MAIN GqPCRs Click here for their STP.
Common biological outputs : Both PS and PI are found esclusively in the cytosolic layer of the plasma membrane, of which they represent 8% and 1%, respectively : they are both translocated in the extracellular layer upon platelets activation and in cells undergoing apoptosis, where it acts as a "eat-me" flag.

Proteolytic activation of PARs is irreversible and cleaved receptors internalize and are degraded in lysosomes. Therefore, PARs are single-use receptors that probably mediate signaling during pathophysiological or "emergency" conditions when PAR agonists are generated or released.
 
GPCR name
physiological ligand(s)
expressed on ...
agonists
antagonists
NK1 SP > NKA > NKB microglia 
colon circular muscle
substance P methyl ester SR140333 
LY303870 
L-733,060 
CP99994 
CJ-12,255
aprepitant (Emend)
spantide I 
NK2 NKA > NKB > SP corpus cavernosum and spongiosum. b-[Ala8]NKA4-10 GR94800 
GR159897 
nepadutant 
NK3 NKB > NKA > SP
GR138676 SR142802 
SB223412
neuromedin B receptor NMB normal and neoplastic lung and for gastrointestinal epithelial tissue

Y2 NPY neurons 
epithelia in colon mucosa.
NPY13-16
NPY18-36

a1A / a 1C (4 different isoforms) adrenaline < noadrenaline smooth muscle (cutaneous blood vessels, genitourinary, intestinal) hepatocytes, cardiomyocytes  a1-selective 
  • methoxamine hydrochloride (Vasoxyl)
  • phenylephrine (AK-Dilate, Mydfrin, Neo-Synephrine, ...)
  • mephentermine sulfate (Wyamine sulfate)
  • metaraminol bitartrate (Aramine)
  • midodrne (Proamatine)
alkylating holoalkylamine 
  • phenoxybenzamine hydrochloride (Dibenzyline)
benzenesulfonamide 
  • tamsulosin (Flomax, Omnic) (high)
imidazolines 
  • phentolamine mesylate (Regitine)
  • tolazoline hydrochloride (Priscoline) (also an a2-antagonist)
piperazinyl quinazolines 
  • prazosin hydrochloride (Minipress, Alpress, Hypotens, Hypovase, Sinetens) (high)
  • terazosin hydrochloride (Hytrin, Teraprost)
  • doxazosin (Cardura)
    • doxazosin gastrointestinal therapeutic system (GITS) 
  • alfuzosin (Uroxatral, Xatral)
indoles  haloperidol
chlorpromazine
ketanserin (Sufrexal, Aseranox, Ketensin, Ketenserina, Perketan, Serepress, Sparfloxacine
urapidil 
bunazosin (Detantol
carvedilol (Coreg
labetalol hydrochloride (Normodyne, Trandate, ...) 
medroxalol 
bucindol
a1B adrenaline < noadrenaline smooth muscle (cutaneous blood vessels, genitourinary, intestinal) hepatocytes, cardiomyocytes a1-selective 
  • methoxamine hydrochloride (Vasoxyl)
  • phenylephrine (AK-Dilate, Mydfrin, Neo-Synephrine, ...)
  • mephentermine sulfate (Wyamine sulfate)
  • metaraminol bitartrate (Aramine)
  • midodrne (Proamatine)
alkylating holoalkylamine  imidazolines :  piperazinyl quinazolines :  indoles :  haloperidol
chlorpromazine
ketanserin
urapidil
bunazosin
carvedilol
labetalol
medroxalol
bucindol
a1D adrenaline < noadrenaline smooth muscle (cutaneous blood vessels, genitourinary, intestinal) hepatocytes, cardiomyocytes a1-selective 
  • methoxamine hydrochloride (Vasoxyl)
  • phenylephrine (AK-Dilate, Mydfrin, Neo-Synephrine, ...)
  • mephentermine sulfate (Wyamine sulfate)
  • metaraminol bitartrate (Aramine)
  • midodrne (Proamatine)
alkylating holoalkylamine :  benzenesulfonamide : 
  • tamsulosin (Flomax, Omnic) (high)
imidazolines :  piperazinyl quinazolines :  indoles  haloperidol
chlorpromazine
ketanserin
urapidil
bunazosin
carvedilol
labetalol
medroxalol
bucindol
H1 histamine solitary tract nucleus => hypothermy, anorexia, arterial pressure, analgesia, arousal; endothelial cells => contraction 2-aminoethylthiazole 
6-[2-(4-imidazolyl)ethylamino]-N
(4-trifluoromethylphenyl)hepatanecarboxamide (HTMT) 
2-methylhistamine 
2-pyridylethylamine 
2-thiazolylethylamine 
2-(3-trifluoromethylphenyl)histamine (FMPH) 
chlorpromazine
ketanserin
mianserin (Athymil, Bolvidon, Norval, Tolvin
antazoline 
mirtazepine (Remeron, Norset, Zipsin
emedastine difumarate (Emadine
olopatadine hydrochloride / AL-4943A / KW-4679 (Opatanol, Patanase, Patanol) (high affinity; low affinity for H2)
ketotifen fumarate (Zaditor
nortriptyline (Aventyl, Pamelor
triprolidine 
iodobolpyramine
iodoazidophenpyramine
risperidone (Risperdal, Risperidal, Belivon, Risperin, Rispolept, Rispolin
sedative antihistamines / lipophilic / first generation 
  • tricyclic dibenzoxepins
    • doxepin hydrochloride (Zonalon, Sinequan)
  • ethanolamines
    • carbinoxamine maleate (Rondec)
    • clemastine fumarate (Tavist)
    • diphenhydramine hydrochloride (Allerga, Benadon, Benadryl, Benylin, Caladryl, Nautamine)
    • dimenidrate (Xamamine)
  • ethylenediamines
    • pyrilamine maleate (Poly-histine-D)
    • tripelennamine hydrochloride or citrate (PBZ)
  • alkylamines
    • pheniramine
    • chlorpheniramine maleate (Chlor-Trimeton, Polamin, Polaramin, Polaramin AR, Polaramin espettorante)
    • brompheniramine maleate (Bromphen)
  • pyperazines
    • hydroxyzine hydrochloride (Atarax, Maraz, AH3 N, Apo Hydroxyzine, Elroquil N, Hydroxyzin, Hydroxyzinum, Iremofar, Masmoran, Multipax, Navicalm, Novo-Hydroxyzine, PMS-Hydroxyzine, Q-Med hydroxyzine, Ucerax) or pamoate (Vistaril)
    • benclizine (Hexafene in combination with hydroxyzine)
    • chlorcyclizine (Di-Paralene, Trihistan)
    • cyclizine hydrochloride or lactate (Marezine)
    • meclonizine (Diligan in combination with hydroxyzine and nicotinic acid)
    • meclizine hydrochloride (Antivert, Meclozine, Dramamine II)
  • phenothiazines
    • promethazine hydrochloride (Farganesse, Phenergan)
  • piperidines
    • cyproheptadine hydrochloride (Carpantin, Periactin)
    • phenindamine tartrate (Nolahist)
  • mepyramine
nonsedative antihistamines / hydrophilic / second generation 
  • alkylamine
    • acrivastine (Semprex-D)
  • piperazines
    • cetirizine hydrochloride (Zirtec, Zyrtec)
    • levocetirizine (Xyzal)
  • phthalazinones
    • azelastine hydrochloride (Astelin, Azeptin)
  • piperidines
    • levocabastine hydrochloride (Livostin)
    • loratadine (Claritin)
    • azatadine (Optomine)
    • desloratadine (Azomyr)
    • fexofenadine (FEX) (Allegra, Telfast)
    • terfenadine (Trexyl, Terfed, Terin)
    • astemizole (Acemix, Acipax, Afdizol, Alerzote, Astelong, Astem, Hismanal, Histalong, Histeeise, Minastem, Perione, Stemix)
  • bepotastine or betotastine besilate / TAU-284 (Talion)
  • epinastine (Relestat)
M1 ACh gastroenteric tract ; autonomic ganglia, CNS (solitary tract nucleus, chemo-receptor trigger zone (CTZ; area postrema), striatum) McN-A-433 (functional rather than subtype-specific selectivity) 
(S)-BN 228 
oxotremorine 
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 
  • short-acting
    • ipratropium bromide (Atrovent; in combination with fenoterol in Duovent, Berodual; in combination with albuterol in Combivent)
    • oxitropium bromide
  • long-acting
    • tiotropium bromide (Spiriva)
  • methscopolamine bromide (Pamine)
  • glycopyrrolate (Robinul)
  • homatropine methylbromide
  • propantheline bromide (Pro-Banthine)
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 
clozapine 
NRI : 
  • protriptyline (Vivactil)
SNRI 
  • amitriptyline (Laroxil, Elavil)
  • imipramine (Tofranil)
  • paroxetine
phenothiazines : 
  • ethopropazine / profenamine (Pardidol, Parsidol, Parsitan, Dibutil, Lysivane, Rodipal
M3 (it can homodimerize) ACh smooth muscle, bladder, vasculature endothelium, secretory glands (basolateral membrane of parietal cells of stomach, lachrimal and  salivatory glands,...), striatum cevimeline (Evoxac
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)
  • methscopolamine bromide (Pamine)
  • oxitropium bromide
  • propantheline bromide (Pro-Banthine)
  • tiotropium bromide (Spiriva)
tetriary amines 
  • homatropine hydrobromide (Isopto Homatropine)
  • cyclopentolate hydrochloride (AK-Pentolate, Cyclogyl, Pentolair)
  • tropicamide (Mydriacyl, Tropicacyl, Opticyl)
  • benztropine mesylate (Cogentin)
  • trihexyphenidyl hydrochloride (Artane)
  • dicyclomine hydrochloride (Bentyl, ...)
  • flavoxate hydrochloride (Urispas; Cistalgan in combination with propyphenazone)
  • oxybutynin chloride (Ditropan)
  • tolterodine (Detrol)
  • solifenacin succinate (Vesicare)
olanzapine 
clozapine 
NRI : 
  • protriptyline (Vivactil)
SNRI 
  • amitriptyline (Laroxil, Elavil)
  • imipramine (Tofranil)
  • paroxetine (Paxil, Seroxat)
darifenacin 
hexahydrosiladifenidol
M5 ACh CNS 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)
  • methscopolamine bromide (Pamine)
  • oxitropium bromide
  • propantheline bromide (Pro-Banthine)
  • tiotropium bromide (Spiriva)
tetriary amines 
  • homatropine hydrobromide (Isopto Homatropine)
  • cyclopentolate hydrochloride (AK-Pentolate, Cyclogyl, Pentolair)
  • tropicamide (Mydriacyl, Tropicacyl, Opticyl)
  • benztropine mesylate (Cogentin)
  • trihexyphenidyl hydrochloride (Artane)
  • dicyclomine hydrochloride (Bentyl, ...)
  • flavoxate hydrochloride (Urispas; Cistalgan in combination with propyphenazone)
  • oxybutynin chloride (Ditropan)
  • tolterodine (Detrol)
olanzapine (Zyprexa
clozapine (Clozaril, Leponex) (high affinity; also low affinity D2 antagonist) 
NRI : 
  • protriptyline (Vivactil)
SNRI : 
  • amitriptyline (Laroxil, Elavil)
  • imipramine (Tofranil)
  • paroxetine (Paxil, Seroxat)
TRH receptor TRH


5-HT2A / 2 / D receptor 5-HT platelets, smooth muscle, astrocytes, vascular endothelial, choroid plexus cells, oligodendrocytes (?), lymphocytes natural and semisynthetic ergot alkaloids
a-methyl-5-HT 
dobutamine 
DOI 
trazodone (Desyrel, Trittico, Molipaxin, Pragmarel, Thombran, Trazodil, Trazolan)  => m-chlorophenylpiperazine (mCPP) 
ketanserin (Sufrexal, Aseranox, Ketensin, Ketenserina, Perketan, Serepress, Sparfloxacine) (also on 5-HT2C receptor)
ritanserin (Tisterton) (also on 5-HT2B and 5-HT2C receptor)
deramciclane 
LY53857 
MDL 100,907 (selective)
cyproheptadine hydrochloride (Carpantin, Periactin, Dronactin, Cipractin, Nuran, Oractin, Periactinol
methysergide (Sansert
AT-1015 
"atypical" antipsychotics : 
  • clozapine (Clozaril, Leponex) (high affinity; also low affinity D2 antagonist)
  • mirtazepine (Remeron, Norset, Zipsin
  • olanzapine (Zyprexa)
  • quetiapine fumarate (Seroquel)
  • zotepine (Zoleptil)
  • sertindole (Serlect, Serdolect)
  • ORG-5222
  • iloperidone (Zomaril)
  • risperidone (Risperdal, Risperidal, Belivon, Risperin, Rispolept, Rispolin)
  • tiospirone 
  • trazodone
  • ziprasidone (Geodon, Zeldox)
5-HT2B / 2F 5-HT stomach fundus natural and semisynthetic ergot alkaloids
a-methyl-5-HT 
dobutamine 
DOI 
trazodone (Desyrel, Trittico, Molipaxin, Pragmarel, Thombran, Trazodil, Trazolan)  => m-chlorophenylpiperazine (mCPP) 
LY53857 
minaprine (Cantor
ritanserin (Tisterton
sertindole (Serlect, Serdolect
tiospirone 
5-HT2C / 1C (also GiPCR ?)  5-HT choroid plexus natural and semisynthetic ergot alkaloids
a-methyl-5-HT 
dobutamine 
DOI 
trazodone (Desyrel, Trittico, Molipaxin, Pragmarel, Thombran, Trazodil, Trazolan)  => m-chlorophenylpiperazine (mCPP) 
ketanserin (Sufrexal, Aseranox, Ketensin, Ketenserina, Perketan, Serepress, Sparfloxacine) (also on 5-HT2A)
LY53857 
mesulergine 
methysergide (fsert
mirtazepine (Remeron, Norset, Zipsin
ritanserin (Tisterton
sertindole (Serlect, Serdolect
tiospirone 
SB206553 (selective)
ritanserin (also on 5-HT2B and 5-HT2A receptor)
V1a AVP / ADH vascular smooth muscle, platelets, myometre, renal, adrenal, hepatocytes (ACTH-secreting anterior pituitary cells) [Phe2, Ile3, Orn8]AVP
terlipressin (Variquel, Glypressin)
d(CH2)5[Tyr(Me)2]AVP
dP [Tyr(Me)2]AVP 
SR 49059 / relcovaptan
OPC-21268 
YM 087 / conivaptan (Vaprisol) (also antagonist on V2)
mozavaptan / OPC-31260 (Physuline) (also antagonist on V2)
V1b / V3 AVP / ADH ACTH-secreting anterior pituitary cells, ACTH-secreting pituitary adenomas, adrenal medulla, brain, pancreas, bronchial carcinoids responsible for the ectopic ACTH syndrome deamino [D-3-(3'-pyridyl)-Ala2]AVP dP [Tyr(Me)2]AVP
SSR-149415
OT receptor (Gq and G11) OT myometrium  [Thr4, Gly7]OT d(CH2)5 [Tyr(Me)2, Thr4, Orn8]OT1-8
atosiban (1-deamino-2-d-Tyr(OEt)-4-Thr-8-Orn-oxytocin) 
barusiban
P2Y1 ADP placenta, brain, prostate, ovary, platelets 2-methylthioATP Reactive Blue 2
suramin
P2Y4 UTP placenta
PPADS
P2Y5 orphan


P2Y6 UDP

PPADS; 
suramin
P2Y8


suramin
P2Y11 (also GsPCR) ATP

suramin
P2Y12
platelets

P2Y13



ETA endothelin-1

PD 180988 (CI-1034) 
PD 156707 (CI-1020) 
BQ-123 
BQ-788 
TAK-044 
nonpeptide antagonists : 
  • atrasentran
  • bosentan (Tracleer)
  • sitaxsentan
ETB endothelin-1
endothelin-2
endothelin-3


TAK-044
EP1 (also on nuclear envelope) PGE2 neurons, endothelial cells  of CNS ONO-D1-004 
gemeprost
AH6809 ; 
L-818638
EP3_ (also on nuclear envelope) (also GiPCR and GsPCR) PGE2 neurons in the organum vasculosa lamina terminalis (OVLT) at the midline of the preoptic area (POA), endothelial cells of CNS ONO-AE-248; 
sulprostone; 
misoprostol (Arthrotec, together with diclofenac
gemeprost
L-826266
FP (+ FP negative regulator) PGF2a
prodrugs :
  • latanoprost / AFP-168 (Xalatan)
  • tafluprost / DE-085
isopropyl unoprostone (Rescula)
bimatoprost (Lumigan) is a structural analog of PGF2a-ethanolamide (prostamide F2a), which is formed from the endocannabinoid anandamide by a biosynthetic pathway involving COX-2. The target receptor for bimatoprost and the prostamides appears unique and unrelated to PG- and endocannabinoid-sensitive receptorsref
travoprost (Travatan)

TP (also G12PCR
  • TPa (platelets)
  • TPb (vascular smooth muscle cells (VSMC))
In addition to being products of differential splicing, are under the transcriptional control of distinct promoters
TxA2
PGH2
  U46619 
picotamide (N,N'bis(3-pyridinylmethyl)-4-methoxy-isophthalamide) 
SQ 29,548 (1S-(1a,2b(5Z),3b,4 a))-7-(3((2-((phenylamino)carbonyl)hydrazino) methyl)-7-oxabicyclo(2.2.1)hept-2-yl)-5-heptenoic acid)
GR32191
EDG1 / S1P1 sphingosine-1-phosphate endothelial cells, lymphocytes FTY720
suramin

EDG2 / ventricular zone gene (VZG)-1 / LPA1 LPA neurons in the ventricular zone of the developing cortex : its expression in neurons declines after birth, but is induced again in the myelinating cells of the adult nervous system (Schwann cells, oligodendrocytes), adipocytes, T lymphocytes, fibroblasts

EDG3 / S1P3 (also GiPCR and G12PCR) sphingosine-1-phosphate vascular system FTY720 suramin
EDG4 / LPA2 (also GiPCR) LPA constitutive in CD4+ T lymphocytes, induced in ovarian cancer cell lines

EDG5 / S1P2 (also GiPCR and G12PCR) sphingosine-1-phosphate vascular smooth muscle cells, melanoma cells (FTY720)
EDG6 / S1P4 sphingosine-1-phosphate T lymphocytes FTY720
EDG7 / LPA3 LPA species with sn-2 unsaturated fatty acid ester


EDG8 / S1P55 sphingosine-1-phosphate neurons FTY720
mGluRI 1 Glu hippocampus quisqualate ; 
trans-ACPD (+/--1-aminocyclopentane-trans-1,3-dicarboxylic acid, an equimolecular mixture of 1S, 3R and 1R, 3S-ACPD and an agonist at both group I and group II mGluRs) 

mGluRI 5 Glu
quisqualate ; 
trans-ACPD (+/--1-aminocyclopentane-trans-1,3-dicarboxylic acid, an equimolecular mixture of 1S, 3R and 1R, 3S-ACPD and an agonist at both group I and group II mGluRs) 
2-methyl-6-(2-phenylethenyl)pyridine (SIB-1893) 
calcium acamprosate / N-acetylhomotaurine (Campral, Aotal, Zulex)
CCR1 CCL3 / MIP-1a
CCL5 / RANTES
CCL7 / MCP-3
CCL12 / MIP-5
CCL13 / MCP-4
CCL14a / HCC-1
CCL23 / CKb-8 / MPIF-1-1
monocytes, Th1 lymphocytes and Th2 lymphocytes, B cells, neutrophil, basophils, eosinophils, immature MDCs, NK cells, smooth muscle cells, syncytiotrophoblast 

CCR2 : CCR2A and CCR2B (sulfation of amino-terminal tyrosines) isoforms. It can heterodimerize with CXCR4 / CD184 / fusin / LESTR or with CCR5. CCL2 / MCP-1
CCL5 / RANTES
CCL7 / MCP-3
CCL8 / MCP-2
CCL13 / MCP-4
CCL15 / HCC-2 / leukotactin / Lkn-1 / MIP-1d / MIP-5
monocytes, activated T cell, B cells, basophils, DCs, NK cells, eosinophils, smooth muscle cells (?), skin fibroblast (?), synovial fibroblast, bronchial epithelial cells
AMD3100 (Mozobil; source : AnorMED, Inc)ref1, ref2
CTCE-0021 : a cyclized CXCR4 agonist peptideref
4f-benzoyl-TN14003
CCR3 CCL5 / RANTES
CCL7 / MCP-3
CCL8 / MCP-2
CCL11 / eotaxin-1
CCL12 / MIP-5
CCL13 / MCP-4
CCL24 / eotaxin-2
CCL26 / eotaxin-3
Th2 lymphocytes, eosinophils, mast cells, basophils, DCs, airway epithelial cells, syncytiotrophoblast 

CCR4 CCL2 / MCP-1
CCL3 / MIP-1a
CCL5 / RANTES
CCL17 / TARC
CCL22 / MDC
Th2 lymphocytes, basophils (?), immature DCs, NK cells (?)

CCR5 / CD195. Sulfation of amino-terminal tyrosines. It can heterodimerize with CCR2B. CCL3 / MIP-1a
CCL4 / MIP-1b
CCL5 / RANTES
CCL8 / MCP-2
monocytes, Th1 lymphocytes (?), immature MDCs, NK cells (?), astrocytes, neurons, synovial fibroblast CMPD167
CCR6 CCL19 / MIP-3b / ELC
CCL20 / exodus-1 / MIP-3a / LARC
b-defensins
memory T cells, B cells, immature BMDCs, PBMCs, syncytiotrophoblast 

CCR7 / CDw197 CCL19 / MIP-3b / ELC
CCL21 / SLC / 6Ckine / exodus-2
naive CD4+ and CD8+ T-cell lines, B-cell lines (?), mature MDCs, NK cells (?), breast cncer cells

CCR8 CCL1 / I-309
CCL17 / TARC
CCL19 / MIP-3b / ELC
Th2 lymphocytes, NK cells, monocytes (?)

CCR9 / chemokine binding protein 2 (CCBP2) CCL2 / MCP-1
CCL3 / MIP-1a
CCL3L1
CCL5 / RANTES
CCL8 / MCP-2
CCL11 / eotaxin
CCL13 / MCP-4
CCL19 / MIP-3b / ELC
CCL25 / TECK
immature and mature DCs, thymocytes, macrophages

CCR10 CCL2 / MCP-1
CCL27 / CTACK
skin-homing memory T cells, breast cancer cells

CCR11 CCL2 / MCP-1
CCL19 / MIP-3b / ELC
CCL21 / 6Ckine / exodus-2 / SLC
CCL25 / TECK
various organs (heart, small intestine, murine astrocytes and microgliaref)

CXCR1 / IL-8Ra / CDw128a (also activates rho) CXCL6 / GCP-2
CXCL7 / NAP-2 / CTAP-II
CXCL8 / IL-8ref
neutrophils, NK cells

CXCR2 / IL-8Rb / CDw128b (also stimulates EGFR cascade) CXCL1 / GRO-a
CXCL2 / GRO-b
CXCL3 / GRO-g
CXCL5 / ENA-78
CXCL6 / GCP-2
CXCL7 / NAP-2 / CTAP-II
CXCL8 / IL-8
CTAP-III
DC inflammatory protein-1 (DCIP1)
neutrophil chemoattractant N-acetyl Pro-Gly-Pro (PGP), derived from the breakdown of extracellular matrix (ECM)ref
neutrophils, NK cells, fibroblasts, neurons, endothelial cells, melanoma cells
N-(3-(aminosulfonyl)-4-chloro-2-hydroxyphenyl)-N'-(2,3-dichlorophenyl) urea
SB-251353 : an N-terminal truncated form of human CXCL2ref
CXCR3 / CD183 CXCL9 / MIG
CXCL10 / IP-10
CXCL11 / I-TAC
- in mice but not in humans  - CCL21
Th1 lymphocytes, CD8+ CTL, NK cells, B cells, B cell chronic lymphocytic leukemia, MALTomas, and other B cell non-Hodgkin lymphomas

CXCR4 / CD184 / fusin / LESTR. Sulfation of amino-terminal tyrosines or chondroitin sulfate chain at serine 18. It can heterodimerize with CCR2. CXCL12 / SDF-1 T cells, monocytes, immature and mature MDCs, naive and mature B cells, NK cells , astrocytes, neurons, synovial fibroblast, enterocytes, melanoma cells, syncytiotrophoblast 
  • POL5551
  • plerixafor / AMD-3100 (Mozobil; source : AnorMED, Inc)ref1, ref2
CXCR5 CXCL13 / BCA-1 / BLC activated T cells, naive B cells

CXCR6 / STRL33 / Bonzo / TYMSTR CCL16 / HCC-4 / SexCkine Th1 lymphocytes, NK cells (?)

CX3CR1 fractalkine / CX3CL1 monocytes, neutrophils (?), and peripheral blood killer cells (NK cells, ...)

XCR1 lymphotactin / neurotactin / XCL1 activated T cells, NK cells

XCR2 XCL2 / ATAC / SCM-1b


MLT2 / MT2 / Mel1b melatonin
ramelton (Rozerem) (also MLT1 agonist) 4-P-PDOT
GRP / bombesine receptor GRP / bombesine


AT1a (it can homodimerize) angiotensin II
mechanical stressref
cardiovascular cells : 
  • juxtaglomerular cells (JGC) for short-loop negative feedback mechanism of renin incretion
  • vascular smooth muscle cells of precapillary arterioles and postcapillary venules
  • heart (?)

-artans : 
  • bithienylmethylacrylic acid derivative
    • eprosartan (Teveten)
  • biphenylmethyl derivatives
    • candesartan cilexetil (Amias, Atacand)
    • irbesartan (Avapro, Aprovel, Karvea)
    • losartan (Cozaar)
    • telmisartan (Micardis) (also a PPAR-g agonist)
    • valsartan (Diovan; Exforge in combination with amlodipine)
GnRH-R / LHRH-R GnRH-1 / LHRH-1
GnRH-2 / LHRH-2

"superactive" GnRH analogs (GnRHa) that, given repeatedly, down-regulate GnRH-R  : 
  • nonapeptides :
    • buserelin (Receptal, Suprefact, Supercur)
    • deslorelin (Somagard, Ovuplant
    • fertirelin
    • goserelin (Zoladex
    • histrelin (Supprelin
    • leuprolide / leuprorelin (Lucrin, Lupron, Enantone
  • decapeptides :
    • nafarelin (Synarel
    • triptorelin (Trelstar, Decapeptyl)
Name 
Amino acid sequence 
  1 pGlu  2 His  3 Trp  4 Ser  5 Tyr  6 Gly  7 Leu  8 Arg  9 Pro  10 Gly-NH2
Human GnRH 
GnRH-1  1 2 3 4 5 6 7 8 9 10
GnRH-II  1 2 3 4 His 6 Trp Tyr 9 10
GnRH III  1 2 3 4 5 6 Trp Leu 9 10
GnRH agonist 
Nonapeptides
Leuprorelin  1 2 3 4 5 D-Leu 7 8 9- N-Et-NH2
Buserelin  1 2 3 4 5 D-Ser(But) 7 8 9- N-Et-NH2
Goserelin  1 2 3 4 5 D-Ser(But) 7 8 9- AzaGly-NH2
Histrelin  1 2 3 4 5 d-His(Imbzl)  7 8 9- N-Et-NH2
Deslorelin  1 2 3 4 5 d-Trp  7 8 9- N-Et-NH2
fertirelin
1
2
3
4
5
6
7
8
9-
N-Et-NH2
Decapeptides
Nafarelin  1 2 3 4 5 (d-Nal) 7 8 9 Gly-NH2
Triptorelin  1 2 3 4 5 d-Trp  7 8 9 Gly-NH2
GnRH antagonist
Abarelix  D-Ala  D-Phe  D-Ala  4 5 D-Asp  7 Lys(iPr)  9 D-Ala 
Antarelix  D-Nal  D-Phe  D-Pal  4 Phe  D-Hcit  7 Lys(iPr)  9 D-Ala 
Cetrorelix  D-Nal  D-Phe  D-Pal  4 5 D-Cit 7 8 9 D-Ala 
Ganirelix  D-Nal  D-Phe D-Pal  4 5 D-hArg  7 HArg  9 D-Ala
iturelix D-Nal D-Phe D-Pal  4 NicLys  D-NicLys  7 Lys(iPr)  9 D-Ala 
Nal-Glu  D-Nal  D-Phe  D-Pal  4 D-Glu  D-Glu  7 8 9 D-Ala
 
abarelix (Plenaxis
antarelix
cetrorelix (Cetrotide
ganirelix (Antagon, Orgalutran
iturelix (Antide
Nal-Glu
GRP39 GHRH
hexarelin ; 
MK-0677 ; 
EP51389 ;
JV-1-36
JV-1-42
GPR54 kisspeptins neurons in pons, midbrain, thalamus, hypothalamus, hippocampus, amygdala, frontal cortex, striatum, cerebellum, brainstem, and spinal cord, pituitary, placenta, pancreas, liver, intestine

GH secretagogue receptor (GHSR) ghrelin
cortistatin

GH-releasing peptides (GHRP) (orally active) 
  • GHRP-2
  • His-D-Trp-Ala-Trp-D-Phe-Lys-NH2 (GHRP-6)
  • [D-Lys-3]-GHRP-6

GRP38 / MTLR1 GHRH
Mo
smooth muscle cells in duodenum and antrum macrolide antibiotics
CCK1 / CCKA CCK8 >> gastrin = CCK4 gallbladder and exocrine pancreas cells
devazepide
lorglumide 
loxiglumide 
dexloxiglumide 
CCK2 / CCKB CCK8 > gastrin = CCK4 ECL cells and basolateral membrane of parietal cells in stomach 
parafollicular C cells of thyroid
pentagastrin (Peptavlon
minigastrin / Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala -Tyr-Gly-Trp-Met-Asp-Phe-NH2
CI988
JB-5008 (Gastrazole
YM022 
PD-135,158. 
L-365,26 
S-0509
galanin receptor 2 (also GiPCR) galanin childhood neuroblastic tumors, brain, gastrointestinal system, and hypothalamopituitary axis

neurexin 1
cholinergic neurons a-latrotoxin / BWSV
some odorants



B1(inducible) BK
Lys-BK / kallidin
low levels in normal tissues but can be induced in response to pathophysiological stimuli, gastric cancer  des-Arg9-bradykinin 
des-Arg10-kallidin
des-Arg9-[Leu8]-bradykinin
B2 (constitutive : it can heterodimerize with AT1) Lys-BK / kallidin
Lys-des-Arg-BK
many cell types (including dendritic cells)
HOE-140 / icatibant (Firazyr ; source : Jerini)
CP 0127 
FRI 73657
B-LT1 / P2Y7 LTB4 pancreatic cancer tissues
CP105696 
LY223982
cysLT1 LTC4
LTD4
LTE4
UDP
nasal mucosa, bronchial smooth muscle cells and postcapillary venule endothelial cells
zafirlukast (Accolate
pranlukast 
montelukast (Singulair
L649,923
cysLT2 LTC4
LTD4
LTE4
pulmonary vein, Purkinje fibers of the heart, discrete regions of the adrenal gland, brain, spleen

neurotensin receptor 1 neurotensin

SR48692
neurotensin receptor 2 neurotensin brain
levocabastine hydrochloride (Livostin)
some sweet molecules



some bitter molecules



PAR-1 proteases that cleave the extracellular NTD, which then acts as a ligand :  endothelial cells 
oral epithelial cells 
platelets
thrombin receptor activating peptide (TRAP) 
  • SFLLR-NH2 (SF-NH2
  • TFLLR-NH2 (TF-NH2
heterocycle-based peptide-mimetic :
  • RWJ-56110
  • RWJ-58259 
  • aparafluoroFRCyclohexylACitY-NH2 (Cit-NH2)
PAR-2 proteases that cleave the extracellular NTD, which then acts as a ligand : 
  • coagulation factor VIIa
  • coagulation factor Xa 
  • trypsin 
  • tryptase 
eosinophils
endothelial cells 
oral epithelial cells 
myocytes 
nerve fibers
activating peptide (AP) 
SFLLR-NH2 (SF-NH2)

PAR-3 proteases that cleave the extracellular NTD, which then acts as a ligand :  eosinophils
platelets
endothelial cells (?)
oral epithelial cells

neutrophil serine proteinases : 
PAR-4 proteases that cleave the extracellular NTD, which then acts as a ligand :  platelets GYPGKF-NH2
AYPGKF-NH2
GYPGQV-NH2

FPR1 bacterial N-formyl-Met-Leu-Phe (fMLP) (high affinity)

cyclosporin H (CsH) 
spinorphin
FPR-like (FPRL) 1 / ALXR inflammatory : various synthetic peptides
anti-inflammatory :
  • ANXA1 
  • Ac2-26 
  • constitutively expressed on neutrophils, eosinophils, and monocytes, induced on epithelium and vascular endothelium Helicobacter pylori peptide Hp
    FPR-like (FPRL) 2



    C3aR (Ga16; also Gai-coupled) C3a brain, endothelial cells and activated B lymphocytes

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

    calcium sensor receptor (CASR) (it can homodimerize) (also GiPCR) high Ca2+ECM parathyroid chief cells, thyroid C-cells, cells of the kidney tubule, bone, colonic crypt epithelial cells (including colon carcinoma cells), brain, epidermis, lens, stomach, pancreas, liver, breast, ovary, placenta, prostate, testis, and bone marrow cells (including myeloma cells) polycations : the lack of selectivity and relatively low potency of these cations for the CaR indicate that charged residues in the ECD of the CaR are critical for receptor activation through electrostatic interactions.
    Although not perfect, a correlation exists between the potencies of cations at the CaR and their net positive charge density. In addition, recent studies indicate the possibility that the CaRs act as sensors for pHref and L-amino acidsref. Indeed, L-amino acids suppress PTH secretion in vitro, suggesting that L-amino acids are physiological regulators of PTH secretion and whole body calcium metabolism.
  • inorganic polycations : 
  • Gd3+ > (neomycin B > Ca2+ >) Mg2+
  • Be2+, Ba2+, Sr2+, La3+
  • organic polycations :
  • spermine
  • hexacyclin
  • polylysine
  • polyarginine
  • protamine
  • amyloid b--peptide
  • neomycin B
  • gentamicin
  • calcimimetics : allosteric agonists to stabilize an active conformation of CaR
    • first generation : 
      • phenylalkylamines
        • NPS R467
        • L-phenylalanine
        • NPS R-568 
        • (R)-2-[1-(1-naphthyl)ethylaminomethyl]-1H-indole (Calindol
    • second generation : 
      • AMG 073
      • cinacalcet hydrochloride / KRN1493 (in Japan) (Sensipar (source : Amgen) in USA, Mimpara in Europe)
    calcilytics (allosteric inverse agonists to stabilize an inactive conformation of CaR)ref :
    • NPS 2143 
    • Calhex 231
    GPR91 citric acid cycle intermediate succinateref


    GPR99 / GPR80 citric acid cycle intermediate a-ketoglutarateref


    Web resources :


    Copyright 2001-2014 Daniele Focosi. All rights reserved Terms of use  | Legal notices
    About this site  |  Site map  |  Acknowledgements | ; |    |  Current link partners
     Abbreviations and acronyms  |  Medical terminology  |  Add a link  |  Translate this site into your favourite language  |  Softwares Cite this page!


    This website subscribes to the
          HONcode principles of the HON Foundation. Click to verify.
    PicoSearch
     

    Search 



    Search 
    for 



    Search Medical Dictionary 
    for