Angiotensin II human is a vasoconstrictor that acts on the AT1 and the AT2 receptor.
AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice[1][2].
Amezinium metilsulfate has multiple mechanisms, including stimulation of alpha and beta-1 receptors and inhibition ofnoradrenaline and tyramine uptake. Target: alpha and beta-1 receptorsAmezinium metilsulfate is a sympathomimetic drug used for the treatment of low blood pressure. Cardiovascular effects of the new sympathomimetic Amezinium metilsulphate are investigated in 25 patients compared with a control group (n = 25). During spinal/epidural anaesthesia 5 mg amezinium is given i.v. if blood pressure dropped greater than 20 mmHg. from starting-point. A significant recovery of blood pressure (epidural anaesthesia: syst 21%, diast 9%; spinal anaesthesia: syst 13%, diast 6.6%) and a decrease in heart rate (6.8% resp. 4,5%) are thought due to peripheral vasoconstriction. Amezinium proves a stimulating drug for alpha- and beta 1-receptors by stabilising the systemic blood pressure in spinal/epidural anaesthesia.
Moxisylyte (hydrochloride) is (alpha 1-blocker) antagonist，it can vasodilates cerebral vessels without reducing blood pressure。It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. [1][2]
Lotusine is a pure alkaloid extracted from the green seed embryo of Nelumbo nucifera Gaertn. Lotusine shows effects on the action potentials in myocardium and slow inward current in cardiac Purkinje fibers[1].
MYLS22 is a first-in-class and selective optic atrophy 1 (OPA1) inhibitor. MYLS22 can target endothelial OPA1 to curtail tumor growth and inhibits angiogenesis by impinging on NFkB activity and on angiogenic gene expression[1].
D-Val-Leu-Lys-chloromethylketone is a polypeptide containing three amino acids. D-Val-Leu-Lys-chloromethylketone can act as an anticoagulant[1].
Ciglitazone is a potent and selective PPARγ agonist (EC50=3 μM). Ciglitazone inhibits proliferation and differentiation of th17 cells. Ciglitazone is a hypoglycemic agent orally active in the obese-hyperglycemic animal models. Ciglitazone induces apoptosis accompanied by activation of p38 MAPK and nuclear translocation of apoptosis inducing factor (AIF) in opossum kidney (OK) renal epithelial cells[1][2][3][4].
Rilmenidine phosphate, an antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate is also an alpha 2-adrenoceptor agonist. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is an inhibitor of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity[1]. Astaxanthin has potential in the treatment of various diseases, such as cancers and Parkinson’s disease, cardiovascular disease[2]. Due to its bright red colour, Astaxanthin could be used as a food colorant in animal feeds[3].
Aficamten (CK-274) is a novel cardiac myosin inhibitor with an IC50 of 1.4 μM. Aficamten can be used for the research of hypertrophic cardiomyopathy (HCM)[1].
N-Feruloylserotonin, an antioxidative component and bioactive serotonin derivative, from the Seed of Carthamus tinctorius L., ameliorates atherosclerosis and distensibility of the aortic wall in Kurosawa and Kusanagi-hypercholesterolemic (KHC) rabbits[1].
Pinusolidic acid is a platelet-activating factor (PAF) inhibitor with an IC50 of 23 μM[1].
Deoxypyridinoline is an endogenous metabolite present in Urine that can be used for the research of Heart Failure[1][2].
Drobuline hydrochloride is an anti-arrhythmic agent with cardiac depressant.
Z-FK-ck (Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone) is a potent and selective gingipain-K-specific inhibitor. Z-FK-ck prolongs plasma thrombin time (TT) in a dose- and time-dependent manner[1].
PI3KC2α-IN-1 is a potent PI3KC2α inhibitor (IC50: 95 nM). PI3KC2α-IN-1 interacts with the ATP-binding site of PI3KC2α. PI3KC2α-IN-1 can be used in the research of thrombosis, diabetes and cancers[1].
Dopropidil is a novel anti-anginal calcium ion modulating agent, possessing intracellular calcium antagonist activity and anti-ischemic effects in several predictive animal models.
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.IC50 value:Target: Factor Xa Otamixaban is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa. In vivo experiments have demonstrated that Otamixaban is highly efficacious in rodent, canine and porcine models of thrombosis. In addition, recent clinical findings indicate that Otamixaban is efficacious, safe and well tolerated in humans and therefore has considerable potential for the treatment of acute coronary syndrome. This review article chronicles the discovery and pre-clinical data surrounding the fXa inhibitor Otamixaban as well as the recent clinical findings in humans.
Bradykinin (1-5) is a major stable metabolite of Bradykinin, formed by the proteolytic action of angiotensin-converting enzyme (ACE).
Fesomersen is an antisense oligonucleotide designed to inhibit the production of Factor XI.
Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively [1].
Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes[1].
Arginyl-Glutamine is a dipeptide that can decrease VEGF levels and inhibit retinal neovascularization in a mouse model of oxygen-induced retinopathy[1].
Ozagrel hydrochloride (OKY-046 hydrochloride) is a thromboxane A2 (TXA2) synthase inhibitor. Ozagrel hydrochloride is an antiplatelet agent, which selectively inhibits human platelet aggregationwith an IC50 of 53.12 μM[1].
Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor, with a Ki value of 57 pM for [3H]PAF binding, at least 5-fold lower than that of unlabeled PAF itself. Foropafant potently inhibits PAF-induced aggregation of rabbit and human platelets[1].
Cleistanthin B (Diphyllin O-glucoside) is an orally active arylnaphthalene lignan lactone glycoside. Cleistanthin B exhibits anti-SARS-CoV-2 effects in Vero cells, with EC50 of 6.51 µM. Cleistanthin B also exhibits antitumor, diuretic and antihypertensive effects in vivo[1][2][3][4].
Batifiban, a cyclic peptide, is a platelet glycoprotein GPⅡb/Ⅲa antagonist, and inhibits platelet aggregation. Batifiban blocks circulating vitronectin binding to integrin ανβ3, Batifiban can be used for research of acute coronary syndromes[1].
Hirudin is a Thrombin inhibitor with blood anticoagulant property. Hirudin has potent anti-thrombotic, wound repair, anti-fibrosis, anti-tumor and anti-hyperuricemia effects. Hirudin also affects diabetic complications, cerebral hemorrhage, and others[1].
U-44069 is a stable prostaglandin (PG) H2 analogue and a potent vasoconstrictor. U-44069 induces Ca influx at preglomerular vessels[1].