TABLE 1

Selective ligands for purinergic receptors

ReceptorSignalingAgonistsAntagonistsAllosteric modulators
P2 receptors
P2X1ligand-gated ion channel2-MeSATP, L-β,γ-meATP, α,β-meATP, BzATP, HT-AMP, PAPET-ATP, Ap5A, CTPTNP-ATP, Ip5I, NF023, NF449, NF 279, PPNDS, Ro 0437626, IsoPPADS, MRS2159, phenol red, suramin
P2X2ligand-gated ion channelNF770, NF778, NF 279, PSB-10211, PPADS, RB-2, suramin, TNP-ATP
P2X3ligand-gated ion channel2-MeSATP, α,β-meATP, BzATP, D-β,γ-Me-ATP, 2-MeSATP, HT-AMP, PAPET-ATP, Ap5ATNP-ATP, A317491, AF-906, AF-219, RO3, NF110, spinorphin
P2X4ligand-gated ion channelBX-430, BBG, phenolphtalein, TNP-ATP 5-BDBD, PSB-12062, paroxetineIvermectin (positive)
P2X5ligand-gated ion channel
P2X6ligand-gated ion channel
P2X7ligand-gated ion channelBrilliant Blue G, A804598, A839977, decavanadate, KN62, KN-04, BBG, oxidized-ATP, A740003, A438079, AZ10606110AZ10606120 (negative), GW791343 (positive), GW791343 (negative), chelerythrine (negative), AZ11645373(negative) KN62 (negative) Ivermectin (positive)
P2Y1Gq2-Cl-ADP(α-BH3), 2-MeSADP, ADPβS, MRS 2365MRS2500, MRS2279, MRS2179, PIT2,2′-pyrydilisatogen tosylate (negative), BMS compound 16 (negative)
P2Y2GqUTPgS, Ap4A, 2-thioUTP, MRS2698, MRS2768, PSB1114
P2Y4GqMRS4062, MRS2927, (N)methanocarba UTP, UTPγSPPADS, reactive blue-2, ATP
P2Y6GqUDP, 3-phenacyl UDP PSB0474, MRS2693, MRS2957MRS2578, MRS2567
P2Y11GqATPγS, NF546, AR-C67085, NAD+NF157, NF340
P2Y12Gi2-MeSADP, ADPβSPSB-0739, AR-C 66096, ATP, AZD1283, ARL66096, cangrelor, Ap4a, ticlopidine
P2Y13Gi2-MeSADP, 2-MeSATPMRS2211, MRS2603, cangrelor, Ap4a
P2Y14GiMRS2905, αβ methilen 2-thioUTP, 2-thioUDPPPTN
P1 receptors
A1Gi/0R-PIA, GW493838, CHA, CPA, CCPA, TCPA, 2′-Me-CCPA, GR79236, selodenoson, capadenoson, tecadenoson, GS9667PSB36, DPCPX, CPFPX, KW-3902, toponafylline derenofylline, FK-453, SLV320, WRC-0571, DU172PD81723 (positive)
A2AGsCGS21680, ATL-313, ATL-146e, UK-432097, compound 4g, sonedenoson, binodenoson, regadenosonKW6002, CSC, MSX-2, SYN-115, BIIB014, ST-1535, SCH442416, ZM241385, SCH58261, preladenant
A2BGs, GqNECA, Bay 60-6583PSB603, PSB-0788, PSB1115, ATL 802, LAS8096, MRS1754, CVT-6883, MRE -2029-F20
A3Gs, GqCF-101, CF-102, CF-502, CO 608,039, HEMADO, MRS 5151, IB-MECA, MRS5698KF26777, PSB-10, PSB-11, MRE-3008-F20, MRS1220,VUF5574, MRS1523, MRS1191LUF6000 (positive), LUF6096 (positive)
  • A317491, 5-[[[(3-phenoxyphenyl)methyl][(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]carbonyl]-1,2,4-benzenetricarboxylic acid sodium salt hydrate; A438079, 3-(5-(2,3-dichlorophenyl)-1H-tetrazol-1-yl)methyl pyridine hydrochloride hydrate; A740003, N-(1-{[(cyanoimino)(5-quinolinylamino) methyl] amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide; A804598, N-Cyano-N′′-[(1S)-1-phenylethyl]-N′-5-quinolinyl-guanidine; A839977, 1-(2,3-dichlorophenyl)-N-[[2-(2-pyridinyloxy)phenyl]methyl]-1H-tetrazol-5-amine; ADPβS, adenosine 5-O-(2-thiodiphosphate); AF-219, 5-(2,4-diaminopyrimidin-5-yl)oxy-2-methoxy-4-propan-2-ylbenzenesulfonamide; AF-906, 2-[[4-amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propane-1,3-diol; Ap5A, P1,P5-Di(adenosine-5′)pentaphosphate; AR-C67085, [[[[(2R,3S,4R,5R)-5-(6-amino-2-propylsulfanylpurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]-dichloromethyl]phosphonic acid; AR-C 66096, 2-(propylthio)adenosine-5′-O-(β,γ-difluoromethylene)triphosphate tetrasodium salt; ARL66096, 2-(propylthio)adenosine-5′-O-(β,γ-difluoromethylene)triphosphate tetrasodium salt; ATL-146e, 4-{3-[6-amino-9-(5-ethylcarbamoyl-3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-cyclohexanecarboxylic acid methyl ester; ATL-313, methyl 4-[3-[6-amino-9-[(2R,3R,4S,5S)-5-(cyclopropylcarbamoyl)-3,4-dihydroxyoxolan-2-yl]purin-2-yl]prop-2-ynyl]piperidine-1-carboxylate; ATPγS, adenosine-5′-(γ-thio)-triphosphate; AZD1283, ethyl 5-cyano-2-methyl-6-[4-[[[(phenylmethyl)sulfonyl]amino]carbonyl]-1-piperidinyl]-3-pyridinecarboxylate; 5-BDBD, 5-(3-bromophenyl)-1,3-dihydro-2H-benzofuro[3,2-e]-1,4-diazepin-2-one; BX-430, N-[2,6-dibromo-4-(1-methylethyl)phenyl]-N′-(3-pyridinyl)urea; BzATP, 2′(3′)-O-(4-benzoylbenzoyl)adenosine 5′-triphosphate triethylammonium; CCPA, 2-chloro-N6-cyclopentyladenosine; CF-502, [(1′R,2′R,3′S,4′R,5′S)-4-{2-chloro-6-[(3 chlorophenylmethyl)amino]purin-9-yl}-1-(methylaminocarbonyl)bicyclo[3.1.0]hexane-2,3-diol]; CHA, N6-cyclohexyl adenosine; 2-Cl-ADP(α-BH3), [[(2R,3S,4R,5R)-5-(6-amino-2-chloropurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy phosphonooxyphosphoryl]boron(1-); CPA, N6-cyclopentyladenosine; CPFPX, 8-cyclopentyl-3-(3-fluoranylpropyl)-1-propyl-7H-purine-2,6-dione; CSC, 8-[(E)-2-(3-chlorophenyl)vinyl]-1,3,7-trimethyl-3,7-dihydro-1H-purine-2,6-dione; CVT-6883, 3-ethyl-3,9-dihydro-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-4-yl]-1H-purine-2,6-dione; CVT-6883, 3-ethyl-3,9-dihydro-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-4-yl]-1H-purine-2,6-dione; DPCPX, 8-cyclopentyl-1,3-dipropylxanthine; GR79236, N-[(1S,2S)-2-hydroxycyclopentyl]adenosine; GS9667, 5′-S-(2-fluorophenyl)-N-[(1R,2R)-2-hydroxycyclopentyl]-5′-thioadenosine; GW493838, (2S,3S,4R,5R)-2-(5-tert-butyl-1,3,4-oxadiazol-2-yl)-5-{6-[(4-chloro-2-fluorophenyl)amino]-9H-purin-9-yl}oxolane-3,4-diol; HEMADO, 2-(1-hexynyl)-N-methyladenosine; HT-AMP, [(2R,3S,4R,5R)-5-(6-amino-2-hexylsulfanylpurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl dihydrogen phosphate; Ip5I, diinosine pentaphosphate; KF26777, (2-(4-bromophenyl)-7,8-dihydro-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one dihydrochloride); KN62, 4-[(2S)-2-[(5-isoquinolinylsulfonyl)methylamino]-3-oxo-3-(4-phenyl-1-piperazinyl)propyl] phenyl isoquinolinesulfonic acid ester; KW-3902, 1,3-dipropyl-8-(3-noradamantyl)xanthine, 8-(hexahydro-2,5-methanopentalen-3a(1H)-yl)-3,7-dihydro-1,3-dipropyl-1H-purine-2,6-dione; KW6002, (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methylxanthine, 8-[(1E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1H-purine-2,6-dione; L-β,γ-meATP, l-beta,gamma-metilen ATP; 8MDP, 2,2′,2″,2′″-[[4,8-bis(hexahydro-1(2H)-azocinyl)pyrimido[5,4-d]pyrimidine-2,6-diyl]dinitrilo]tetrakisethanol; α,β-meATP, alpha, beta metilen ATP; 2′-Me-CCPA, 2′-metil 2-chloro-N6-cyclopentyladenosine; 2-MeSADP, [(2R,3S,4R,5R)-5-(6-amino-2-methylsulfanylpurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylphosphono hydrogen phosphate; 2-MeSATP, 2-(methylthio)adenosine 5′-triphosphate tetrasodium salt; MRS1191, 3-ethyl-5-benzyl-2-methyl-4-phenylethynyl-6-phenyl-1,4-(±)-dihydropyridine-3,5-dicarboxylate; MRS1220, 9-chloro-2-(2-furyl)-5-phenylacetylamino[1,2,4]-triazolo[1,5-c]quinazoline; MRS1523, 2,3-diethyl-4,5-dipropyl-6-phenylpyridine-3-thiocarboxylate-5-carboxylate; MRS1754, 8-[4-[[(4-cyano)phenylcarbamoylmethyl]oxy]phenyl]-1,3-di-(n-propyl)xanthine; MRS2179, 2′-deoxy-N6-methyladenosine 3′,5′-bisphosphate tetrasodium salt; MRS2211, 2-[(2-chloro-5-nitrophenyl)azo]-5-hydroxy-6-methyl-3-[(phosphonooxy)methyl]-4-pyridinecarboxaldehyde disodium salt; MRS2279, (1R*,2S*)-4-[2-chloro-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hexane-1-methanol dihydrogen phosphate ester diammonium salt; MRS 2365, [[(1R,2R,3S,4R,5S)-4-[6-amino-2-(methylthio)-9H-purin-9-yl]-2,3dihydroxybicyclohex-1-yl]methyl] diphosphoric acid mono ester; MRS2567, 1-isothiocyanato-4-[2-(4-isothiocyanatophenyl)ethyl]benzene; MRS2578, 1,4-di[3-(3-isothiocyanatophenyl)thioureido]butane; MRS2603, [(2Z)-2-[(4-chloro-3-nitrophenyl)hydrazinylidene]-4-formyl-6-methyl-5-oxopyridin-3-yl]methyl dihydrogen phosphate; MRS2693, 5-iodouridine-5′-O-diphosphate trisodium salt; MRS2905, 2-thiouridine-5′-O-(α, β-methylene)diphosphate trisodium salt; MRS2957, P1-[5′(N4-methoxycytidyl)]-P3-(5′-uridyl)-triphosphate tri(triethylammonium) salt; MRS4062, [[(2R,3S,4R,5R)-3,4-dihydroxy-5-[2-oxo-4-(3-phenylpropoxyamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate; MRS 5151,6-(2-chloro-6-(((9-((1S,2R,3S,4R,5S)-3,4-dihydroxy 5(methylcarbamoyl)bicyclo[3.1.0]hexan-2-yl)-9H-purin-6-yl)amino)methyl)phenyl)hex-5-ynoic acid; MRS5698, (1S,2R,3S,4R,5S)-4-[6-[[(3-chlorophenyl)methyl]amino]-2-[2-(3,4-difluorophenyl)ethynyl]-9H-purin-9-yl]-2,3-dihydroxy-N-methylbicyclo[3.1.0]hexane-1carboxamide; NF023, 8,8′-[carbonylbis(imino-3,1-phenylenecarbonylimino)]bis-1,3,5-naphthalene-trisulphonic acid, hexasodium salt; NF157, 8,8′-[carbonylbis[imino-3,1-phenylenecarbonylimino(4-fluoro-3,1-phenylene)carbonylimino]]bis-1,3,5-naphthalenetrisulfonic acid hexasodium salt; NF 279, 8,8′-[carbonylbis(imino-4,1-phenylenecarbonylimino-4,1-phenylenecarbonylimino)]bis-1,3,5-naphthalenetrisulfonic acid hexasodium salt; NF340, 4,4′-(carbonylbis(imino-3,1-(4-methyl-phenylene)carbonylimino))bis(naphthalene-2,6-disulfonic acid) tetrasodium salt; NF449, 4,4′,4″,4′″-[carbonylbis(imino-5,1,3-benzenetriyl-bis(carbonylimino))]tetrakis-1,3-benzenedisulfonic acid, octasodium salt; NF546, 4,4′-(carbonylbis(imino-3,1-phenylene-carbonylimino-3,1-(4-methyl-phenylene)carbonylimino))-bis(1,3-xylene-alpha,alpha′;-diphosphonic acid tetrasodium salt; NF770, 5-methoxy-3-[[3-[[3-[[3-[[5-[(8-methoxy-3,6-disulfonaphthalen-2-yl)carbamoyl]-2 methylphenyl]carbamoyl]phenyl]carbamoylamino]benzoyl]amino]-4 methylbenzoyl]amino]naphthalene-2,7-disulfonic acid; NF778, 6,6-(carbonylbis(imino-3,1-phenylenecarbonylimino-3,1-(4-methyl-phenylene)carbonylimino))bis(1-methoxy-naphthalene-3,5-disulfonic acid) tetrasodium salt; (N)methanocarba UTP, [[4-(2,4-dioxopyrimidin-1-yl)-2,3-dihydroxy-1-bicyclo[3.1.0]hexanyl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate; PAPET-ATP, 2-[2-(4-aminophenyl)ethylthio]adenosine 5′-triphosphate; 3-phenacyl UDP, [(2R,3S,4R,5R)-5-(2,4-dioxo-3-phenacylpyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphono hydrogen phosphate; PPADS, pyridoxalphosphate-6-azophenyl-2′,4′-disulfonic acid; PPNDS, pyridoxal-5′-phosphate-6-(2′-naphthylazo-6′-nitro-4′,8′-disulfonate); PSB0474, 3-(2-oxo-2-phenylethyl)-uridine-5′-diphosphate disodium salt; PSB-0739, 1-amino-9,10-dihydro-9,10-dioxo-4-[[4-(phenylamino)-3-sulfophenyl]amino]-2-anthracenesulfonic acid sodium salt; PSB-0788, 8-[4-[4-(4-chlorobenzyl)piperazide-1-sulfonyl)phenyl]]-1-propylxanthine; PSB-10, 8-ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride; PSB-10211, 1-amino-4-[3-[(4,6-dichloro-1,3,5-triazin-2-yl)amino]anilino]-9,10-dioxoanthracene-2-sulfonic acid; PSB-11, (8R)-8-ethyl-1,4,7,8-tetrahydro-4-5H-imidazo[2,1-i]purin-5-one hydrochloride; PSB1115, 4-(2,3,6,7-tetrahydro-2,6-dioxo-1-propyl-1H-purin-8-yl)-benzenesulfonic acid; PSB-12062, 10-[(4-methylphenyl)sulfonyl]-10H-phenoxazine; PSB-12379, N6-benzyl-α,β-methyleneadenosine 5′-diphosphate disodium salt; PSB36, 1-butyl-3-(3-hydroxypropyl)-8-(3-noradamantyl)xanthine,1-butyl-8-(hexahydro-2,5 methanopentalen-3a(1H)-yl)-3,9-dihydro-3-(3-hydroxypropyl)-1H-purine-2,6-dione; PSB603, 8-[4-[4-(4-chlorophenzyl)piperazide-1-sulfonyl)phenyl]]-1-propylxanthine; Ro 0437626, N-[(1R)-2-[[(1S,2R,3S)-1-(cyclohexylmethyl)-3-cyclopropyl-2,3-dihydroxypropyl]amino]-2-oxo-1-(4 thiazolylmethyl)ethyl]-1H-benzimidazole-2-carboxamide; R-PIA, (2R,3S,4R,5R)-2-(hydroxymethyl)-5-[6-[[(2R)-1-phenylpropan-2-yl]amino]purin-9-yl]oxolane-3,4-diol; SCH442416, 2-(2-furanyl)-7-[3-(4-methoxyphenyl)propyl]-7H-pyrazolo [4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine; SCH58261, 7-(2-phenylethyl)-5-amino-2-(2-furyl)-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine; SLV320, trans-4-[(2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexanol; ST-1535, 2-butyl-9-methyl-8-(2H-1,2,3-triazol-2-yl)-9H-purin-6-amine; SYN-115, 4-hydroxy-N-[4-methoxy-7-(4-morpholinyl)-2-benzothiazolyl]-4-methyl-1-piperidinecarboxamide; TCPA, N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine; 2-thioUDP, [(2R,3S,4R,5R)-3,4-dihydroxy-5-(4-oxo-2-sulfanylidenepyrimidin-1-yl)oxolan-2-yl]methyl phosphono hydrogen phosphate; 2-thioUTP, 2-thiouridine-5′-triphosphate; TNP-ATP, 2′,3′-O-(2,4,6-trinitrophenyl) adenosine 5′-triphosphate; UK-432097, (2S,3S,4R,5R)-5-{6-[(2,2-diphenylethyl)amino]-2-[(2-{N-[1-(pyridin-2-yl)piperidin-4-yl]-(C-hydroxycarbonimidoyl)amino}ethyl)carbamoyl]-9H-purin-9-yl}-N-ethyl-3,4-dihydroxyoxolane-2-carboximidic acid; VUF5574, N-(2-methoxyphenyl)-N′-[2-(3-pyridinyl)-4-quinazolinyl]-urea; WRC-0571, 5-[[9-methyl-8-[methyl(propan-2-yl)amino]purin-6-yl]amino]bicyclo[2.2.1]heptan-2-ol; ZM241385, 4-[2-(7-amino-2-(2-furyl)[1,2,4-triazolo[2,3-a] [1,3,5]triazin-5-yl-amino]ethyl phenol.