platelets

Atopaxar, a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling. Atopaxar has been investigated for the treatment of Coronary Artery Disease and Acute Coronary Syndrome.

TRAP-6 (Thrombin Receptor Activator Peptide 6)(2TFA) is an agonist of protease-activated receptor 1 (PAR1).

Siguazodan (SKF 94836) is an effective, selective, orally active phosphodiesterase III ((PDE-III)) inhibitor with an IC50 of 117 nM. Siguazodan inhibited phenylephrine induced 5-HT release with an IC50 value of 4.2 μM. Siguazodan can increase cAMP accumulation in intact platelets, with EC50 of 18.88 μM.

Zoniporide hydrochloride is a selective inhibitor of NHE-1 with IC50 of 14 nM which is >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride shows an IC50 of 59 nM for NHE-1-dependent swelling of human platelets.

Atopaxar (E5555), a reversible PAR-1 thrombin receptor antagonist, interferes with platelet signaling. Atopaxar has been investigated for the treatment of Coronary Artery Disease and Acute Coronary Syndrome.

(Rac)-Modipafantis an orally available and selective platelet-activating factor receptor (PAFR) antagonist that inhibits PAF-induced aggregation of washed platelets in rabbits, and can be used to study arthritis and ischemia reperfusion (I R) in the superior mesenteric artery (SMA) of the rat.

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid and a potent, selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Additionally, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets, making it promising for cardiovascular disease research.

Aglafoline inhibits in a concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor). The IC50 values of Aglafoline on PAF (3.6 nM)-induced platelet aggregation were about 50 μM.

Carbazochrome (Adchnon) is an antihemorrhagic, or hemostatic, agent that will cease blood flow by causing the aggregation and adhesion of platelets in the blood to form a platelet plug, ceasing blood flow from an open wound. It is hoped that this drug can be used in the future for preventing excessive blood flow during surgical operations and the treatment of hemorrhoids, but research on its effectiveness and the severity of possible side effects remains to be fairly inconclusive. Carbazochrome has been investigated for use in the treatment of hemorrhoids in a mixture with troxerutin.

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Chlorobutanol hemihydrate (Chlorbutol hemihydrate) is an orally toxic preservative with antimicrobial activity that inhibits Gram-positive and Gram-negative bacteria and fungi, inhibits the aggregation and release of human platelets in vitro, and is commonly used in cosmetics.

Clopidogrel hydrogen sulfate ((S)-(+)-Clopidogrel bisulfate) , a selective, high-affinity P2Y12 receptor antagonist, suppressess fibrinogen binding to platelets and platelet adhesion and aggregation.

Elaidic acid (trans-Oleic Acid) is the 9-trans isomer of oleic acid. It is a monounsaturated trans-fatty acid which can be found in partially hydrogenated cooking oils. In human platelets incubated with arachidonic acid, elaidic acid inhibits HHT and HETE formation while inducing prostaglandin and thromboxane synthesis.

Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analog that preferentially activates cGMP-dependent protein kinase (PKG). It inhibits [3H]-arachidonic acid release in human platelets stimulated by gamma thrombin and can induce peripheral analgesia by activating ATP-sensitive K+ channels.

Aloxistatin (E64d) is an inhibitor of cysteine protease with blood platelet aggregation inhibiting activity. Aloxistatin is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases with the ability to inhibit calpain activity in intact platelets.

Rupatadine (UR-12592) is a potent dual PAF H1 antagonist with Ki values of 0.55 μM in rabbit platelet membranes and 0.1 μM in guinea pig cerebellum membranes.

U-73122 (U73122) , an effective PLC inhibitor, reduces agonist-induced Ca2+ increases in platelets and PMN.

Calpeptin is a potent, cell-permeable calpain inhibitor.

Bivalirudin (BG-8967) is a reversible inhibitor of α- and ζ-thrombin (Kis = 2.56 and 1.84 nM, respectively), enzymes that exhibit high fibrinogen-clotting activities.

Parmodulin 2 (ML 161) is the inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50: 0.26 μM for the inhibition of platelet P-selectin expression on human platelets). It also inhibits thrombin-induced platelet activation.

Arg-Gly-Glu-Ser acetate is a RGD related peptide that is a control for the RGDS activity of fibrinogen binding to activated platelets.

R 59-022 hydrochloride (DKGI-I hydrochloride) is a 5-HT Receptor antagonist that activates protein kinase C (PKC).R 59-022 hydrochloride is a DGK inhibitor (IC50:2.8 µM) that inhibits the phosphorylation of OAG to OAPA.R 59-022 enhances thrombin-induced triglyceride production in platelets and inhibits the production of phosphatidic acid in neutrophils. R 59-022 enhances thrombin-induced diglyceride production in platelets and inhibits phosphatidic acid production in neutrophils.

Foropafant (SR27417) is a highly potent and selective platelet-activating factor (PAF) receptor antagonist (Ki: 57 pM). Foropafant potently inhibits the PAF-induced aggregation of rabbit and human platelets.

SCH79797 dihydrochloride is an effective and selective antagonist of protease activated receptor 1 (PAR1) with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects.