201PathwayTiclopidine Action PathwayTiclopidine, marketed as Ticlid, is an antiplatelet drug that targets the P2Y12 receptor of platelets. Ticlopidine is taken orally and is a prodrug that must be metabolically activated before it can be effective. It first enters the liver and enters the endoplasmic reticulum where it is metabolized to form the active metabolite. First, it is catalyzed by cytochromes P450 2C19, 2B6 and 1A2 into 2-oxoclopidogrel. Secondly, it is processed by cytochromes P450 2B6, 2C9, 2C19, 3A4, 3A5, and serum paraoxonase/arylesterase 1 into the active metabolite of clopidogrel. The active metabolite of clopidogrel then enters the blood stream, where it binds irreversibly to the P2Y purinoreceptor 12 on the surface of platelet cells, preventing ADP from binding to and activating it. Clopidogrel prevents the activation of the Gi protein associated with the P2Y12 receptor from inactivating adenylate cyclase in the platelet, leading to a buildup of cAMP. This cAMP then activates calcium efflux pumps, preventing calcium buildup in the platelet, which would cause activation, and later, aggregation.Drug ActionPW000287TopPathwayVisualizationContext3031200800#000099PathwayVisualization207201Ticlopidine PathwayTiclopidine, marketed as Ticlid, is an antiplatelet drug that targets the P2Y12 receptor of platelets. Ticlopidine is taken orally and is a prodrug that must be metabolically activated before it can be effective. It first enters the liver and enters the endoplasmic reticulum where it is metabolized to form the active metabolite. First, it is catalyzed by cytochromes P450 2C19, 2B6 and 1A2 into 2-oxoclopidogrel. Secondly, it is processed by cytochromes P450 2B6, 2C9, 2C19, 3A4, 3A5, and serum paraoxonase/arylesterase 1 into the active metabolite of clopidogrel. The active metabolite of clopidogrel then enters the blood stream, where it binds irreversibly to the P2Y purinoreceptor 12 on the surface of platelet cells, preventing ADP from binding to and activating it. Clopidogrel prevents the activation of the Gi protein associated with the P2Y12 receptor from inactivating adenylate cyclase in the platelet, leading to a buildup of cAMP. This cAMP then activates calcium efflux pumps, preventing calcium buildup in the platelet, which would cause activation, and later, aggregation.Drug188818520712Jennings LK, Saucedo JF: Antiplatelet and anticoagulant agents: key differences in mechanisms of action, clinical application, and therapeutic benefit in patients with non-ST-segment-elevation acute coronary syndromes. Curr Opin Cardiol. 2008 Jul;23(4):302-8. doi: 10.1097/HCO.0b013e3283021ad9.201Pathway8893304967Saltiel E, Ward A: Ticlopidine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in platelet-dependent disease states. Drugs. 1987 Aug;34(2):222-62.201Pathway2Platelet CL:00002331CellCL:00000001Homo sapiens9606EukaryoteHuman10Cell MembraneGO:000588611Extracellular SpaceGO:00056152Endothelium BTO:00003938Blood VesselBTO:0001102741114101PW_BS00001416212PW_BS0000168681111PW_BS0000868752TiclopidineHMDB0014353Ticlopidine is an effective inhibitor of platelet aggregation. The drug has been found to significantly reduce infarction size in acute myocardial infarcts and is an effective antithrombotic agent in arteriovenous fistulas, aorto-coronary bypass grafts, ischemic heart disease, venous thrombosis, and arteriosclerosis. [PubChem]55142-85-3C07140547295885273DB00208ClC1=CC=CC=C1CN1CCC2=C(C1)C=CS2C14H14ClNSInChI=1S/C14H14ClNS/c15-13-4-2-1-3-11(13)9-16-7-5-14-12(10-16)6-8-17-14/h1-4,6,8H,5,7,9-10H2PHWBOXQYWZNQIN-UHFFFAOYSA-N5-[(2-chlorophenyl)methyl]-4H,5H,6H,7H-thieno[3,2-c]pyridine263.786263.05354785-4.080ticlopidine01Ticlopidina;TiclopidinumPW_C008752Ticlopi3405141853P2Y purinoceptor 12Q9H244Receptor for ADP and ATP coupled to G-proteins that inhibit the adenylyl cyclase second messenger system. Not activated by UDP and UTP. Involved in platelets aggregationHMDBP02244P2RY123q24-q25AB0526841964143457161361808672P2Y purinoceptor 121PW_P0000728618531754falsePW_R001754Right659987521Compoundfalse6600721ProteinComplexfalse6786875214157false28531010regular200190288718531480false2806958subunitregular200130255572207142876288710287M385 500 C385 530 385 704 385 720 148false18falsetrueM 625.2419513485014 282.68328157299976 L 640 280 L 654.7580486514986 277.3167184270002410288M385 720 C385 690 521 180.5 545 197.5 5true1820052071754147003678610287Left39255510288Right7877440151.01.00211580250473M113 862 C113 812 163 762 213 762 C328 762 476 762 591 762 C641 762 691 812 691 862 C691 902 691 955 691 995 C691 1045 641 1095 591 1095 C476 1095 328 1095 213 1095 C163 1095 113 1045 113 995 C113 955 113 902 113 862 1true6578.0333.036224914546263756115744710894