• Ga₁₁
• Ga₁₄
• Ga₁₅ / Ga₁₆
• Ga_q
• Ga_z

• opening of Ca²⁺ HVA N channels and closure of K⁺_M channels =>
• depolarization or excitatory postsynaptic potential (EPSP)
• exocytosis
• contraction of smooth and skeletal muscles

platelets

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
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  indoramin ergotoxin 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  phenoxybenzamine imidazolines :  phentolamine tolazoline (also an a2-antagonist) piperazinyl quinazolines :  prazosin (high) terazosin doxazosin alfuzosin  indoles :  indoramin ergotoxin 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 :  phenoxybenzamine benzenesulfonamide :  tamsulosin (Flomax®, Omnic®) (high) imidazolines :  phentolamine tolazoline (also an a2-antagonist) piperazinyl quinazolines :  prazosin (high) terazosin doxazosin alfuzosin  indoles  indoramin ergotoxin 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  atropine / dimethylscopolamine  scopolamine  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 :  atropine / dimethylscopolamine  scopolamine  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  atropine / dimethylscopolamine  scopolamine  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	blood vessels, hepatocytes, ACTH-secreting anterior pituitary cells	[Phe2, Ile3, Orn8]AVP	d(CH2)5[Tyr(Me)2]AVP dP [Tyr(Me)2]AVP  SR 49059  OPC-21268  OPC-31260  YM 087 / conivaptan (Vaprisol®) (also antagonist on V2)
V1b / V3	AVP / ADH	ACTH-secreting anterior pituitary cells, ACTH-secreting pituitary adenomas, bronchial carcinoids responsible for the ectopic ACTH syndrome	deamino [D-3-(3'-pyridyl)-Ala2]AVP	dP [Tyr(Me)2]AVP
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		AMD3100ref1, ref2
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
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		AMD-3100
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			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®) valsartan (Diovan®)
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 erythromycin  oleandomycin  azithromycin  clarithromycin
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)		icatibant (HOE-140)  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 :  thrombin	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 :  thrombin	eosinophils platelets endothelial cells (?) oral epithelial cells		neutrophil serine proteinases :  human leukocytre elastase (HLE) cathepsin G proteinase 3 (PR3)
PAR-4	proteases that cleave the extracellular NTD, which then acts as a ligand :  thrombin trypsin cathepsin G proteinase 3 (PR3)	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 : bacterial N-formyl-Met-Leu-Phe (fMLP) (low affinity)  serum amyloid A (SAA) LXA4 aspirin-triggered lipoxin (ATL) / 15(R)-epi-LXA4 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® 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 :

• Signaling through PKC
• Ga_q pathway at STKE [free registration required !]

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