MAIN GsPCRs Click here for their STP.
Common biological outputs :
GPCR name
expressed on ...
physiological ligand(s)
agonists
antagonists
b1 cardiomyocytes (high in SA node, atria, AV node, His-Purkinje system, and ventricles => positive batmo-, dromo- and inotropic effects), 
juxtaglomerular cells, renal arterioles, adipocytes, neurohypophysis
adrenaline = noadrenaline isoproterenol / isopropylarterenol / isopropylnorepinephrine / isoprenaline / isopropylnoradrenaline / d,l-b-[3,4-dihydroxyphenyl]- a-isoprylaminoethanol hydrochloride (Isuprel®
dobutamine hydrochloride (Dobutrex®
SNRI : 
  • venlafaxine (Effexor®)
selective : 
  • acebutolol hydrochloride (Sectral®) (ISA)
  • atenolol (Antipressan®, Atehexal®, Atenol®, Blokium®, Bresben®, Ibinolo®, Neatenol®, Normiten®, Tenif®, Tenoretic®, Tenormin®)
  • betaxolol (Betoptic®, Betoptic-S®)
  • bisoprolol (Zebeta®)
  • celiprolol (Selector®)
  • esmolol hydrochloride (Brevibloc®)
  • metoprolol tartrate (Lopressor®
  • nevebilol
non-subtype-selective b-adrenergic antagonists: 
  • propanolol hydrochloride (Inderal®)
  • nadolol (Corgard®, Nadolol®)
  • pindolol (Visken®) (ISA)
  • labetalol hydrochloride (dilevalol stereoisomer : partial agonist) (Normodyne®, Trandate®, ...)
  • alprenolol (Alprenolol®)
  • metoprolol (Betaloc®, Lopresor®, Lopressor®, Toprol XL®)
  • carvedilol (Coreg®)
  • timolol maleate (Timoptic®, Timoptic XE®, Betimol®, Blocadren®)
  • sotalol (Betapace®, Rytmobeta®)
  • bopindol (Sandonorm®, ...)
  • carteolol (Cartrol®, Ocupress®, ...)
  • oxprenolol (Apsolox®, Slow-Trasicor®, Trasicor®)
  • penbutolol (Levatol®)
  • medroxalol
  • bucindolol (Intracardial®)
  • practolol (Eraldin®)
  • propafenone (Rythmol®)
  • levobunolol (Akbeta®, Betagan®, Betagan Liquifilm®, ...)
  • metipranolol (Optipranolol®)
  • CGP 20712A
b2 (after phosphorylation by BARK, it couples to Gi) cardiomyocytes (low in SA node, atria, AV node, His-Purkinje system, and ventricles), 
skeletal muscles, 
smooth muscle (vascular, tracheal and bronchial, stomach, intestine, and gallbladder, detrusor muscle of urinary bladder, uterus), 
hepatocytes, adipocytes, bronchial glands, ciliary muscle of eye; arterioles (except skin, mucosa and brain) and veins, spleen capsule, b cells of Langerhans' islets in endocrine pancreas, T cells, B cells, monocytes, macrophages
adrenaline >> noadrenaline isoproterenol / isopropylarterenol / isopropylnorepinephrine / isoprenaline / isopropylnoradrenaline / d,l-b-[3,4-dihydroxyphenyl] -a-isoprylaminoethanol hydrochloride  (Isuprel®
dobutamine hydrochloride (Dobutrex®
clenbuterol (Broncodil®, Broncoterol®, Cesbron®, Clenbuterol Pharmachim®, Contrasmina®, Contraspasmina®, Monores®, Novegam®, Planipart®, Prontovent®, Spiropent®, Spasmo-Mucosolvan®, Ventolase®, Ventipulmin®
selective agonists : 
  • short-acting b2 agonists (SABA) 
    • celiprolol (Selector®)
    • metaproterenol / orciprenaline sulfate (Alupent®)
    • terbutaline sulfate (Brethaire®, Brethine®, Bricanyl®, ...)
    • albuterol / salbutamol (Ventolin®, Proventil®, ...; Zarent® in combination with sodium nedocromyl; Combivent® in combination with ipratropium)
    • levalbuterol (Xopenex®)
    • isoetharine
    • pirbuterol acetate (Maxair®)
    • ritodrine
    • fenoterol (Airum®, Berotec®, Dosberotec® and Partusisten®; Duovent®, Berodual® in combination with ipratropium)
    • procaterol (Mascacin®, ...)
  • long-acting b2 agonists (LABA)
    • bitolterol mesylate (Tornalate®) => colterol
    • formoterol fumarate (Atock®, Foradil®, Oxeze®, Oxis®; Symbicort® in combination with budesonide)
    • salmeterol xinafoate (Serevent®; Advair/Seretide® in combination with fluticasone)
ICI 118551 
salmeterol 
albuterol 
butoxamine 
dopexamine (Dopacard®
non-subtype-selective b-adrenergic antagonists: 
  • propanolol hydrochloride (Inderal®)
  • nadolol (Corgard®)
  • pindolol (Visken®, Durapindol®, Pectobloc®, Pinbetol®) (ISA)
  • labetalol hydrochloride (Normodyne®,. Trandate®, ...)
  • carvedilol (Coreg®)
  • timolol maleate (Timoptic®, Timoptic XE®, Betimol®, Blocadren®)
  • sotalol (Betapace®)
  • bopindol (Sandonorm®, ...)
  • carteolol (Cartrol®, Ocupress®, ...)
  • oxprenol
  • penbutolol (Levatol®)
  • medroxalol
  • bucindol
  • propafenone (Rythmol®)
  • levobunolol (Akbeta®, Betagan®, Betagan Liquifilm®, ...)
  • metipranolol (Optipranolol®)
b3 adipocytes adrenaline < noadrenaline isoproterenol / isopropylarterenol / isopropylnorepinephrine / isoprenaline / isopropylnoradrenaline / d,l-b-[3,4-dihydroxyphenyl] -a-isoprylaminoethanol hydrochloride  (Isuprel®
dobutamine hydrochloride (Dobutrex®
BRL 37344
ICI 118551 
BRL 37344 
CGP 20712A 
non-subtype-selective b-adrenergic antagonists: 
  • propanolol hydrochloride (Inderal®)
  • nadolol (Corgard®)
  • pindolol (Visken®) (ISA)
  • labetalol hydrochloride (Normodyne®,. Trandate®, ...)
  • carvedilol (Coreg®)
  • timolol maleate (Timoptic®, Timoptic XE®, Betimol®, Blocadren®)
  • sotalol (Betapace®)
  • bopindol (Sandonorm®, ...)
  • carteolol (Cartrol®, Ocupress®, ...)
  • oxprenol
  • penbutolol (Levatol®)
  • medroxalol
  • bucindol
  • propafenone (Rythmol®)
  • levobunolol (Akbeta®, Betagan®, Betagan Liquifilm®, ...)
  • metipranolol (Optipranolol®)
glucagon receptor hepatocytes glucagon

GLP-1 receptor (GLP1R) brain, pancreatic b-cell GLP-1 exendin-4 / exenatide (Byetta®), a natural peptide with >50% sequence homology to GLP-1, but with greater potency and longer duration of action, produced in the saliva of the Gila monster (Heloderma suspectum) exendin-(9-39)
GLP-2 receptor (GLP2R) gastrointestinal tract GLP-2

D1 postsynaptic in striatum, neocortex dopamine apomorphine 
fenoldopam (Corlopam®
SKF38393 
pergolide (Celance®, Pharken®, Permax®
SCH-23390 
SCH-39166 / ecopipam 
SKF-83566 
butyrrophenons 
phenothiazines 
thioxanthenes 
diphenylbutylpiperidine 
bromocriptine (Ergoset®, Lactismine®, Parlodel®, Parlodel-LAR®, Parlodel-MR®, Pravidel®, Pravidel-Depot®, Serocryptin®
cabergoline (Cabasex®, Sogilen/Dostinex®) (partial antagonist)
D5 (it can heterodimerize with g2-containing GABAA) hippocampus, hypothalamus dopamine apomorphine butyrrophenons 
phenothiazines 
thioxanthenes 
diphenylbutylpiperidine
V2 basolateral membrane of distal convoluted tubule and collecting ducts, type II pneumocytes, vascular endothelium, vascular smooth muscle, fetal lung tissue and lung cancer  AVP / ADH 1-deamino-8-D-Arg vasopressin (DDAVP) / desmopressin / d[dArg8]VP 
desmopressin acetate (Minirin®
deamino[Val4, D-Arg8]AVP
des Gly-NH29-d(CH2)5[D-Ile2, Ile4]AVP 
d(CH2)5[dIle2, Ile4, Ala-NH29]AVP
vaptans : 
  • satavaptan / SR 121463-B (Aquilda®)
  • SR 121463A
  • YM 087 / conivaptan (Vaprisol®) (also antagonist on V1a)
  • tolvaptan / OPC-41061 (Samsca®)
  • lixivaptan / VPA-985 (Lixar®)
  • mozavaptan / OPC-31260 (Physuline®) (also antagonist on V1a)
H2 vascular smooth muscle cells, ventricular and right atrial cardiomyocytes, basolateral membrane of parietal cells of stomach, Th2 lymphocytes, DCs histamine dimaprit 
4(5)-methylhistamine 
impromidine
amthamine
ranitidine (Ranidil®, Zantac®; in combination with bismuth subcitrate or subsalicylate as Tritec®, Pylorid®
cimetidine (Tagamet®
famotidine (Pepcid®)
nizatidine (Axid®, Antizid®, Calmaxid®, Cronizat®, Distaxid®, Gastrax®, Naxidine®, Nizax®, Nizaxid®, Panaxid®, Tazac®, Zanizal®
burimamide (partial agonist in humans, antagonist in rats; also on H3)
tiotidine 
iodoaminopotentidine
iodoazidopotentidine
olopatadine / AL-4943A / KW-4679 (Opatanol®, Patanase®, Patanol®) (low affinity; high affinity for H1)
CRHR1
CRF / CRH cortagine is a CRF1-specific peptidic agonist by synthesis of chimeric peptides derived from human/rat CRF, ovine CRF (oCRF), and sauvagine (Svg) antalarmin
3-(4-Chloro-2-morpholin-4-yl-thiazol-5-yl)-8- (1-ethylpropyl)-2,6-dimethyl-imidazo[1,2-b]pyridazine (MTIP)
CRHR2
CRF / CRH

LH / hCG receptor Leydig cells, internal techa, granulosa cells LH
hCG


FSH receptor Sertoli cells, granulosa cells FSHref

TSH receptor thyroid cell, 
fibroblast, preadipocytes and adipocytes 
TSH

calcitonin receptor
calcitonin

CGRP receptor (+ CGRPRCP)
CGRP
BIBN 4096 BS
MK-0974 / telcagepant
adrenomedullin receptor (ADMR)
adrenomedullin

GIP receptor pancreatic islet b-cells  GIP

PACAPR1 trigeminal, otic and superior cervical ganglia (prejunctional) and cerebral arteries (postjunctional) PACAP

VIPR1 / VPAC1 / PACAPR2 T cells PACAP = VIP >> helodermin-like peptide = secretin K(15), R(16,) L(27)]VIP(1-7)/GRF(8-27) 
[R(16)]ChSn

VIPR2 / VPAC2
VIP
PACAP
RO 25-1553
secretin receptor exocrine pancreas secretin

5-HT4 hippocampus , gastrointestinal tract 5-HT enantiomeric, substituted benzamides 
  • cisapride (Propulsid®
  • renzapride 
  • zacopride 
  • ecabapide
  • metoclopramide (Plasil®, Reglan®
  • prucalopride 
tegaserod (Zelmac®, Zelnorm®
BIMU8 
RS67506 
ML10302
tropisetron (Navoban®) (weak
ondansetron (Zofran®) (weak
GR113808 
SB204070
5-HT6 striatum 5-HT

5-HT7 hypothalamus, intestine 5-HT

EP2 monocyte-derived dendritic cells  PGE2 ONO-AE1-259-01 
gemeprost 
11-deoxy-PGE1

EP3 (also on nuclear envelope) (also GiPCR and GqPCR) neurons, endothelial cells  of CNS PGE2 ONO-AE-248; 
sulprostone; 
misoprostol (Cytotec®; Mifeprex® in combination with mifepristone
gemeprost
L-826266
EP4 monocyte-derived dendritic cells,  T cells  PGE2 gemeprost 
11-deoxy-PGE1
L-161982
IP platelets, smooth muscle cells PGI2 / PC
PGE1
misoprostol (Cytotec®; Mifeprex® in combination with mifepristone)
DP / DP1
PGD2 BW245C
DP2 / CRTH2 / GPR44
PGD2

Frizzled homolog 1



Frizzled homolog 2 fetal kidney and lung and in adult colon and ovary.


Frizzled homolog 3 hair follicle 


Frizzled homolog 4



Frizzled homolog 5
Wnt-5A

Frizzled homolog 6



Frizzled homolog 7 poorly differentiated human esophageal carcinomas


Frizzled homolog 8



Frizzled homolog 9 brain, testis, eye, skeletal muscle, and kidney


Frizzled homolog 10 primary colon cancer


GC / GBG



some odorantsref tongue


some sweet molecules tongue
aspartame

saccharine

some bitter molecules tongue


A2a basal ganglia, neutrophils, vasculature and platelets P1 for Ado CGS 21680
APEC 
HENECA 
ATL-146e
CSC
ZM241385
DMPX
SCH58261
CO66713 
xanthines : 
  • aminophylline
  • istradefylline (KW-6002)
methylxanthines :  imiquimod
A2b blood vessels, enterocytes netrin-1 
P1 for Ado

xanthines : 
  • aminophylline
methylxanthines 
P2Y11 (also GqPCR)
ATP

PTHR1 osteoblasts PTH
PTHrp


PTHR2 osteoblasts PTH

MC1R melanocytes a-MSH (agonist) 
AgRP (antagonist)
melanotan II 
PT-141

MC2R / ACTH receptor (ACTHR zonae fasciculata and reticularis of the adrenal cortex ACTH

MC3R tissues other than the adrenal cortex and melanocytes (including arcuate nucleus) g1-MSH (agonist) 
AgRP (inverse agonist)
SHU 9119 
MC4R arcuate nucleus AgRP (inverse agonist) SHU 9119 
HS014

MC5R



G protein-coupled receptor 3 (GPR3) / adenylate cyclase constitutive activator (ACCA) ovarian follicle


G protein-coupled bile acid receptor 1 (GPBAR1) / TGR5 placenta and spleen > lung and fetal liver ; resting CD14+ monocytes  bile acids at 25 µM :
  • lithocholic acid (LCA)
  • DCA
  • CDCA


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