|
|
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a2A | adrenaline![]() ![]() |
presynaptic on solitary tract nucleus and presynaptic
neurons in ortosympathetic
system, pancreatic islets b
cells, platelets![]() |
a2-selective
adrenergic
agonists
![]() |
alkylating holoalkylamine
chlorpromazine (CPZ) hydrochloride (Largactil®, Thorazine®, Chlomazine®, Dormazine®, Fenactil®, Hibernal®, Ormazine®, Promaz®, Prozil®, Solidon®, Sonazine®, Taroctyl®) atipamezole mianserin (Athymil®, Bolvidon®, Norval®, Tolvin®) etoperidone |
a2B | adrenaline![]() ![]() |
presynaptic on solitary tract nucleus and presynaptic
neurons in ortosympathetic
system, pancreatic islets b
cells, platelets![]() |
a2-selective
adrenergic agonists
![]() |
alkylating holoalkylamine
chlorpromazine (CPZ) hydrochloride (Largactil®, Thorazine®, Chlomazine®, Dormazine®, Fenactil®, Hibernal®, Ormazine®, Promaz®, Prozil®, Solidon®, Sonazine®, Taroctyl®) |
a2C | adrenaline![]() ![]() |
presynaptic on solitary tract nucleus and presynaptic
neurons in ortosympathetic
system, pancreatic islets b
cells, platelets![]() |
a2-selective
adrenergic agonists
![]() |
alkylating holoalkylamine
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
|
alkaloids
butylscopolamine (Buscopam®)
methylatropine quaternary ammonium
osenapine clozapine (Clozaril®, Leponex®) NRI :
tripitramine methoctramine procyclidine (Arpicolin®, Kemadren®, Kemadrin®, Kemadrine®, Osnervan®, Procyclid®) |
M4 | ACh![]() |
striatum | synthetic choline derivatives
|
alkaloids
butylscopolamine (Buscopam®)
methylatropine quaternary ammonium
clozapine (Clozaril®, Leponex®) NRI :
![]() tropicamide procyclidine (Arpicolin®, Kemadren®, Kemadrin®, Kemadrine®, Osnervan®, Procyclid®) |
MLT1A / MT1 | melatonin![]() |
hypothalamic suprachiasmatic nucleus and hypophysial pars tuberalis | ramelton (Rozerem®)
(also MLT2![]() |
|
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
|
|
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 :
|
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=>
|
SST![]() cortistatin ![]() |
|
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![]() ![]() 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 :
|
|||
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![]() ![]() |
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![]() |
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![]() |
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 :
|
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
|
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![]() ![]() ![]() |
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![]() ![]() ![]() |
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) | morphine![]() |
vascular tissue, mononuclear cells, neutrophils, and neuroblastoma cells. | ||
k1
opiates / opioids receptor (KOR) (it can homodimerize or
heterodimerize
with d
opiods![]() |
dynorphins![]() ![]() |
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 ![]() ICI174864 ICI 199441 ![]() TRK-820 bremazocine and ketocyclazocine >> morphine ![]() ![]() |
naloxone![]() naltrexone ![]() N-phenylpropyl-4b-methyl-5-(3-hydroxyphenyl)- 7a-[3-(1-piperidinyl)propanamido]morphan [(-)-3b] DIPPA UPHIT fedotozine nor-binaltorphimine ![]() GNTI ![]() |
k2 opiates / opioids receptor (KOR) | dynorphin A![]() ![]() |
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![]() ![]() |
|||
d1
opiates / opioids receptor (DOR) (it can heterodimerize with
k
opiods![]() |
Met5-enkephalin![]() ![]() |
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 ![]() |
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![]()
![]() |
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![]() |
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![]() |
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) :
/ levomepromazine (Levoprome®, Nozinan®, Neurocil®, Veractil®, Sinogan®) |
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![]() |
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
|
|
PAFR (expressed even on nuclear envelope) (may couple with Gi, Gs, or Gq proteins depending on the cell type) | PAF![]() LTA ![]() |
platelets![]() |
natural compounds :
synthetic compounds :
|
|
C3aR (Gai;
also Ga16![]() |
C3a![]() |
brain, endothelial cells and activated B lymphocytes | ||
CD88
/ C5aR (Gai;
also Ga16-coupled![]() |
C5a![]() |
skin mast 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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for |
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