5-HT<sub>1A</sub> receptor | 5-Hydroxytryptamine receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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5-HT1A receptor

target has curated data in GtoImmuPdb

Target id: 1

Nomenclature: 5-HT1A 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.  » Email us

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 422 5q11.2-q13 HTR1A 5-hydroxytryptamine receptor 1A 24,96
Mouse 7 421 13 D2.1 Htr1a 5-hydroxytryptamine (serotonin) receptor 1A 15
Rat 7 422 2q16 Htr1a 5-hydroxytryptamine receptor 1A 3,26
Previous and Unofficial Names
ADRBRL1 | 5-HT1A | ADRB2RL1 | serotonin receptor 1A | Gpcr18 | 5-hydroxytryptamine (serotonin) receptor 1A, G protein-coupled
Database Links
Specialist databases
GPCRDB 5ht1a_human (Hs), 5ht1a_mouse (Mm), 5ht1a_rat (Rn)
Other databases
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
5-hydroxytryptamine

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]NLX-112 Hs Full agonist 8.9 pKd 34
pKd 8.9 (Kd 1.4x10-9 M) [34]
[3H]8-OH-DPAT Hs Full agonist 6.0 – 9.4 pKd 9,40,69,72
pKd 6.0 – 9.4 (Kd 1x10-6 – 3.98x10-10 M) [9,40,69,72]
[3H]S-15535 Hs Partial agonist 5.8 – 5.9 pKd 72
pKd 5.8 – 5.9 [72]
S-14671 Hs Full agonist 10.2 – 10.5 pKi 70,72
pKi 10.2 – 10.5 [70,72]
LY293284 Hs Full agonist 10.1 pKi 9
pKi 10.1 [9]
5-CT Hs Full agonist 9.4 – 10.3 pKi 68,70,72-73
pKi 9.4 – 10.3 [68,70,72-73]
lisuride Hs Full agonist 9.7 – 9.8 pKi 60,68,72
pKi 9.7 – 9.8 [60,68,72]
U92016A Hs Full agonist 9.7 pKi 57
pKi 9.7 [57]
vilazodone Hs Partial agonist 9.7 pKi 19
pKi 9.7 (Ki 2x10-10 M) [19]
Description: Binding of vilazodone to human 5-HT1A receptors against [3H]8-OH-DPAT (DPAT)
S-14506 Hs Full agonist 9.6 – 9.7 pKi 70,72
pKi 9.6 – 9.7 [70,72]
roxindole Hs Partial agonist 9.4 – 9.9 pKi 60,60
pKi 9.4 – 9.9 [60,60]
5-hydroxytryptamine Hs Full agonist 9.1 – 9.7 pKi 40,68-70,72-73
pKi 9.1 – 9.7 [40,68-70,72-73]
flesinoxan Hs Full agonist 9.3 pKi 70
pKi 9.3 [70]
L-694,247 Hs Full agonist 9.3 pKi 68
pKi 9.3 [68]
S-15535 Hs Partial agonist 9.2 pKi 72
pKi 9.2 [72]
Lysergide Hs Full agonist 9.0 pKi 74
pKi 9.0 [74]
RU 24969 Hs Full agonist 9.0 pKi 70
pKi 9.0 [70]
flibanserin Hs Agonist 9.0 pKi 10
pKi 9.0 (Ki 1x10-9 M) [10]
8-OH-DPAT Hs Full agonist 8.4 – 9.4 pKi 20,30,40,49,61,70,72-73
pKi 8.4 – 9.4 (Ki 3.98x10-9 – 3.98x10-10 M) [20,30,40,49,61,70,72-73]
LY 165,163 Hs Full agonist 8.9 pKi 70
pKi 8.9 [70]
spiroxatrine Hs Full agonist 8.8 pKi 70
pKi 8.8 [70]
ipsapirone Hs Partial agonist 8.6 – 8.8 pKi 70,72
pKi 8.6 – 8.8 [70,72]
FG-5893 Hs Full agonist 8.7 pKi 70
pKi 8.7 [70]
pergolide Hs Partial agonist 8.7 pKi 60
pKi 8.7 [60]
7-methoxy-1-naphthylpiperazine Hs Full agonist 8.6 pKi 39
pKi 8.6 [39]
(R)-UH 301 Hs Partial agonist 8.6 pKi 70
pKi 8.6 (Ki 2.74x10-9 M) [70]
NLX-101 Hs Full agonist 8.6 pKi 71
pKi 8.6 [71]
terguride Hs Partial agonist 8.5 pKi 60
pKi 8.5 [60]
ziprasidone Hs Partial agonist 7.9 – 8.9 pKi 70,91
pKi 7.9 – 8.9 [70,91]
S 16924 Hs Partial agonist 8.4 pKi 58
pKi 8.4 [58]
aripiprazole Hs Partial agonist 8.2 pKi 94
pKi 8.2 [94]
tandospirone Hs Full agonist 8.2 pKi 70
pKi 8.2 [70]
lurasidone Rn Partial agonist 8.2 pKi 35
pKi 8.2 (Ki 6.75x10-9 M) [35]
asenapine Hs Full agonist 8.0 – 8.3 pKi 70,91
pKi 8.0 – 8.3 [70,91]
zalospirone Hs Full agonist 8.1 pKi 70
pKi 8.1 [70]
1-naphthylpiperazine Hs Full agonist 8.0 pKi 39
pKi 8.0 [39]
ocaperidone Hs Full agonist 8.0 pKi 27
pKi 8.0 [27]
bromocriptine Hs Partial agonist 7.9 pKi 60
pKi 7.9 [60]
buspirone Hs Partial agonist 7.7 – 8.0 pKi 70,72-73
pKi 7.7 – 8.0 [70,72-73]
vortioxetine Hs Partial agonist 7.8 pKi 7
pKi 7.8 (Ki 1.5x10-8 M) [7]
LY334370 Hs Full agonist 7.8 pKi 98
pKi 7.8 [98]
BRL-15572 Hs Partial agonist 7.7 pKi 84
pKi 7.7 [84]
cabergoline Hs Full agonist 7.7 pKi 60
pKi 7.7 [60]
donitriptan Hs Full agonist 7.6 pKi 38
pKi 7.6 [38]
eletriptan Hs Full agonist 7.4 pKi 67
pKi 7.4 [67]
naratriptan Hs Full agonist 7.1 – 7.6 pKi 67-68
pKi 7.1 – 7.6 [67-68]
nafadotride Hs Full agonist 7.3 pKi 70
pKi 7.3 [70]
LP-44 Hs Agonist 7.3 pKi 51
pKi 7.3 (Ki 5.27x10-8 M) [51]
frovatriptan Hs Agonist 7.2 pKi 102
pKi 7.2 (Ki 6x10-8 M) [102]
LP-12 Hs Agonist 7.2 pKi 51
pKi 7.2 (Ki 6.09x10-8 M) [51]
BMY-14802 Hs Full agonist 7.2 pKi 70
pKi 7.2 [70]
xanomeline Hs Full agonist 7.2 pKi 100
pKi 7.2 [100]
avitriptan Rn Agonist 7.2 pKi 90
pKi 7.2 (Ki 7.08x10-8 M) [90]
GR 127935 Hs Partial agonist 7.1 – 7.2 pKi 39,84
pKi 7.1 – 7.2 [39,84]
apomorphine Hs Partial agonist 6.9 pKi 60
pKi 6.9 [60]
clozapine Hs Full agonist 6.8 – 6.9 pKi 58,70,91
pKi 6.8 – 6.9 [58,70,91]
EMDT Hs Full agonist 6.8 pKi 29
pKi 6.8 [29]
fluparoxan Hs Partial agonist 6.8 pKi 61
pKi 6.8 [61]
LP-211 Hs Agonist 6.7 pKi 52
pKi 6.7 (Ki 1.88x10-7 M) [52]
zolmitriptan Hs Full agonist 6.6 pKi 67
pKi 6.6 [67]
quetiapine Hs Full agonist 6.5 – 6.6 pKi 70,91
pKi 6.5 – 6.6 [70,91]
piribedil Hs Partial agonist 6.4 pKi 60
pKi 6.4 [60]
rizatriptan Hs Full agonist 6.4 pKi 67
pKi 6.4 [67]
LY344864 Hs Full agonist 6.3 pKi 80
pKi 6.3 [80]
SB 216641 Hs Partial agonist 6.3 pKi 84
pKi 6.3 [84]
CP 93129 Hs Full agonist 6.1 pKi 68
pKi 6.1 [68]
capeserod Hs Partial agonist 6.0 pKi 64
pKi 6.0 [64]
sumatriptan Hs Full agonist 6.0 pKi 67
pKi 6.0 [67]
quinpirole Hs Full agonist 5.8 pKi 69
pKi 5.8 [69]
olanzapine Hs Full agonist 5.6 – 5.8 pKi 70,91
pKi 5.6 – 5.8 [70,91]
vilazodone Hs Partial agonist 9.5 pIC50 32
pIC50 9.5 (IC50 3x10-10 M) [32]
BMY-7378 Hs Partial agonist 6.8 – 8.0 pIC50 43
pIC50 6.8 – 8.0 [43]
L-772,405 Hs Full agonist 7.2 pIC50 88
pIC50 7.2 [88]
SEP-363856 Hs Agonist 5.6 pIC50 21
pIC50 5.6 (IC50 2.3x10-6 M) [21]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]robalzotan Hs Antagonist 9.8 pKd 36
pKd 9.8 (Kd 1.58x10-10 M) [36]
[3H]WAY100635 Hs Antagonist 9.5 pKd 43
pKd 9.5 (Kd 3x10-10 M) [43]
[3H]p-MPPF Hs Antagonist 8.4 pKd 40
pKd 8.4 [40]
Rec 15/3079 Hs Antagonist 9.7 pKi 50
pKi 9.7 [50]
NAN 190 Hs Antagonist 9.4 pKi 70
pKi 9.4 [70]
repinotan Hs Antagonist 9.4 pKi 20
pKi 9.4 [20]
robalzotan Hs Antagonist 9.2 pKi 37
pKi 9.2 (Ki 6.31x10-10 M) [37]
SB 649915 Hs Antagonist 8.6 pKi 99
pKi 8.6 [99]
WAY-100635 Hs Antagonist 7.9 – 9.2 pKi 70,72
pKi 7.9 – 9.2 (Ki 1.26x10-8 – 6.31x10-10 M) [70,72]
p-MPPI Hs Antagonist 8.4 pKi 40
pKi 8.4 [40]
tiospirone Hs Antagonist 8.3 pKi 70
pKi 8.3 [70]
(-)-tertatolol Hs Antagonist 8.2 pKi 49,70
pKi 8.2 [49,70]
pindolol Hs Antagonist 8.1 pKi 72
pKi 8.1 [72]
SB 272183 Hs Antagonist 8.0 pKi 101
pKi 8.0 [101]
WAY-100135 Hs Antagonist 8.0 pKi 72
pKi 8.0 [72]
methiothepin Hs Antagonist 7.8 – 8.1 pKi 70,72
pKi 7.8 – 8.1 [70,72]
(S)-UH 301 Hs Antagonist 7.9 pKi 70
pKi 7.9 (Ki 1.35x10-8 M) [70]
spiperone Hs Antagonist 6.7 – 8.8 pKi 70,72-73
pKi 6.7 – 8.8 [70,72-73]
(-)-propranolol Hs Antagonist 7.5 pKi 68
pKi 7.5 [68]
(S)-flurocarazolol Hs Antagonist 7.5 pKi 87
pKi 7.5 [87]
pizotifen Hs Antagonist 7.4 pKi 68
pKi 7.4 [68]
GR 125,743 Hs Antagonist 7.3 pKi 68
pKi 7.3 [68]
yohimbine Hs Antagonist 7.3 pKi 61
pKi 7.3 [61]
fluspirilene Hs Antagonist 7.2 pKi 91
pKi 7.2 [91]
thioridazine Hs Antagonist 7.1 pKi 70
pKi 7.1 [70]
iloperidone Hs Antagonist 7.0 pKi 41
pKi 7.0 [41]
mesoridazine Hs Antagonist 7.0 pKi 17
pKi 7.0 (Ki 1.05x10-7 M) [17]
GR 218,231 Hs Antagonist 6.8 pKi 59
pKi 6.8 [59]
iloperidone Rn Antagonist 6.8 pKi 44
pKi 6.8 [44]
pimozide Hs Antagonist 6.8 pKi 70
pKi 6.8 [70]
(R)-flurocarazolol Hs Antagonist 6.5 pKi 87
pKi 6.5 [87]
SB 714786 Hs Antagonist 6.5 pKi 99
pKi 6.5 [99]
sertindole Hs Antagonist 6.4 – 6.6 pKi 70,91
pKi 6.4 – 6.6 [70,91]
zotepine Hs Antagonist 6.5 pKi 91
pKi 6.5 [91]
risperidone Hs Antagonist 6.4 – 6.5 pKi 70,91
pKi 6.4 – 6.5 [70,91]
(+)-butaclamol Hs Antagonist 6.4 pKi 70
pKi 6.4 [70]
cyamemazine Hs Antagonist 6.3 pKi 30
pKi 6.3 [30]
9-OH-risperidone Hs Antagonist 6.2 pKi 91
pKi 6.2 [91]
chlorpromazine Hs Antagonist 6.2 pKi 70
pKi 6.2 [70]
risperidone Rn Antagonist 6.2 pKi 44
pKi 6.2 [44]
MPDT Hs Antagonist 5.8 pKi 29
pKi 5.8 [29]
haloperidol Hs Antagonist 5.7 – 5.8 pKi 49,58,70,91
pKi 5.7 – 5.8 [49,58,70,91]
pipamperone Hs Antagonist 5.6 pKi 91
pKi 5.6 [91]
raclopride Hs Antagonist 5.2 pKi 70
pKi 5.2 [70]
ketanserin Hs Antagonist 5.0 pKi 73
pKi 5.0 [73]
SDZ-216525 Hs Antagonist 7.8 – 8.2 pIC50 43
pIC50 7.8 – 8.2 [43]
ritanserin