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.

Carglumic Acid (Ureidoglutaric acid) is an orphan drug used to treat hyperammonemia in patients with N-acetyl glutamate synthase absence. This rare hereditary disease results in elevated blood levels of ammonia, which can eventually cross the blood-brain barrier and lead to neurologic problems, coma, cerebral edema, and death. Carglumic acid was approved by the U.S. FDA on 18 March 2010.

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.

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.

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

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).

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

N-Formyl-Met-Leu-Phe-Lys (fMLFK) is a peptide that acts as a potent and selective agonist of FPR1, with EC50s of 3.5 nM for FPR1, 6.7 μM for FPR2, and 0.88 μM for FPR2-D2817.32G. This chemotactic peptide binds specifically to receptors on leukocyte membranes and its uptake can contribute to the quantitative assessment of neutrophils in localized inflammatory processes, independent of associated edema formation or microcirculatory compromise.

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.

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.

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.

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).

Alnustone ((4E,6E)-1,7-Diphenyl-4,6-heptadien-3-one) exerts significant anti-inflammatory activity in the assay of carrageenin-induced hind paw edema in rats.

Piceatannol 3'-O-glucoside (Piceatannol 3-glycoside) increases pulmonary blood oxygen tension and decreases pulmonary interstitial edema, so it can protect lung injury.

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

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

Halobetasol propionate (BMY-30056) is the propionate salt form of halobetasol, a synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictor activities. Halobetasol, a topical steroid, diffuses across cell membranes to interact with cytoplasmic corticosteroid receptors located in both the dermal and intradermal cells, thereby activating gene expression of anti-inflammatory proteins mediated via corticosteroid receptor response element. Specifically, this agent induces phospholipase A2 inhibitory proteins, which inhibit the release of arachidonic acid, thereby inhibiting the biosynthesis of potent mediators of inflammation, such as prostaglandins and leukotrienes. As a result, halobetasol reduces edema, erythema, and pruritus through its cutaneous effects on vascular dilation and permeability.

1. Periplocin (Periplocoside) has anti-cancer effects on lung cancer cells, induces apoptosis and inhibits growth of cancer cells by the beta-catenin/Tcf signaling pathway. 2. Periplocin is used for treatment of rheumatoid arthritis, reinforcement of bones and tendons, palpitations or shortness of breath and lower extremity edema in traditional medicine.

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

Mercaptomerin sodium can be used to treat cardiac edema.

Ruboxistaurin mesylate monohydrate is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and GRAP pathways. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin inhibits retinal neovascularization via suppression of phosphorylation of ERK1/2 and Akt.

Methazolamide-d6 is intended for use as an internal standard for the quantification of methazolamide by GC- or LC-MS. Methazolamide is a carbonic anhydrase inhibitor. It reduces intraocular pressure and cerebrospinal fluid flow in a rat model of glaucoma. Methazolamide reduces electroshock-induced seizures in rats with an ED50 value of 19.2 mg/kg. It also inhibits production of reactive oxygen species (ROS) in a primary cortical neuron (PCN) cellular model of subarachnoid hemorrhage (SAH) and reduces cerebral edema in a mouse model of SAH.3 Methazolamide is larvicidal, with a 50% larvicidal concentration (LC50) value of 724 ppm, but has no activity when administered in the diet to adult A. aegypti. Formulations containing methazolamide have been used in the treatment of glaucoma.

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.

SDZ 224-015 is an orally active inhibitor of interleukin-1β (IL-1β) converting enzyme and caspase-1, exhibiting anti-COVID-19 and anti-inflammatory activity, and reducing carrageenan gum-induced paw edema in rats.

Yonkenafil (Tunodafil), a novel phosphodiesterase 5 (PDE5) inhibitor, effectively reduces cerebral infarction, neurological deficits, edema, and neuronal damage in the infarcted area, potentially enhancing cognitive function through neurogenesis modulation and offering therapeutic effects on Alzheimer's disease.

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.

Escin IIB has positive effects on acute inflammation in animals, it can inhibit the induced by serotonin in rats, the hind paw edema induced by carrageenin, and the scratching behavior induced by compound 48/80 in mice.

Nogotrienone is an anabolic steroid with fertility and contraceptive activity that has been studied as a therapeutic agent for hereditary angioneurotic edema.

Methylene Blue (Basic Blue 9) hydrate functions as an inhibitor of guanylyl cyclase (sGC), monoamine oxidase A (MAO-A), and NO synthase (NOS). This compound, known for its vasopressor activity, is widely utilized as a dye in various medical procedures. It operates via the nitric oxide synthase/guanylate cyclase signaling pathway to diminish prepulse inhibition and possesses the capacity to cross the blood-brain barrier. Methylene Blue hydrate acts as a REDOX cycling compound and inhibits Tau protein aggregation. Moreover, it is effective in reducing cerebral edema, damping microglial activation, and alleviating neuroinflammation, demonstrating its multifaceted therapeutic potential [1] [2] [3].

Polythiazide (NSC-108161, P-2525) is used to treat fluid retention (edema) caused by a variety of causes, including congestive heart failure, severe liver disease (cirrhosis), kidney disease, or steroid or hormonal medication.

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

16 alpha-Hydroxytrametenolic acid can inhibit 12-O-tetradecanoylphorbol 13-acetate (TAP)-induced mouse ear edema.

Plasma kallikrein-IN-3, a potent inhibitor ( IC 50 : 0.15 μM) of plasma kallikrein, finds application in research related to hereditary angioedema, diabetic macular edema, and diabetic retinopathy [1].

Arjunglucoside I has anti-inflammatory activity, it exhibits significant activity against carrageenan-induced paw edema in rat. It also shows antiproliferative activity against the A2780 human ovarian cancer cell line with an IC(50) value of 1.2 microM.

Kopsininic acid, a natural product isolated from Kopsia hainanensis, has potential applications in researching rheumatoid arthritis, pharyngitis, tonsillitis, and edema [1].

Ozolinone is an active metabolite of etozoline which acts as a loop diuretic --- a diuretic that acts at the ascending limb of the loop of Henle in the kidney. Loop diuretics are primarily used in medicine to treat hypertension and edema often due to cong

VUF-10214 is an H4 receptor-ligand. VUF-10214 has significant anti-inflammatory properties in the carrageenan-induced paw edema model in vivo studies in the rat reveal.

Betulonaldehyde is a pentacyclic triterpenoid and derivative of the cholesterol biosynthesis inhibitor betulin that has been found in Betula. It is active against P. falciparum (IC50 = 3.36 µg/ml) and cytotoxic to NCI H187 lung cancer cells and non-cancerous Vero cells (IC50s = 19.23 and 17.09 µg/ml, respectively). Topical application of betulonaldehyde (1 mg/ear) reduces ear edema induced by phorbol 12-myristate 13-acetate (TPA; Item No. 10008014) in mice. It has also been used a precursor in the semisynthesis of C-2 and C-28 betulonic aldehyde derivatives.

JNJ-26076713, an orally active alpha V integrin antagonist, represents a potential therapeutic candidate for the treatment of macular edema, age-related macular degeneration, and proliferative diabetic retinopathy.

Luffariellolide is an inhibitor of human synovial fluid phospholipase A2 (HSF-PLA2) with an IC50 of 5 μM and effectively inhibits PMA-induced ear edema (ED50 = 50 μg ear) [1].

Benzydamine is a benzyl-indazole having analgesic, antipyretic, and anti-inflammatory effects. Benzydamine is used to reduce post-surgical and post-traumatic pain and edema and to promote healing.

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.

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.

Acetazolamide sodium (OT-302 sodium) is a potent carbonic anhydrase (CA)IX inhibitor with diuretic, antigonococcal, and antihypertensive activity and may be used for indications such as epilepsy, glaucoma, edema, and altitude sickness.

Ketorolac (RS37619) hemicalcium is a nonselective COX inhibitor with IC50 values of 20 nM for COX-1 and 120 nM for COX-2. This non-steroidal anti-inflammatory drug (NSAID) is used as a 0.5% ophthalmic solution for researching allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Additionally, it is a DDX3 inhibitor applicable in cancer research [1] [4].

Thielavin B, produced by Thielavia terricola, functions as an inhibitor of prostaglandin biosynthesis, specifically targeting the synthesis of prostaglandin E2 from the endoperoxide. It demonstrates significant efficacy in reducing carrageenan-induced edema in rats when administered intravenously.

Lamiide has anti-inflammatory activity in carrageenin-induced paw edema test. It shows lipid peroxidation inhibition on rat-brain phospholipid peroxidation.

Kaji-ichigoside F1 shows antiinflammatory/antinociceptive action in acetic acid-induced writhing and hot plate testing and in a carrageenan-induced paw edema model in mice and rats. Kaji-ichigoside F1 exhibits in vivo hepatoprotective effects, it inhibite

Peptide 401 is an antimicrobial peptide (AMP) derived from the venom of bees and wasps. Peptide 401 induces mast cell degranulation, activating histamine release from peritoneal mast cells. Additionally, peptide 401 exhibits some anti-inflammatory activit