit significant association to anorexia nervosa. Mol Psychiatry8: 397-406. [PMID:12740597]

2. Boulenguez P, Segu L, Chauveau J, Morel A, Lanoir J, Delaage M. (1992) Biochemical and pharmacological characterization of serotonin-O-carboxymethylglycyl[125I]iodotyrosinamide, a new radioiodinated probe for 5-HT1B and 5-HT1D binding sites. J. Neurochem.58 (3): 951-9. [PMID:1738002]

3. Davidson C, Ho M, Price GW, Jones BJ, Stamford JA. (1997) (+)-WAY 100135, a partial agonist, at native and recombinant 5-HT1B/1D receptors. Br J Pharmacol121: 737-742. [PMID:9208142]

4. Dizeyi N, Bjartell A, Nilsson E, Hansson J, Gadaleanu V, Cross N, Abrahamsson PA. (2004) Expression of serotonin receptors and role of serotonin in human prostate cancer tissue and cell lines. Prostate59: 328-336. [PMID:15042609]

5. Domenech T, Beleta J, Palacios JM. (1997) Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol356: 328-334. [PMID:9303569]

6. Ennis MD, Ghazal NB, Hoffman RL, Smith MW, Schlachter SK, Lawson CF, Im WB, Pregenzer JF, Svensson KA, Lewis RA et al.. (1998) Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects. J. Med. Chem.41 (13): 2180-3. [PMID:9632349]

7. Gaster LM, Blaney FE, Davies S, Duckworth DM, Ham P, Jenkins S, Jennings AJ, Joiner GF, King FD, Mulholland KR, Wyman PA, Hagan JJ, Hatcher J, Jones BJ, Middlemiss DN, Price GW, Riley G, Roberts C, Routledge C, Selkirk J, Slade PD. (1998) The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. J Med Chem41: 1218-1235. [PMID:9548813]

8. Glennon RA, Lee M, Rangisetty JB, Dukat M, Roth BL, Savage JE, McBride A, Rauser L, Hufeisen S, Lee DK. (2000) 2-Substituted tryptamines: agents with selectivity for 5-HT(6) serotonin receptors. J Med Chem43: 1011-1018. [PMID:10715164]

9. Hamblin MW, McGuffin RW, Metcalf MA, Dorsa DM, Merchant KM. (1992) Distinct 5-HT1B and 5-HT1D serotonin receptors in rat: structural and pharmacological comparison of the two cloned receptors. Mol. Cell. Neurosci.3: 578-587.

10. Hamblin MW, Metcalf MA. (1991) Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. Mol Pharmacol40: 143-148. [PMID:1652050]

11. Hou M, Kanje M, Longmore J, Tajti J, Uddman R, Edvinsson L. (2001) 5-HT(1B) and 5-HT(1D) receptors in the human trigeminal ganglion: co-localization with calcitonin gene-related peptide, substance P and nitric oxide synthase. Brain Res909: 112-120. [PMID:11478927]

12. John GW, Pauwels PJ, Perez M, Halazy S, Le Grand B, Verscheure Y, Valentin JP, Palmier C, Wurch T, Chopin P, Marien M, Kleven MS, Koek W, Assie MB, Carilla-Durand E, Tarayre JP, Colpaert FC. (1999) F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine. J Pharmacol Exp Ther290: 83-95. [PMID:10381763]

13. Jorand-Lebrun C, Pauwels PJ, Palmier C, Moret C, Chopin P, Perez M, Marien M, Halazy S. (1997) 5-HT1B receptor antagonist properties of novel arylpiperazide derivatives of 1-naphthylpiperazine. J Med Chem40: 3974-3978. [PMID:9397179]

14. Laporte AM, Doyen C, Nevo IT, Chauveau J, Hauw JJ, Hamon M. (1996) Autoradiographic mapping of serotonin 5-HT1A, 5-HT1D, 5-HT2A and 5-HT3 receptors in the aged human spinal cord. J Chem Neuroanat11: 67-75. [PMID:8841890]

15. Law H, Dukat M, Teitler M, Lee DK, Mazzocco L, Kamboj R, Rampersad V, Prisinzano T, Glennon RA. (1998) Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation. J Med Chem41: 2243-2251. [PMID:9632357]

16. Lesage AS, Wouters R, Van Gompel P, Heylen L, Vanhoenacker P, Haegeman G, Luyten WH, Leysen JE. (1998) Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Br J Pharmacol123: 1655-1665. [PMID:9605573]

17. Leysen JE, Gommeren W, Heylen L, Luyten WH, Van de Weyer I, Vanhoenacker P, Haegeman G, Schotte A, Van Gompel P, Wouters R, Lesage AS. (1996) Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan. Mol Pharmacol50: 1567-1580. [PMID:8967979]

18. Lin SL, Setya S, Johnson-Farley NN, Cowen DS. (2002) Differential coupling of 5-HT(1) receptors to G proteins of the G(i) family. Br J Pharmacol136: 1072-1078. [PMID:12145108]

19. Ma QP. (2001) Co-localization of 5-HT(1B/1D/1F) receptors and glutamate in trigeminal ganglia in rats. Neuroreport12: 1589-1591. [PMID:11409721]

20. Millan MJ, Gobert A, Newman-Tancredi A, Lejeune F, Cussac D, Rivet JM, Audinot V, Dubuffet T, Lavielle G. (2000) S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626. J Pharmacol Exp Ther293: 1048-1062. [PMID:10869410]

21. Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A. (2002) Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J Pharmacol Exp Ther303: 791-804. [PMID:12388666]

22. Millan MJ, Newman-Tancredi A, Audinot V, Cussac D, Lejeune F, Nicolas JP, Cogé F, Galizzi JP, Boutin JA, Rivet JM, Dekeyne A, Gobert A. (2000) Agonist and antagonist actions of yohimbine as compared to fluparoxan at alpha(2)-adrenergic receptors (AR)s, serotonin (5-HT)(1A), 5-HT(1B), 5-HT(1D) and dopamine D(2) and D(3) receptors. Significance for the modulation of frontocortical monoaminergic transmission and depressive states. Synapse35: 79-95. [PMID:10611634]

23. Miller KJ, Teitler M. (1992) Quantitative autoradiography of 5-CT-sensitive (5-HT1D) and 5-CT-insensitive (5-HT1E) serotonin receptors in human brain. Neurosci Lett136: 223-226. [PMID:1641195]

24. Moser PC, Bergis OE, Jegham S, Lochead A, Duconseille E, Terranova JP, Caille D, Berque-Bestel I, Lezoualc'h F, Fischmeister R, Dumuis A, Bockaert J, George P, Soubrie P, Scatton B. (2002) SL65.0155, a novel 5-hydroxytryptamine(4) receptor partial agonist with potent cognition-enhancing properties. J Pharmacol Exp Ther302: 731-741. [PMID:12130738]

25. Mota A, Bento A, Penalva A, Pombo M, Dieguez C. (1995) Role of the serotonin receptor subtype 5-HT1D on basal and stimulated growth hormone secretion. J Clin Endocrinol Metab80: 1973-1977. [PMID:7775648]

26. Napier C, Stewart M, Melrose H, Hopkins B, McHarg A, Wallis R. (1999) Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol368: 259-268. [PMID:10193663]

27. Newman-Tancredi A, Cussac D, Audinot V, Millan MJ. (1999) Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors. Naunyn Schmiedebergs Arch Pharmacol359: 447-453. [PMID:10431754]

28. Nilsson T, Longmore J, Shaw D, Pantev E, Bard JA, Branchek T, Edvinsson L. (1999) Characterisation of 5-HT receptors in human coronary arteries by molecular and pharmacological techniques. Eur J Pharmacol372: 49-56. [PMID:10374714]

29. Phebus LA, Johnson KW, Zgombick JM, Gilbert PJ, Van Belle K, Mancuso V, Nelson DL, Calligaro DO, Kiefer AD, Branchek TA, Flaugh ME. (1997) Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci61: 2117-212. [PMID:9395253]

30. Pierce PA, Xie GX, Levine JD, Peroutka SJ. (1996) 5-Hydroxytryptamine receptor subtype messenger RNAs in rat peripheral sensory and sympathetic ganglia: a polymerase chain reaction study. Neuroscience70: 553-559. [PMID:8848158]

31. Pineyro G, de Montigny C, Blier P. (1995) 5-HT1D receptors regulate 5-HT release in the rat raphe nuclei. In vivo voltammetry and in vitro superfusion studies. Neuropsychopharmacology13: 249-260. [PMID:8602897]

32. Potrebic S, Ahn AH, Skinner K, Fields HL, Basbaum AI. (2003) Peptidergic nociceptors of both trigeminal and dorsal root ganglia express serotonin 1D receptors: implications for the selective antimigraine action of triptans. J Neurosci23: 10988-10997. [PMID:14645495]

33. Price GW, Burton MJ, Collin LJ, Duckworth M, Gaster L, Gothert M, Jones BJ, Roberts C, Watson JM, Middlemiss DN. (1997) SB-216641 and BRL-15572 compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch. Pharmacol.356: 312-320. [PMID:9303567]

34. Reavill C, Taylor SG, Wood MD, Ashmeade T, Austin NE, Avenell KY, Boyfield I, Branch CL, Cilia J, Coldwell MC, Hadley MS, Hunter AJ, Jeffrey P, Jewitt F, Johnson CN, Jones DN, Medhurst AD, Middlemiss DN, Nash DJ, Riley GJ, Routledge C, Stemp G, Thewlis KM, Trail B, Vong AK, Hagan JJ. (2000) Pharmacological actions of a novel, high-affinity, and selective human dopamine D(3) receptor antagonist, SB-277011-A. J Pharmacol Exp Ther294: 1154-1165. [PMID:10945872]

35. Reynolds GP, Mason SL, Meldrum A, De Keczer S, Parnes H, Eglen RM, Wong EH. (1995) 5-Hydroxytryptamine (5-HT)4 receptors in post mortem human brain tissue: distribution, pharmacology and effects of neurodegenerative diseases. Br J Pharmacol114: 993-998. [PMID:7780656]

36. Rousselle JC, Plantefol M, Fillion MP, Massot O, Pauwels PJ, Fillion G. (1998) Specific interaction of 5-HT-moduline with human 5-HT1b as well as 5-HT1d receptors expressed in transfected cultured cells. Naunyn Schmiedebergs Arch Pharmacol358: 279-286. [PMID:9774213]

37. Russell MG, Matassa VG, Pengilley RR, van Niel MB, Sohal B, Watt AP, Hitzel L, Beer MS, Stanton JA, Broughton HB, Castro JL. (1999) 3-[3-(Piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists. J Med Chem42: 4981-5001. [PMID:10585208]

38. Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE. (1996) Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl)124: 57-73. [PMID:8935801]

39. Selkirk JV, Scott C, Ho M, Burton MJ, Watson J, Gaster LM, Collin L, Jones BJ, Middlemiss DN, Price GW. (1998) SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity. Br J Pharmacol125: 202-208. [PMID:9776361]

40. Shapiro DA, Renock S, Arrington E, Chiodo LA, Liu LX, Sibley DR, Roth BL, Mailman R. (2003) Aripiprazole, a novel atypical antipsychotic drug with a unique and robust pharmacology. Neuropsychopharmacology28: 1400-1411. [PMID:12784105]

41. Ward SE, Harrington FP, Gordon LJ, Hopley SC, Scott CM, Watson JM. (2005) Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist. J Med Chem48: 3478-3480. [PMID:15887956]

42. Watson J, Brough S, Coldwell MC, Gager T, Ho M, Hunter AJ, Jerman J, Middlemiss DN, Riley GJ, Brown AM. (1998) Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors. Br J Pharmacol125: 1413-1420. [PMID:9884068]

43. Watson J, Roberts C, Scott C, Kendall I, Collin L, Day NC, Harries MH, Soffin E, Davies CH, Randall AD, Heightman T, Gaster L, Wyman P, Parker C, Price GW, Middlemiss DN. (2001) SB-272183, a selective 5-HT(1A), 5-HT(1B) and 5-HT(1D) receptor antagonist in native tissue. Br J Pharmacol133: 797-806. [PMID:11454652]

44. Watson JM, Burton MJ, Price GW, Jones BJ, Middlemiss DN. (1996) GR127935 acts as a partial agonist at recombinant human 5-HT1D alpha and 5-HT1D beta receptors. Eur J Pharmacol314: 365-372. [PMID:8957260]

45. Weinshank RL, Zgombick JM, Macchi MJ, Branchek TA, Hartig PR. (1992) Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1Dα and 5-HT1Dβ. Proc. Natl. Acad. Sci. U.S.A.89: 3630-3634. [PMID:1565658]

46. Weydert A, Cloez-Tayarani I, Fillion MP, Simon-Chazottes D, Guenet JL, Fillion G. (1992) Molecular cloning of two partial serotonin 5-HT1D receptor sequences in mouse and one in guinea pig. C R Acad Sci III314: 429-435. [PMID:1521164]

47. Whale R, Bhagwagar Z, Cowen PJ. (1999) Zolmitriptan-induced growth hormone release in humans: mediation by 5-HT1D receptors?. Psychopharmacology (Berl)145: 223-226. [PMID:10463324]

48. Wurch T, Colpaert FC, Pauwels PJ. (1998) Chimeric receptor analysis of the ketanserin binding site in the human 5-Hydroxytryptamine1D receptor: importance of the second extracellular loop and fifth transmembrane domain in antagonist binding. Mol. Pharmacol.54 (6): 1088-96. [PMID:9855638]

49. Xie Z, Lee SP, O'Dowd BF, George SR. (1999) Serotonin 5-HT1B and 5-HT1D receptors form homodimers when expressed alone and heterodimers when co-expressed. FEBS Lett.456 (1): 63-7. [PMID:10452531]

50. Xu YC, Schaus JM, Walker C, Krushinski J, Adham N, Zgombick JM, Liang SX, Kohlman DT, Audia JE. (1999) N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist. J. Med. Chem.42 (3): 526-31. [PMID:9986723]

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 21/10/2014. IUPHAR database (IUPHAR-DB),

Contact us | Print | Back to top | Help
Copyright © 2014 IUPHAR