venous

Pentoxifylline (PTX) modulates immunologic activity by stimulating cytokine production. Pentoxifylline is a methylxanthine derivative that inhibits phosphodiesterase and affects blood rheology. It also inhibits platelet aggregation and improves blood flow by increasing erythrocyte and leukocyte flexibility.

Taurolidine is a synthetic taurine analog with antimicrobial and anti-neoplastic actions. It displays broad bactericidal and fungicidal activity.

LY 517717 is an orally active inhibitor of coagulation factor Xa with antithrombotic activity for the study of venous thromboembolism (VTE).

Zifaxaban (TY-602) is an orally active, competitive and selective inhibitor of factor Xa (FXa) with an IC50 of 11.1 nM for human FXa.Zifaxaban has a very high affinity, more than 10,000-fold higher than that of other serine proteases.Zifaxaban can be used to study arterial and venous thrombosis.

Eribaxaban (PD348292) is an orally available factor Xa inhibitor for the prevention and treatment of venous thromboembolism.

Flovagatran (TGN 255) is an orally active, potent, and selective inhibitor of thrombin and parenteral direct factor II.Flovagatran is used to study venous thromboembolism.

Naroparcil, an orally available thioglycoside analog of 4-methylumbelliferyl β-D-xyloside, showed antithrombotic effects in the Wessler sludge model of venous thrombosis (jugular vein).Naroparcil enhanced the formation of the thrombin heparin cofactor II complex, induced dermatophyte sulfate-like substances in plasma from treated rabbits appearance, but reduced the formation of thrombin antithrombin III complexes in plasma incubated with (125I)-human alpha-thrombin.

LI-2242 is a potent inositol hexakisphosphate kinase (IP6K) inhibitor with IC50s of 31 nM, 42 nM, 8.7 nM, and 1944 nM for IP6K1, IP6K2, IP6K3, and IPMK, respectively.LI-2242 ameliorated hepatic steatosis by reducing the expression of genes that enhance lipid uptake, lipid stabilization, and adipogenesis, and enhanced mitochondrial oxygen consumption rate (OCR) and insulin signaling in adipocytes and hepatocytes in vitro. LI-2242 ameliorated diet-induced obesity, hyperglycemia and hepatic steatosis in mice.LI-2242 can be used to study type II diabetes, obesity, metabolic complications, venous thrombosis and psychiatric disorders.

Nicorandil (SG-75)(Ikorel) acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It undertakes this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of cGMP leading to both arterial and venous vasodilatation by de-phosphorylation of the myosin light chain.

Chromocarb (Chromone-2-carboxylic acid) is a vascular protective agent used to treat venous disorders and microvascular affections.

An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.

Norepinephrine bitartrate acts directly on the α- and β-adrenergic receptors. Norepinephrine Bitartrate is a bitartrate salt of norepinephrine, a synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine. Clinically, norepinephrine is used as a peripheral vasoconstrictor that causes constriction of arterial and venous beds via its alpha-adrenergic action. It is also used as a potent inotropic and chronotropic stimulator of the heart mediated through its beta-1 adrenergic action.

Saponins (Sapogenins Glycosides) are a mixture of triterpene and steroid saponins isolated from medicinal plants such as Aesculus hippocastanum L., Hedera helix L. and Ruscus aculeatus L., which are claimed to be effective for the treatment/prevention of venous insufficiency.

Iodoantipyrine (Arthripur) is a commonly-used indicator and is used to evaluate in rats by measuring torcular venous efflux after systemic injection of the indicator under conditions of normal and high CBF.

Betrixaban maleate is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa.

Thrombin inhibitor 5 (compound 385) is a thrombin inhibitor with IC50 values ranging from 0.1 μM to 1 μM, suitable for venous thromboembolism research[1].

Inogatran is a synthetic thrombin inhibitor, developed for the possible treatment and prophylaxis of venous and arterial thrombotic diseases.

Midodrine is converted to its active metabolite, desglymidodrine by deglycination reaction. Desglymidodrine selectively binds to and activates alpha-1-adrenergic receptors of the arteriolar and venous vasculature. This causes smooth muscle contraction and leads to an elevation of blood pressure. Desglymidodrine diffuses poorly across the blood-brain barrier and is therefore not associated with effects on the central nervous system. Midodrine hydrochloride (Pro-Amatine) is the hydrochloride salt form of midodrine, a direct-acting prodrug and sympathomimetic agent with antihypotensive properties.

Darexaban (Tanexaban, YM-150) is a direct inhibitor of Factor Xa.Darexaban and Darexaban glucuronide selectively and competitively inhibit FXA and inhibit prothrombin activity at the site of blood clot (thrombus) formation. This leads to a reduction in blood clot formation in a dose-dependent manner. Reducing clotting will reduce blockages in blood flow, which may reduce the risk of myocardial infarction, unstable angina, venous thrombosis, and ischemic stroke.

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

Escin Ie, a derivative of Aescine found in Aesculi Semen extract, is characterized by its anti-inflammatory properties and potential therapeutic applications in treating chronic venous insufficiency and edema.

Betrixaban (PRT054021) is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa [1]. It was selected among all lead compounds due to its low hERG channel affinity while sustaining its factor Xa inhibition capacity [3]. Betrixaban, now developed by Portola Pharmaceuticals Inc., is prescribed as a venous thromboembolism (VTE) prophylactic for adult patients with moderate to severe restricted motility or with other risks for VTE [2]. VTE can be manifested as deep vein thrombosis or pulmonary embolism and it is a leading cause of preventable death in hospitalized patients [4].

Desirudin (CGP 39393) is a thrombin inhibitor that prevents thrombosis and venous stasis thrombosis. It is utilized for studying thrombocytopenia or platelet dysfunction associated with thrombocytopenia.

Aspirin calcium is the prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5)