edema

TGN-020 is an inhibitor of Aquaporin 4 (AQP4, IC50: 3.1 μM), the most abundant water channel in the brain.

Cinanserin hydrochloride (SQ 10643), a high-affinity antagonist of the 5-HT2 receptor (Ki: 41 nM), is also a 3C-like protease inhibitor of severe acute respiratory syndrome coronavirus.

SC-58125 is a selective cyclooxygenase 2 (COX-2) inhibitor, with an IC50 of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo, and it also can inhibit edema at the inflammatory site and is analgesic

GSK-872 (GSK2399872A) is an effective and specific RIP3 kinase inhibitor. It binds RIP3 kinase domain with high affinity (IC50: 1.8 nM) and inhibits kinase activity (IC50: 1.3 nM).

Methyclothiazide (Aquatensen) is a substituted benzothiadiazide, used to treat high blood pressure and fluid retention caused by various conditions including heart disease.

3-demethylcolchicine is a natural product isolated from Gloriosa superba.Inhibitory effect on the polymerization of purified bovine brain tubulin.

Furosemide is a potent NKCC2 (Na-K-2Cl symporter) inhibitor, used for edema and chronic renal insufficiency.

Ketorolac (Acuvail) is a non-steroidal anti-inflammatory drug (NSAID) in the family of heterocyclic acetic acid derivatives. It acts by inhibiting the bodily synthesis of prostaglandins.

Taraxasterol acetate has anti-inflammatory activity in bino rats against carrageenan, formaldehyde and adjuvant induced inflammations. Taraxasterol acetate also displays potential antibacterial activities.

LSP-249 is a plasma kallikrein inhibitor under the study for angioedema, with an EC50 less than 100 nM in cell.

Avoralstat (BCX4161) is an oral plasma kallikrein (PKK) inhibitor. Which is used for the treatment of hereditary angioedema.

Rho-Kinase-IN-1 is an inhibitor of ROCK with Kis of 30.5 nM and 3.9 nM for ROCK1 and ROCK2, respectively. Rho-Kinase-IN-1 can be used in studies about excessive cell proliferation, remodeling, edema and inflammation diseases.

KP136 (AL136) is an orally active anti-allergic compound that inhibits histamine release and is used in studies of asthma and allergic edema.

Furaprofen is an orally available, selective and potent HCV inhibitor with anti-inflammatory activity, inhibits carrageenan-induced paw edema in rats and inhibits cotton pellet-induced granulomas in rats at higher doses.

Dixyrazine (UCB 3412)has a transient antihypertensive effect, prevents cerebral edema induced by injections of ichthyosperm sulfate, and may be used in the study of neurologically related disorders.

AA 2379 is an orally available antirheumatic agent with anti-inflammatory and antipyretic activity that dose-dependently inhibits complement-mediated yeast glycan-induced paw edema in rats and yeast glycan-activated serum-induced peritonitis in mice.

Safotibant (LF-22-0542) is a bradykinin B1 receptor antagonist with anti-inflammatory and analgesic activity for the topical treatment of diabetic macular edema.

Aligeron, a non-selective prostaglandin (PG) antagonist, inhibits PGF2α- and PGE2-induced blood pressure decreases in cats and can prevent PGF2α-induced diarrhea in mice and PGE2-induced paw edema in rats. Additionally, Aligeron is recognized for its antioxidant-protective effect against vascular complications.

Kamuvudine-8 (K8) is a zidovudine (AZT) derivative that can be used to study diabetic macular edema.

Zileuton (A 64077) is a synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma.

Diammonium Glycyrrhizinate (Glycyrrhizin) , an extensively used anti-inflammatory agent, is isolated from the licorice root. It is metabolized to glycyrrhetinic acid, which inhibits 11-β-hydroxysteroid dehydrogenase and other enzymes involved in the metabolism of corticosteroids. Therefore, glycyrrhizic acid, the main and sweet component of licorice, has been studied for its ability to cause hypermineralocorticoidism with potassium loss and sodium retention, edema, increased blood pressure, as well as inhibited the renin-angiotensin-aldosterone system.

Benzthiazide (Lemazide) is used in the therapy of edema and hypertension. Like other thiazides, benzthiazide accelerates water loss from the body (diuretics). They inhibit Na+/Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

Dextran (Dextran 40) inhibits platelet aggregation and coagulation factors, can partially replace whole blood during transfusion, and is commonly used as a plasma volume expander; it can also be used in paw edema models.

Esculetin (Cichorigenin) is a coumarin derivative from various natural plant products with various biological and pharmaceutical properties including anti-edema, anti-inflammatory and anti-tumour effects. It inhibits lipoxygenases (LOs).