arterial

Furegrelate sodium (U-63557A) is a selective thromboxane synthase inhibitor with oral activity. Furegrelate sodium(U-63557A) inhibits thromboxane A2 (TXA2) synthase in human platelet microsomes with an IC50 of 15 nM.

Macitentan (ACT-064992) is an endothelin receptor antagonist utilized in the treatment of pulmonary arterial hypertension (PAH).

NTP42 is an antagonist of thromboxane A2 (TXA2) receptor(IC50 of 3.278 nM)

Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.

Eprazinone dihydrochloride (NSC 317935) is a mucolytic with antitussive and mucolytic effect.

Seralutinib (GB002) is an inhibitor of inhaled PDGFRα and PDGFRβ. It is used in the study for pulmonary arterial hypertension.

Pulmonary arterial hypertension agent-1 (example 15), recognized as a click chemistry reagent in [1], includes an Alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with Azide group-containing molecules. This compound is utilized specifically for treating pulmonary arterial hypertension.

Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid extracted from the seeds of Crotalaria plants. It inhibits organic cation transporters OCT-1 and OCT-2, with IC50 values of 36.8 µM and 1.8 mM, respectively. Monocrotaline exhibits antitumor activity and shows certain cytotoxicity against liver cancer cells such as HepG2. It is also commonly used to induce pulmonary arterial hypertension models in rodents.

SY-LB-57 is a highly effective agonist of bone morphogenetic protein (BMP) receptor signaling, suitable for studies of conditions such as bone fractures and pulmonary arterial hypertension [1].

FUREGRELATE, a thromboxane A2 (TxA2) synthase inhibitor, blunts the development of pulmonary arterial hypertension in neonatal piglets.

TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6, which has the potential for the treatment of pulmonary arterial hypertension (PAH). TPN171 was proven to exert a longer lasting effect than sildenafil in animal models, providing a foundation for a once-daily oral administration for its clinical use.

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.

Elsibucol (AGI 1096) is a VCAM1 inhibitor for the study of organ transplant rejection.Elsibucol is a metabolically stable propanol derivative with antioxidant, anti-inflammatory and anti-proliferative properties. It lowers blood cholesterol levels and reduces oxidative stress and inflammatory responses in injured arteries, thereby inhibiting atherosclerosis and protecting endothelial healing after arterial injury.

Propanidid (Sombrevin) is a gamma-aminobutyric acid type A receptor (GABAA) agonist and a fast-acting intravenous anesthetic that lowers arterial blood pressure.

PCI-27483 is an activated coagulation factor VIIa inhibitor with antithrombotic effects in a baboon model of arterial thrombosis. It also inhibits the growth of BxPC3 xenografts by 42% and 85% at doses of 60 and 90 mg/kg, respectively.

Nebentan potassium (YM598) is an orally active and selective nonpeptide endothelin receptor (ETA receptor) antagonist.Nebentan potassium inhibits pulmonary arterial hypertension and may be useful in the study of neurologic and cardiovascular diseases.

Imitrodast is a small molecule thromboxane A2 synthase (TXA2 synthase) inhibitor for the treatment of immune system disorders, respiratory disorders, and cardiovascular diseases, and can be used in studies of arterial thrombosis, asthma, and coronary vasospasm.

Benzoquinamide hydrochloride (3-carbamoyl-N,N-diethyl-1,3,4,6,7,11b-hexahydro-9,11-dimethoxy-2H-benzo[a]quinolizin-2-yl acetate hydrochloride) is an antiemetic agent and increases intra-arterial pressure due to the increased peripheral vascular resistance.

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.

Nisoldipine (BAY-k 5552) is a dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent.

Etidronic acid (HEDP) is a diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.

Buflomedil hydrochloride (Fonzylane), a vasodilator, is used in therapy of claudication or the symptoms of the peripheral arterial disease.

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.

Sodium etidronate (Didronel) is a synthetic therapeutic diphosphonate analog of endogenous pyrophosphate. As a member of the family of drugs known as bisphosphonates, Sodium etidronate differs from endogenous pyrophosphate in its resistance to enzymatic hydrolysis. This agent adsorbs to hydroxyapatite cells and reduces the number of osteoclasts, thereby inhibiting abnormal bone resorption. Etidronate may also directly stimulate bone formation by osteoblasts.