Purinergic signaling (Homo sapiens)

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1915, 20, 214cAMP up due to ADORA1->Bronchoconstriction->Afferent arteriolar constriction in Kidney-> decreased heart ratecAMP up due to ADORA2A->Coronary artery vasodilatation->Decreased dopaminergic activity in CNS->Inhibition of central neuron excitation.ADORA1stimulateschannel permeability for:Gi/oprotein familyPhysiological downstream effects in target tissuecAMP down due to ADORA3->Cardiac muscle relaxation->Smooth muscle contraction->Cardioprotective in cardiac ischemia->Inhibition of neutrophil degranulationvia cGMP and Adenylyl cyclaseG protein couplingPro-InflammationP1 or Adenosine receptorscations in generalAgonist bindingAntagonist bindingMRE3008F20ADORA2AIstradefyllineMRS-1334PSB 10PSB-11GNAI1P2RY8CP-532,903P2RY10ADORA2BGNAI3MRS-1706TheophyllinePANX1P2RY2GNAT3AMPcAMPGNAT1LPAR6LPACGS-21680RegadenosonPSB 36SCH-442,416ATL-146eP2RY4ADORA1AdenosineMRS-3777CVT-6883UTPGNAZ2'-MeCCPAGNAT28-Phenyl-1,3-dipropylxanthineMRS-1220VUF-5574P2RX35'-N-ethylcarboxamidoadenosineN6-3-methoxyl-4-hydroxybenzyl adenine ribosideP2RX2P2RY1MRS-1523LPAR4PSB-603ATPP2RX7CaffeineCPXN-methyl-D-glucamineUDP-glucoseP2RX4SCH-58261MRS-1754P2RY11CCPAN6-CyclopentyladenosineLUF-5835SDZ WAG 994Gq/11LUF-5845BAY 60–6583ZM-241,385ADPMRS-1191PSB-1115GR 79236P2RX6HEMADOP2RY12GNAO1P2RX1P2RX5IB-MECAMRS-35582-Cl-IB-MECAADORA3PSB-0788P2RY14DPCPXP2RY13UDPP2RY6P2Y groupP2X groupligand gated ion channels1416861041617117316164421319GiGNASBLU-59375, 9Gefapixant12OpiranserinIvermectinZn(2+)19SuraminPPADS 1919L-Glutathione1, 1819Ca(2+)Mg(2+)Cu(2+)19GNAI219cAMP up due to ADORA2B ->Bronchoconstriction->BronchospasmADORA3inhibitsCa(2+)


Purinergic signalling is involved in several processes including neurologic, endocrine, and immune system signalling.

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  1. Freitas HR, Ferraz G, Ferreira GC, Ribeiro-Resende VT, Chiarini LB, do Nascimento JL, Matos Oliveira KR, Pereira Tde L, Ferreira LG, Kubrusly RC, Faria RX, Herculano AM, Reis RA; ''Glutathione-Induced Calcium Shifts in Chick Retinal Glial Cells.''; PLoS One, 2016 PubMed Europe PMC Scholia
  2. Li Q, Ye K, Blad CC, den Dulk H, Brouwer J, Ijzerman AP, Beukers MW; ''ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor.''; J Pharmacol Exp Ther, 2007 PubMed Europe PMC Scholia
  3. Baraldi PG, Tabrizi MA, Fruttarolo F, Romagnoli R, Preti D; ''Recent improvements in the development of A(2B) adenosine receptor agonists.''; Purinergic Signal, 2008 PubMed Europe PMC Scholia
  4. Froestl W, Muhs A, Pfeifer A; ''Cognitive enhancers (nootropics). Part 1: drugs interacting with receptors.''; J Alzheimers Dis, 2012 PubMed Europe PMC Scholia
  5. Marucci G, Dal Ben D, Buccioni M, Martí Navia A, Spinaci A, Volpini R, Lambertucci C; ''Update on novel purinergic P2X3 and P2X2/3 receptor antagonists and their potential therapeutic applications.''; Expert Opin Ther Pat, 2019 PubMed Europe PMC Scholia
  6. Mayer CA, Haxhiu MA, Martin RJ, Wilson CG; ''Adenosine A2A receptors mediate GABAergic inhibition of respiration in immature rats.''; J Appl Physiol (1985), 2006 PubMed Europe PMC Scholia
  7. Matsufuji H, Ueo H, Mori M, Kuwano H, Sugimachi K; ''Enhancement of esophageal carcinogenesis induced in rats by N-amyl-N-methylnitrosamine in the presence of 12-O-tetradecanoylphorbol-13-acetate.''; J Natl Cancer Inst, 1987 PubMed Europe PMC Scholia
  8. Martinson EA, Johnson RA, Wells JN; ''Potent adenosine receptor antagonists that are selective for the A1 receptor subtype.''; Mol Pharmacol, 1987 PubMed Europe PMC Scholia
  9. Garceau D, Chauret N; ''BLU-5937: A selective P2X3 antagonist with potent anti-tussive effect and no taste alteration.''; Pulm Pharmacol Ther, 2019 PubMed Europe PMC Scholia
  10. Cerqueira MD; ''The future of pharmacologic stress: selective A2A adenosine receptor agonists.''; Am J Cardiol, 2004 PubMed Europe PMC Scholia
  11. Moresco RM, Todde S, Belloli S, Simonelli P, Panzacchi A, Rigamonti M, Galli-Kienle M, Fazio F; ''In vivo imaging of adenosine A2A receptors in rat and primate brain using [11C]SCH442416.''; Eur J Nucl Med Mol Imaging, 2005 PubMed Europe PMC Scholia
  12. Richards D, Gever JR, Ford AP, Fountain SJ; ''Action of MK-7264 (gefapixant) at human P2X3 and P2X2/3 receptors and in vivo efficacy in models of sensitisation.''; Br J Pharmacol, 2019 PubMed Europe PMC Scholia
  13. Tracey WR, Magee WP, Oleynek JJ, Hill RJ, Smith AH, Flynn DM, Knight DR; ''Novel N6-substituted adenosine 5'-N-methyluronamides with high selectivity for human adenosine A3 receptors reduce ischemic myocardial injury.''; Am J Physiol Heart Circ Physiol, 2003 PubMed Europe PMC Scholia
  14. Klotz KN, Lohse MJ, Schwabe U, Cristalli G, Vittori S, Grifantini M; ''2-Chloro-N6-[3H]cyclopentyladenosine ([3H]CCPA)--a high affinity agonist radioligand for A1 adenosine receptors.''; Naunyn Schmiedebergs Arch Pharmacol, 1989 PubMed Europe PMC Scholia
  15. Hutchinson SA, Scammells PJ; ''A(1) adenosine receptor agonists: medicinal chemistry and therapeutic potential.''; Curr Pharm Des, 2004 PubMed Europe PMC Scholia
  16. Daly JW, Jacobson KA, Ukena D; ''Adenosine receptors: development of selective agonists and antagonists.''; Prog Clin Biol Res, 1987 PubMed Europe PMC Scholia
  17. Zocchi C, Ongini E, Conti A, Monopoli A, Negretti A, Baraldi PG, Dionisotti S; ''The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist.''; J Pharmacol Exp Ther, 1996 PubMed Europe PMC Scholia
  18. Freitas HR, Reis RA; ''Glutathione induces GABA release through P2X7R activation on Müller glia.''; Neurogenesis (Austin), 2017 PubMed Europe PMC Scholia
  19. North RA; ''Molecular physiology of P2X receptors.''; Physiol Rev, 2002 PubMed Europe PMC Scholia
  20. Williams M, Braunwalder A, Erickson TJ; ''Evaluation of the binding of the A-1 selective adenosine radioligand, cyclopentyladenosine (CPA), to rat brain tissue.''; Naunyn Schmiedebergs Arch Pharmacol, 1986 PubMed Europe PMC Scholia
  21. Zablocki JA, Wu L, Shryock J, Belardinelli L; ''Partial A(1) adenosine receptor agonists from a molecular perspective and their potential use as chronic ventricular rate control agents during atrial fibrillation (AF).''; Curr Top Med Chem, 2004 PubMed Europe PMC Scholia


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110333view06:41, 6 May 2020FehrhartOntology Term : 'nucleoside and nucleotide mediated signaling pathway' added !
110280view07:15, 2 May 2020EgonwRemoved whitespace from PubChem identifiers.
110275view07:02, 2 May 2020EgonwReplaced secondary ChEBI identifiers with a primary identifiers.
110157view06:34, 22 April 2020FehrhartWork in progress
110126view10:32, 19 April 2020FehrhartWork in progress
110125view10:18, 19 April 2020FehrhartWork in progress
110112view15:26, 17 April 2020FehrhartWork in progress
110110view10:47, 17 April 2020FehrhartOntology Term : 'nucleotide signaling via the purinergic P2Y receptors.' added !
110109view09:43, 17 April 2020FehrhartWork in progress
110108view09:33, 17 April 2020FehrhartNew pathway

External references


View all...
NameTypeDatabase referenceComment
2'-MeCCPAMetabolite122173097 (PubChem-compound)
5'-N-ethylcarboxamidoadenosineMetabolite3086599 (PubChem-compound)
8-Phenyl-1,3-dipropylxanthineMetabolite90477827 (PubChem-compound)
ADORA1GeneProductENSG00000163485 (Ensembl)
ADORA2AGeneProductENSG00000128271 (Ensembl)
ADORA2BGeneProductENSG00000170425 (Ensembl)
ADORA3GeneProductENSG00000282608 (Ensembl)
ADPMetabolite16761  (ChEBI)
AMPMetabolite16027 (ChEBI)
ATL-146eMetabolite9805430 (PubChem-compound)
ATPMetabolite15422 (ChEBI)
AdenosineMetabolite16335 (ChEBI)
BAY 60–6583Metabolite11717831 (PubChem-compound)
CCPAMetabolite123807 (PubChem-compound)
CGS-21680Metabolite3086599 (PubChem-compound)
CP-532,903Metabolite10479002 (PubChem-compound)
CPXMetabolite1917 (PubChem-compound) 8-Cyclopentyl-1,3-dimethylxanthine
CVT-6883Metabolite11270783 (PubChem-compound)
Ca(2+)MetaboliteCHEBI:29108 (ChEBI)
CaffeineMetabolite27732 (ChEBI)
Cu(2+)MetaboliteCHEBI:29036 (ChEBI)

Metabolite73282 (ChEBI) 8-Cyclopentyl-1,3-dipropylxanthine
GNAI1GeneProductENSG00000127955 (Ensembl)
GNAI2GeneProductENSG00000114353 (Ensembl)
GNAI3GeneProductENSG00000065135 (Ensembl)
GNAO1GeneProductENSG00000087258 (Ensembl)
GNASGeneProductENSG00000087460 (Ensembl) Gs alpha subunit (also Gαs, Gsα)
GNAT1GeneProductENSG00000114349 (Ensembl)
GNAT2GeneProductENSG00000134183 (Ensembl)
GNAT3GeneProductENSG00000214415 (Ensembl)
GNAZGeneProductENSG00000128266 (Ensembl)
GR 79236Metabolite9884817 (PubChem-compound)
GefapixantMetabolite24764487 (PubChem-compound)
HEMADOMetabolite10981286 (PubChem-compound) 2-(1-Hexynyl)-N-methyladenosine
IB-MECAMetabolite123683 (PubChem-compound) CF-101
IstradefyllineMetabolite5311037 (PubChem-compound)
IvermectinMetabolite9812710 (PubChem-compound)
L-GlutathioneMetaboliteCHEBI:16856 (ChEBI)
LPAMetabolite132742 (ChEBI) Lysophosphatidic acid
LPAR4GeneProductENSG00000147145 (Ensembl)
  • P2RY9
  • GPR23
LPAR6GeneProductENSG00000139679 (Ensembl)
MRE3008F20Metabolite5310960 (PubChem-compound)
MRS-1191Metabolite393594 (PubChem-compound)
MRS-1220Metabolite393595 (PubChem-compound)
MRS-1334Metabolite10324445 (PubChem-compound)
MRS-1523Metabolite3661570 (PubChem-compound)
MRS-1706Metabolite5139184 (PubChem-compound)
MRS-1754Metabolite6603931 (PubChem-compound)
MRS-3558Metabolite11248240 (PubChem-compound)
MRS-3777Metabolite56972200 (PubChem-compound)
Mg(2+)MetaboliteCHEBI:18420 (ChEBI)
N-methyl-D-glucamineMetaboliteCHEBI:59732 (ChEBI)
N6-3-methoxyl-4-hydroxybenzyl adenine ribosideMetaboliteB2
N6-CyclopentyladenosineMetabolite657378 (PubChem-compound)
OpiranserinMetabolite71566778 (PubChem-compound)
P2RX1GeneProductENSG00000108405 (Ensembl)
P2RX2GeneProductENSG00000187848 (Ensembl)
P2RX3GeneProductENSG00000109991 (Ensembl)
P2RX4GeneProductENSG00000135124 (Ensembl)
P2RX5GeneProductENSG00000083454 (Ensembl)
P2RX6GeneProductENSG00000099957 (Ensembl)
P2RX7GeneProductENSG00000089041 (Ensembl)
P2RY10GeneProductENSG00000078589 (Ensembl)
P2RY11GeneProductENSG00000244165 (Ensembl)
P2RY12GeneProductENSG00000169313 (Ensembl)
P2RY13GeneProductENSG00000181631 (Ensembl)
P2RY14GeneProductENSG00000174944 (Ensembl)
P2RY1GeneProductENSG00000169860 (Ensembl)
P2RY2GeneProductENSG00000175591 (Ensembl)
P2RY4GeneProductENSG00000186912 (Ensembl)
P2RY6GeneProductENSG00000171631 (Ensembl)
P2RY8GeneProductENSG00000182162 (Ensembl)
PANX1GeneProductENSG00000110218 (Ensembl)
PPADS Metabolite6093163 (PubChem-compound) pyridoxalphosphate-6-azophenyl-2',4'-disulfonic acid
PSB 10Metabolite10318703 (PubChem-compound)
PSB 36Metabolite9864310 (Chemspider)
  • 1-butyl-8-(3- noradamantyl)-3-(3-hydroxypropyl)xanthine
  • 1-Butyl-3-(3-hydroxypropyl)-8-(tricyclo[,7]non-3-yl)-3,7-dihydro-1H-purine-2,6-dione
PSB-0788Metabolite44186581 (PubChem-compound)
PSB-1115Metabolite5311479 (PubChem-compound)
RegadenosonMetabolite219024 (PubChem-compound)
SCH-442,416Metabolite10668061 (PubChem-compound)
SCH-58261Metabolite176408 (PubChem-compound)
SDZ WAG 994Metabolite18755269 (PubChem-compound)
SuraminMetabolite5361 (PubChem-compound)
TheophyllineMetabolite28177 (ChEBI)
UDP-glucoseMetabolite46229 (ChEBI)
UDPMetabolite58223 (ChEBI)
UTPMetabolite15713 (ChEBI)
VUF-5574Metabolite4046493 (PubChem-compound)
ZM-241,385Metabolite176407 (PubChem-compound)
Zn(2+)MetaboliteCHEBI:29105 (ChEBI)
cAMPMetaboliteCHEBI:17489 (ChEBI)

Annotated Interactions

No annotated interactions

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