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P2Y purinoceptor 12 Gαi Adenylate Cyclase Plasma membrane Ca-ADPase Cholinesterase Cytochrome P450 2C19 Cytochrome P450 2C9 Cytochrome P450 3A4 Cytochrome P450 2B6 ADP cAMP R-138727 Ca+ Ca+ Prasugrel Prasugrel Prasugrel R-138727 R-95913 Magnesium cAMP The active metabolite of prasurgrel has high affinity for the P2Y12 receptor to which it binds reversibly, preventing binding of ADP. Gi protein no longer inhibits adenylate cyclase, leading to a buildup of cAMP activating calcium efflux pump and prevents platelet activation Normally, ADP binds to P2Y12, activating the coupled Gi protein, inhibiting adenylate cyclase and leading to a shortage of cAMP. Calcium efflux is inactivated by lack of cAMP, inducing platelet activation and aggregation. Platelet Extracellular Space Affected Organs Symptom Relief Blood Clot Blood Vessel or Cell Damage Prasugrel is administered orally, through first pass metabolism into active metabolites Blood Vessel Endoplasmic Reticulum Prasugrel is a prodrug and through first pass metabolism, it is converted to its active form. The active metabolite then travels to the bloodstream to act on P2Y receptors that are located on platelets Hepatocyte
Melanosome Chloroplast Chloroplast Endoplasmic Reticulum P2RY12 GNAI1 ADCY10 Unknown BCHE CYP2C19 CYP2C9 CYP3A4 CYP2B6 Adenosine diphosphate cAMP R-138727 Calcium Calcium Prasugrel Prasugrel Prasugrel R-138727 R-95913
P2RY12 GNAI1 ADCY10 BCHE CYP2C19 CYP2C9 CYP3A4 CYP2B6 ADP cAMP R Ca+ Ca+ CS-747 CS-747 CS-747 R R-95913 Mg2+ cAMP The active metabolite of prasurgrel has high affinity for the P2Y12 receptor to which it binds reversibly, preventing binding of ADP. Gi protein no longer inhibits adenylate cyclase, leading to a buildup of cAMP activating calcium efflux pump and prevents platelet activation Normally, ADP binds to P2Y12, activating the coupled Gi protein, inhibiting adenylate cyclase and leading to a shortage of cAMP. Calcium efflux is inactivated by lack of cAMP, inducing platelet activation and aggregation. Platelet Extracellular Space Affected Organs Symptom Relief Blood Clot Blood Vessel or Cell Damage Prasugrel is administered orally, through first pass metabolism into active metabolites Blood Vessel Endoplasmic Reticulum Prasugrel is a prodrug and through first pass metabolism, it is converted to its active form. The active metabolite then travels to the bloodstream to act on P2Y receptors that are located on platelets Hepatocyte
Melanosome Chloroplast Chloroplast Endoplasmic Reticulum P2RY12 GNAI1 ADCY10 BCHE CYP2C19 CYP2C9 CYP3A4 CYP2B6 ADP cAMP R Ca2+ Ca2+ CS-747 CS-747 CS-747 R R-95913