MAIN GiPCRs Click here for their STP.
Common biological outputs :
GPCR name
physiological ligand(s)
expressed on ...
agonists
antagonists
a2A adrenaline < noadrenaline presynaptic on solitary tract nucleus and presynaptic neurons in ortosympathetic system, pancreatic islets b cells, platelets, vascular smooth muscle cells a2-selective adrenergic agonists 
  • apraclonidine (Iopidine
  • brimonidine tartrate (Alphagan
  • clonidine (Catapres, Catapres TTS, Dixarit
  • guanabenz (Wytensin
  • guanfacine hydrochloride (Tenex
  • tizanidine (Zanaflex
  • a-methylDOPA (Aldomet) => a-methyldopamine => a-methylnorepinephrine 
  • oxymetazoline
  • desmedetomidine (Precedex)
NRI : 
  • reboxetine (Edronax)
(-) tramadol
alkylating holoalkylamine 
  • phenoxybenzamine hydrochloride (Dibenzyline)
imidazolines 
  • phentolamine mesylate (Regitine)
  • tolazoline hydrochloride (Priscoline) (also an a1-antagonist)
piperazinyl quinazolines 
  • prazosin hydrochloride (Minipress, Alpress, Hypotens, Hypovase, Sinetens) (low)
indoles  haloperidol (decanoate) (Haldol, Serenace, Serenase
chlorpromazine (CPZ) hydrochloride (Largactil, Thorazine, Chlomazine, Dormazine, Fenactil, Hibernal, Ormazine, Promaz, Prozil, Solidon, Sonazine, Taroctyl
atipamezole 
mianserin (Athymil, Bolvidon, Norval, Tolvin
etoperidone 
a2B adrenaline < noadrenaline presynaptic on solitary tract nucleus and presynaptic neurons in ortosympathetic system, pancreatic islets b cells, platelets, vascular smooth muscle cells a2-selective adrenergic agonists 
  • apraclonidine (Iopidine
  • brimonidine tartrate (Alphagan
  • clonidine (Catapres, Catapres TTS, Dixarit
  • guanabenz (Wytensin
  • guanfacine hydrochloride (Tenex
  • tizanidine (Zanaflex
  • a-methylDOPA (Aldomet) => a-methyldopamine => a-methylnorepinephrine (false neurotransmitter)
NRI : 
  • reboxetine (Edronax)
(-) tramadol
alkylating holoalkylamine 
  • phenoxybenzamine hydrochloride (Dibenzyline)
imidazolines 
  • phentolamine mesylate (Regitine)
  • tolazoline (also an a1-antagonist)
piperazinyl quinazolines 
  • prazosin hydrochloride (Minipress, Alpress, Hypotens, Hypovase, Sinetens) (low)
indoles  haloperidol (decanoate) (Haldol, Serenace, Serenase
chlorpromazine (CPZ) hydrochloride (Largactil, Thorazine, Chlomazine, Dormazine, Fenactil, Hibernal, Ormazine, Promaz, Prozil, Solidon, Sonazine, Taroctyl)
a2C adrenaline < noadrenaline presynaptic on solitary tract nucleus and presynaptic neurons in ortosympathetic system, pancreatic islets b cells, platelets, vascular smooth muscle cells a2-selective adrenergic agonists 
  • apraclonidine (Iopidine
  • brimonidine tartrate (Alphagan
  • clonidine (Catapres, Catapres TTS, Dixarit
  • guanabenz (Wytensin
  • guanfacine hydrochloride (Tenex
  • tizanidine (Zanaflex
  • a-methylDOPA (Aldomet) => a-methyldopamine => a-methylnorepinephrine 
NRI : 
  • reboxetine (Edronax)
(-) tramadol
alkylating holoalkylamine 
  • phenoxybenzamine hydrochloride (Dibenzyline)
imidazolines 
  • phentolamine mesylate (Regitine)
  • tolazoline (also an a1-antagonist)
piperazinyl quinazolines 
  • prazosin hydrochloride (Minipress, Alpress, Hypotens, Hypovase, Sinetens) (low)
indoles  haloperidol (decanoate) (Haldol, Serenace, Serenase
chlorpromazine (CPZ) hydrochloride (Largactil, Thorazine, Chlomazine, Dormazine, Fenactil, Hibernal, Ormazine, Promaz, Prozil, Solidon, Sonazine, Taroctyl)
M2 ACh cardiomyocytes (SA node, atrium, AV node, ventricle), striatum synthetic choline derivatives 
  • methacholine chloride (Mecholyl, Provocholine)
  • carbachol (Miostat, Isopto Carbachol, Carboptic)
  • bethanechol chloride (Urecholine)
natural alkaloids 
  • pilocarpine hydrochloride (Akarpine, Isopto Carpine, Ocusert-Pilo, Pilagan, Pilopine-HS, Piloptic, Pilostat, Salagen, Pilocar)
  • muscarine 
  • arecoline
alkaloids  butylscopolamine (Buscopam
methylatropine 
quaternary ammonium 
  • glycopyrrolate (Robinul)
  • homatropine methylbromide
  • ipratropium bromide (Atrovent; Combivent in combination with albuterol / salbutamol; Duovent, Berodual in combination with fenoterol)
  • methscopolamine bromide (Pamine)
  • oxitropium bromide
  • propantheline bromide (Pro-Banthine)
  • tiotropium bromide (Spiriva)
tertiary amines 
  • homatropine hydrobromide (Isopto Homatropine)
  • cyclopentolate hydrochloride (AK-Pentolate, Cyclogyl, Pentolair)
  • tropicamide (Mydriacyl, Tropicacyl, Opticyl)
  • benztropine / benzatropine mesylate (Akitan, Cogentin, Cogentinol)
  • trihexyphenidyl hydrochloride (Artane)
  • dicyclomine hydrochloride (Bentyl, ...)
  • flavoxate hydrochloride (Urispas; Cistalgan in combination with propyphenazone)
  • oxybutynin chloride (Ditropan)
  • tolterodine (Detrol)
olanzapine (Zyprexa, Lanzac
osenapine
clozapine (Clozaril, Leponex
NRI : 
  • protriptyline (Vivactil)
SNRI : 
  • amitriptyline (Laroxil, Elavil)
  • imipramine (Tofranil)
  • paroxetine (Paxil, Seroxat)
AFDX384 
tripitramine 
methoctramine 
procyclidine (Arpicolin, Kemadren, Kemadrin, Kemadrine, Osnervan, Procyclid)
M4 ACh striatum synthetic choline derivatives 
  • methacholine chloride (Mecholyl, Provocholine)
  • carbachol (Miostat, Isopto Carbachol, Carboptic)
  • bethanechol chloride (Urecholine)
natural alkaloids 
  • pilocarpine hydrochloride (Akarpine, Isopto Carpine, Ocusert-Pilo, Pilagan, Pilopine-HS, Piloptic, Pilostat, Salagen, Pilocar)
  • muscarine 
  • arecoline
alkaloids  butylscopolamine (Buscopam
methylatropine 
quaternary ammonium 
  • glycopyrrolate (Robinul)
  • homatropine methylbromide
  • ipratropium bromide (Atrovent; Combivent in combination with albuterol / salbutamol; Duovent, Berodual in combination with fenoterol)
  • methscopolamine bromide (Pamine)
  • oxitropium bromide
  • propantheline bromide (Pro-Banthine)
  • tiotropium bromide (Spiriva)
tertiary amines 
  • homatropine hydrobromide (Isopto Homatropine)
  • cyclopentolate hydrochloride (AK-Pentolate, Cyclogyl, Pentolair)
  • tropicamide (Mydriacyl, Tropicacyl, Opticyl)
  • benztropine / benzatropine mesylate (Akitan, Cogentin, Cogentinol)
  • trihexyphenidyl hydrochloride (Artane)
  • dicyclomine hydrochloride (Bentyl, ...)
  • flavoxate hydrochloride (Urispas)
  • oxybutynin chloride (Ditropan)
  • tolterodine (Detrol)
olanzapine (Zyprexa, Lanzac
clozapine (Clozaril, Leponex
NRI : 
  • protriptyline (Vivactil)
SNRI 
  • amitriptyline (Laroxil, Elavil)
  • imipramine (Tofranil)
  • paroxetine (Paxil, Seroxat
muscarinic toxin 3 (MT3)
tropicamide 
procyclidine (Arpicolin, Kemadren, Kemadrin, Kemadrine, Osnervan, Procyclid)
MLT1A / MT1 melatonin hypothalamic suprachiasmatic nucleus and hypophysial pars tuberalis  ramelton (Rozerem) (also MLT2 agonist)
MLT1B melatonin retina and brain 

HM74 / PUMA-G
adipocytes vitamin B3 / nicotinic acid / niacin
galanin receptor 1 galanin brain, spinal cord, small intestine and heart.

galanin receptor 2 (also GqPCR) galanin brain, gastrointestinal system, and hypothalamopituitary axis

galanin receptor 3 galanin many tissues SNAP 37889 
SNAP 398299ref

Y1 NPY human colon mucosa [Pro34]NPY 
NPY13-16
GR231118 
SR 120107A
Y5 NPY
[Pro34]NPY 
NPY13-16
GR231118 
SR 120107A
AT1b (it can heterodimerize with B2) angiotensin II cardiovascular cells, adrenal glands, pituitary gland
-artans 
  • bithienylmethylacrylic acid derivative
    • eprosartan (Teveten)
  • biphenylmethyl derivatives
    • candesartan cilexetil (Atacand) (prodrug)
    • irbesartan (Avapro)
    • losartan (Cozaar ; Losazid in combination with hydrochlorothiazide)
    • telmisartan (Micardis)
    • valsartan (Diovan)
AT2 angiotensin II In adults, it is highly expressed in myometrium with lower levels in adrenal gland and fallopian tube. It is highly expressed in fetal kidney and intestine

H3 histamine presynaptic on histaminergic neurons that innervate the blood vessels and the heart (negative feedback), smooth muscles  (R)-a-methylhistamine 
N(a)-methylhistamine
immepip
imetit
iodophenpropit 
iodoproxyfan
burimamide 
thioperamide 
clobenpropit 
impentamine
methylthioperamide
N-ethoxycarbonyl-2-ethoxy- 1,2-dihydroquinoline (EEDQ)
burimamide (also on H2)
H4 histamine hippocampus, PBMC imetit 
immepip
thioperamide
A1 adenosine presynaptic neuron 
proconvulsivant neurons 
heart, neutrophils
R-PIA
N6-cyclopentyladenosine
xanthines :  methylxanthines :  BG9719 / CVT-124 (Adentri)
A3 adenosine cardiac ventricular cells IB-MECA
2-Cl-IB-MECA
MRS1067
MRS1097
MRS1220
L-249313
L-268605
methylxanthines : 
GABAB (heterodimer of GABBR1 and GABBR2 / GRR51 isoforms from paralogous genes) GABA hippocampus, temporal lobe baclofen (Lioresal
3-aminopropylphosphinic acid
phaclofen 
2-hydroxy-S-saclofen 
CGP35348 
CGP36742 / SGS742
CGP55845 
CPG64213
SST1 SST
cortistatin
thymic epithelial cells, jejunum, stomach, spinal cord, cortex and hippocampus CH275 
sst des-Ala1,2,5

SST2 =alternative splicing=> 
  • SST2a
  • SST2b
SST
cortistatin
  • pituitary, astrocytes, arcuate nucleus/median eminence 
  • hematopoietic cells, cortex, hippocampus, striatum, and kidney
octreotide acetate (Lar Depot, Sandostatin, Sandostatin-LAR
lanreotide (Somatuline LA)
pasireotide / SOM230 (Signifor)
vapreotide 
seglitide / MK-678
BIM23027
chlorpromazine (CPZ) hydrochloride (Largactil, Thorazine, Chlomazine, Dormazine, Fenactil, Hibernal, Ormazine, Promaz, Prozil, Solidon, Sonazine, Taroctyl
haloperidol (decanoate) (Haldol, Serenace, Serenase
cyanamid 154806
SST3 SST
cortistatin
cortex, olfactory bulb, cerebellum, hippocampus,  and pancreatic islets BIM23052 
NNC269100

SST4 SST
cortistatin
fetal and adult cortex and hippocampus and lung BIM23052
CH275 
NNC269100

SST5 (it can heterodimerize with D2) SST-28 (Ki = 0.19 nM) > SST-14 (Ki = 2.24 nM) 
cortistatin
gastroenteropancreatic endocrine tumors octreotide acetate (Lar Depot, Sandostatin, Sandostatin-LAR
L362855 
BIM23268
BIM23056
CD222 / IGF2 / MPR (90-95% are located intracellularly, only 5-10% on the cell membrane. The internalization rate seems to be enhanced by ligand induced dimerization as well as by phosphorylation of its cytoplasmic Ser IGF-2
M6P-containing proteins : 
  • lysosomal hydrolases
  • TGF-b latency associated peptide (LAP)
  • proliferin 
independently of M6P : 



glicentin receptor glicentin


mGluRII 2 Glu presynaptic in dentate gyrus L-CCG, APDC
mGluRII 3 Glu
N-acetyl-aspartyl-glutamate (NAAG)

L-CCG
 (2R,4R)-4-aminopyrrolidine-2, 4-dicarboxylate (APDC)
(S)-a-ethylglutamic acid (EGLU).
mGluRIII 4 Glu
L-AP4 / APB
mGluRIII 6 Glu
L-AP4 / APB
mGluRIII 7 Glu
L-AP4 / APB
mGluRIII 8 Glu
L-AP4 / APB
EP3_ (also on nuclear envelope) (also GqPCR and GsPCR) PGE2 neurons in the organum vasculosa lamina terminalis (OVLT) at the midline of the preoptic area (POA), endothelial cells  of CNS, basolateral membrane of parietal cells of stomach ONO-AE-248; 
sulprostone; 
misoprostol (Cytotec
gemeprost
L-826266
5-HT1A 5-HT (protean agonist as a function of sodium chloride concentration) raphe nuclei 
hippocampus
natural and semisynthetic ergot alkaloids
buspirone (BuSpar
gepirone (Ariza
roxindole 
ziprasidone (Geodon, Zeldox
ipsapirone 
flesinoxan
OPC-14523 (1-[3-[4-(3-chlorophenyl) -1-piperazinyl]propyl] -5-methoxy-3,4-dihydro -2[1H]-quinolinone monomethanesulfonate) 
8-hydroxy-(2-N,N-dipropylamino) -tertraline (8-OH-DPAT) 
fidanserin (Ectris
methysergide (Sansert
metergolin 
clozapine (Clozaril, Leponex
WAY 100135 
tandospirone (partial agonist) 
trazodone (Desyrel, Trittico, Molipaxin, Pragmarel, Thombran, Trazodil, Trazolan
5-HT1B / 1Db 5-HT (protean agonist as a function of sodium chloride concentration) subiculum 
substantia nigra (inhibitory autoreceptors that regulate serotonin release)
natural and semisynthetic ergot alkaloids
CP93129 
trazodone (Desyrel, Trittico, Molipaxin, Pragmarel, Thombran, Trazodil, Trazolan)  => m-chlorophenylpiperazine (mCPP) 
triptans : 
  • eletriptan bromide (Relpax)
  • almotriptan (Almogran, Axert)
  • zolmitriptan (Zomig)
  • naratriptan (Amerge)
  • oxitriptan (Cincofarm, Levotonine, Levothym, Oxyfan, Serotonyl TM, Serovit, Telesol, Trimag, Tript-OG, Tript-Oh, Triptene TM and Triptum TM)
  • rizatriptan (Maxalt, Maxalt-MLT)
methysergide (Sansert
metergolin 
clozapine (Clozaril, Leponex

inverse agonists reduce the inhibitory influence on serotonin release and alleviate the impaired serotonergic transmission associated with depressive states and could treat memory dysfunction

5-HT1D 5-HT cranial blood vessels (inhibitory autoreceptors that regulate serotonin release) natural and semisynthetic ergot alkaloids
LY694247 
triptans 
  • naratriptan (Amerge)
  • rizatriptan (Maxalt, Maxalt-MLT)
  • sumatriptan (Imitrex; Trexima in combination with naproxen)
  • zolmitriptan (Zomig)
methysergide (Sansert
metergolin 
clozapine (Clozaril, Leponex
GR127935 
ziprasidone (Geodon, Zeldox

inverse agonists reduce the inhibitory influence on serotonin release and alleviate the impaired serotonergic transmission associated with depressive states

5-HT1E 5-HT cortex striatum

5-HT1F / 1Eb 5-HT brain and periphery

5-HT5A 5-HT hippocampus
biphenylmethylamine derivative 11ref
5-HT5B 5-HT


m1 opiates / opioids receptor (MOR) b-endorphin > enkephalins >> dynorphins resynaptic on cholinergic and glutamatergic neurons in periaqueductal grey (PAG), pontine reticular formation, median raphe, nucleus raphe magnus, and adjacent gigantocellular reticular nucleus in the rostral ventromedial medulla (RVM) and spinal cord (medium and large diameter DRG neurons) => supraspinal analgesia, PRL release, decreased ACh release, catalepsy morphine
tetrapeptide A10 (H-Tyr-D-Orn-Phe-Gly-OH) 
DAGO (Tyr-D-Ala-Gly-N(Me) Phe-Gly-OH) 
DAMGO (D-Ala-2, me-Phe4, Gly(01) 5 enkephalin) 
DALDA 
sufentanil
(+) tramadol
levorphanol
naloxone
naltrexone
b-funaltrexamine (FAN) 
cypridine 
nalmefene (Revex
CTOP 
CTAP
m2 opiates / opioids receptor (MOR) b-endorphin > enkephalins >> dynorphins spinal analgesia, respiratory depression, increased GH release, decreased GI motility, anorexia, decreased DA release, cardiovascular effects diphenoxylate hydrochloride (Lomotil
difenoxin hydrochloride (Motofen
loperamide N-oxide => loperamide (Imodium, Imodium A-D)

m3 opiates / opioids receptor (MOR) morphineref vascular tissue, mononuclear cells, neutrophils, and neuroblastoma cells.

k1 opiates / opioids receptor (KOR) (it can homodimerize or heterodimerize with d opiods) dynorphins (expecially A1-32 >>> b-endorphin presynaptic on cholinergic and glutamatergic neurons in periaqueductal grey (PAG), pontine reticular formation, median raphe, nucleus raphe magnus and adjacent gigantocellular reticular nucleus, small and medium diameter DRG neurons, cord blood hematopoietic stem cells => analgesia, ADH release, sedation, anorexia U69593 
CI977 
U-50,488 
U50488.gif
ICI174864 
ICI 199441 
ICI199441.gif
TRK-820 
bremazocine and ketocyclazocine >> morphine
Bremazocine.gif
naloxone
naltrexone
N-phenylpropyl-4b-methyl-5-(3-hydroxyphenyl)- 7a-[3-(1-piperidinyl)propanamido]morphan [(-)-3b] 
DIPPA 
UPHIT 
fedotozine 
nor-binaltorphimine 
Norbinaltorphimine.gif
GNTI 
GNTI.gif
k2 opiates / opioids receptor (KOR) dynorphin A >> b-endorphin presynaptic on cholinergic and glutamatergic neurons => analgesia, ADH release, sedation, decreased gastrointestinal motility => anorexia as for k1 as for k1
k3 opiates / opioids receptor (KOR) dynorphin A >> b-endorphin


d1 opiates / opioids receptor (DOR) (it can heterodimerize with k opiods) Met5-enkephalin > b-endorphin presynaptic  on cholinergic and glutamatergic neurons in dorsal horn of spinal cord (large diameter DRG neurons), vas deferens => supraspinal analgesia, hyperphagia, increased GH release, decreased DA release morphine
D-Pen2,5-enkephalin 
levorphanol
Tyr-D-Ser-Gly-Phe-Leu-Thr (DSLET) 
[dPen2; dPen5]enkephalin (DPDPE) 
Tyr-d-Ser-O-tbutyl- Gly-Phe-Leu-Thr (DSBULLET) 
SNC-80
naloxone
naltrexone
TIPP4 
DALCE 
ICI174864 
naltrindole 
Naltrindole.gif
d2
supraspinal and spinal analgesia, hyperphagia, increased GH release, decreased DA release

s1 opiates / opioids receptor (SOR) is a 223 amino acid protein sharing no homology with other mammalian protein. It is an intracellular protein present on the endoplasmic reticulum membrane, which can translocates to other organelles and plasma membranes after activation. neurosteroids :
  • pregnenolone
  • dehydroepiandrosterone
[progesterone is a potent antagonist]
presynaptic on cholinergic and glutamatergic neurons => dysphoria, contraction of rat vas deferens cyclazocine or N-allylnormetazocine > morphine
SKF 10047 
benzomorphans igmesine 
neuroleptics, antidepressants, cocaine, peptides related to neuropeptide Y or CGRP
opipramol (Insidon, Oprimol
remoxipride (Roxiam
s2 opiates / opioids receptor (SOR)
presynaptic  on cholinergic and glutamatergic neurons => dysphoria, contraction of rat vas deferens

e opiates / opioids receptor (EOR)

psychotomimetics
opiate receptor-like 1 (ORL-1) nociceptin / orphanin FQ periaqueductal grey (PAG), median raphe, roostral ventromedial medulla (RVM)

CB1 / CNR1 anandamide
homo-g-linolenylethanolamide (HEA)
docosatetraenylethanolamide (DEA)
cerebellum, amygdala, anterior pituitary gland, hippocampus,  oligodendrocytes, astrocytes, striatum, cerebral cortex, primary nociceptive neurons, thyroid, keratinocytes, macrophages, stomach, colon, adrenal gland, heart, lung, prostate, uterus, ovary, testis, bone marrow, thymus, tonsils, anterior eye and retina CP 55,940 (partial agonist
WIN55,212-2 
HU-210 
THC
arachidonyl-2'-chloroethylamide/(all Z)-N-(2-cycloethyl)-5,8,11,14-eicosatetraenamide (ACEA) 
SR141716A (Rimonabant) (inverse agonist)
CB2 / CNR2 / CX5 2-arachidonoylglycerol amide (2-AG)
palmitylethanolamide (PEA)
B lymphocytes > NK lymphocytes >> monocytes > neutrophils > CD8+ T lymphocytes > CD4+ T lymphocytes ; keratinocytesref CP 55,940 (partial agonist
WIN55,212-2 
HU-210 
THC
HU-210
AM1241 
cannabinor (source : Pharmos Corp)
SR144528
AM630
NPRC / ANP-C
smooth muscle cell

calcium sensor receptor (CASR) (it can homodimerize) (also GqPCR) see here see here see here see here
EDG1 / S1P1 (Akt-dependent phosphorylation of the third intracellular loop at the Thr236 residue is critical for committing the receptor to regulate Rac and the signaling pathways required for cortical actin assembly, lamellopodia formation, and chemotaxis) sphingosine-1-phosphate (Kd = 8 nM) T lymphocytes, vascular endothelial cells, vascular smooth muscle cells

EDG4 / LPA2 (also GqPCR) LPA


G2A lysophosphatidylcholine (LPC)


GPR68 / OGR-1 / SPC1 sphingosylphosphoryl choline (SPC) ovarian cancer cells

GPR65 / TDAG8 psychosine / galactosylsphingosine


G0-VN1



G0-VN2



VR



Gi-VN



D2 (long and short isoforms : it can heterodimerize with SST5) dopamine presynaptic and postsynaptic in chemo-receptor trigger zone (CTZ; area postrema); 
nucleus tractus solitarius ; striatum; nucleus accumbens ; pituitary gland ; heart ; testes ; esophagus ; stomach
amantadine (Antadine, Contenton, Mantadine, Mantadan, Mantadix, Mantaviral, PK-Merz, Protexin, Symadine, Symmetrel, Virofral
apomorphine (APO-go, Uprima
bromocriptine (Ergoset, Lactismine, Parlodel, Parlodel-LAR, Parlodel-MR, Pravidel, Pravidel-Depot, Serocryptin
cabergoline (Cabasex, Sogilen/Dostinex
lisuride
pergotryl 
pergolide (Celance, Pharken, Permax
pramipexole dihydrochloride (Firol, Mirapex, Mirapexin, Mirapexol, Sifrol
quinagolide 
ropirinole hydrochloride (Requip
roxindole 
talipexole 
tiospirone 
ziprasidone (Geodon, Zeldox
hydrophilic (anyway they reach the CTZ) : 
  • butyrophenones
    • domperidone (Motilium, Peridon
  • enantiomeric, substituted benzamides
    • metoclopramide (Maxeran, Plasil, Reglan)
    • alizapride (Limican, Nausilen)
    • cisapride (Propulsid
    • itopride (Ganaton)
lipophilic : 
  • classical antipsychotics
    • butyrophenones (phenylbutylpiperidine)
      • azaperone (Stresnil)
      • benperidol (Anquil)
      • droperidol (Inapsine)
      • fluspirilene (effective for 1 week)
      • haloperidol (decanoate) (Haldol, Serenace, Serenase)
      • melperone (Buronil, Eunerpan)
      • paliperidone (Invega) extended release tablets
      • penfluridol (effective for 1 week when administered per os)
      • pimozide (Orap, Antalon, Opiran, Pirium, Oralep) (effective for 24h when administered per os)
      • pipamperone (Dipiperon, Piperonyl)
      • risperidone (Risperdal, Risperidal, Belivon, Risperin, Rispolept, Rispolin)
      • spiperone
      • trifluperidol
    • phenothiazines
      • piperazine ring in the side chain (effective for 2 weeks)
        • acetophenazine (Tindal, Mepronizine, Noctran)
        • fluphenazine enanthate or decanoate (Prolixin, Modecate, Permitil)
        • perphenazine (Trilafon, Avomit, Decetan, Fentazin, Mutabon)
        • prochlorperazine / AZ-001  (Compazine
        • trifluoperazine (Stelazine, Vesprin, Terfluzine, Stalabid)
      • piperidine ring in the side chain
        • mesoridazine besylate (Serentil, Lidanil)
        • mepazine / pecazine (Lacumin, Mepasin, Pacatal, Pactal, Paxital, Ravenil, Seral)
        • pipotiazine / pipothiazine palmitate (effective for 4 weeks) undecinelate (effective for 2 weeks) (Piportil)
        • thioridazine hydrochloride (Mellerettes, Melleril, Mellaril)
      • aliphatic side chain
        • chlorpromazine (CPZ) hydrochloride (Largactil, Thorazine, Chlomazine, Dormazine, Fenactil, Hibernal, Ormazine, Promaz, Prozil, Solidon, Sonazine, Taroctyl)
        • levomepromazine (Minozinan, Nozinan, Levoprome, Neurocil, Veractil, Sinogan
        • methopromazine (Quietal)
        • prochlorpromazine (Compazine)
        • promazine (Sparine
        • promethazine (Avomine, Fenerodine, Phenergan, Fargan)
        • trifluopromazine (Vesprin, Psyquil, Psiquil, Siquil, Vesprin)
      • methotrimeprazine

      • / levomepromazine (Levoprome, Nozinan, Neurocil, Veractil, Sinogan)
    • thioxanthenes
      • clopenthixol (Clopixol)
      • flupenthixol decanoate (effective for 1-2 weeks) (Fluanxol, Depixol)
      • chlorprotixene / chlorprothixene (Taractan, Chlorprothixen, Cloxan, Minithixen, Truxal, Truxaletten)
      • thiothixene (Navane
      • zuclopenthixol (Clopixol)
  • "atypical"
    • benzisoxazole
      • iloperidone (Zomaril)
    • dibenzoazepine
      • carpipramine (Prazinil, Defekton
      • clozapine (low affinity, mainly a 5-HT2A antagonist; Clozaril, Leponex)
      • loxapine (Loxitane, Loxapac, Desconex)
    • dihydroindolone
      • molindone (Moban, Lindone)
    • enantiomeric, substituted benzamides
      • amisulpride (Solian)
      • remoxipride (Roxiam
      • sulpiride (Dobren, Sulparex, Dogmatil, Dolmatil, Valirem)  : 12 g / die (anti-dysthymias psychostimulant if given at 100-200 mg/die)
      • L-sulpiride (Levopraid)
      • D,L-sulpiride (Equilid)
      • clebopride (Motilex)
    • imidazolidinone
      • sertindole (Serlect, Serdolect)
D3 dopamine presynaptic and postsynaptic in limbic areas (midbrain => nucleus accumbens tract), olfactory tubercle, hypothalamus, lymphocytes apomorphine
7-OH-DPAT 
ropirinole
roxindole
pramipexole
sulpiride (Dobren, Sulparex, Dogmatil, Dolmatil, Valirem
amisulpride (Solian
R(+)-7-hydroxy-N,N-dipropylaminotetralin 
PD-128,907 
hexahydrobenzophenanthridines 
nafadotride 
BP-897 
ziprasidone (Geodon, Zeldox)
D4 dopamine presynaptic in frontal cortex, medulla and midbrain apomorphine
ABT-724
sulpiride (Dobren, Sulparex, Dogmatil, Dolmatil, Valirem)
trace amine receptor 1 (TAAR1) 3-iodothyronamine (T1AM)
b-phenylethylamineref
(mTAAR3 : isoamylamine; mTAAR5 and mTAAR7f both responded to tertiary amines (trimethylamine and N-methylpiperidine, and N-methylpiperidine, respectively)



TAAR2



TAAR3



rhodopsin / scotopsin / opsin 2 (<=light=> bathorhodopsin => lumirhodopsin => metarhodopsin I <=> metarhodopsin II => dissociation of all-trans-retinal => re-association with 11-cis-retinal)
rods

short wavelength (blue) photopsin / opsin 1
cones

intermediate wavelength (green) photopsin / opsin 1
cones

long wavelength (red) photopsin / opsin 1
cones

P2Y2 / P2U / P2N UTP
ATP
bone INS37217 
INS365 / diquafosol tetrasodium 
suramin
P2Y12 / P2T ADP platelets
thienopyridines
  • first-generation : ticlopidine (Ticlid
  • second-generation : clopidogrel (Plavix
  • third-generation : prasugrel (Effient) (hydrolysis by intestinal carboxylesterases and oxidation by intestinal and hepatic cytochrome P-450 enzymes convert prasugrel into its active metabolite)
  • ticagrelor (Brilinta)ref
PAFR (expressed even on nuclear envelope) (may couple with Gi, Gs, or Gq proteins depending on  the cell type) PAF
LTA
platelets, epidermal cells, leukocytes, smooth muscle cells, endothelium
natural compounds : 
  • terpenes
  • lignans
  • gliotoxins
lexipafant / BB-882
synthetic compounds : 
  • TCV-309
  • BN 52501
  • BN52021
C3aR (Gai; also Ga16-coupled) C3a brain, endothelial cells and activated B lymphocytes

CD88 / C5aR (Gai; also Ga16-coupled) C5a skin mast cells, neutrophils, monocytes, macrophages, hepatocytes (where stimulates synthesis of APPs), lung, smooth muscle and endothelial cells

B-LT2 LTB4


PPYR1 pancreatic polypeptide 1
pancreatic polypeptide 2



TAS2R1 bitter taste molecules taste receptor cells of the tongue and palate epithelia 6-n-propyl-2-thiouracil
TAS2R3 bitter taste molecules taste receptor cells of the tongue and palate epithelia

TAS2R4 bitter taste molecules taste receptor cells of the tongue and palate epithelia

TAS2R5 bitter taste molecules taste receptor cells of the tongue and palate epithelia

TAS2R7 bitter taste molecules taste receptor cells of the tongue and palate epithelia

TAS2R16 (5 SNPs) bitter taste molecules taste receptor cells of the tongue and palate epithelia phenylthiocarbamide (PTC)
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