hemorrhage

3-hydroxy-3-phenylpentanamide is a chiral compound belonging to the class of beta-hydroxyamides. In neurology, it has been shown to have neuroprotective effects against ischemic brain injury and cerebral hemorrhage. In psychiatry, it has been studied as a potential treatment for anxiety, depression and addiction. In oncology, it has been shown to have antitumor activity by inducing apoptosis and inhibiting tumor growth.

CM-352 is a metalloproteinase inhibitor that reduces brain damage and improves functional recovery in rat models of cerebral hemorrhage.

LJP-1586 HCl, a highly selective inhibitor of vascular adhesion protein-1 (VAP-1), exhibits antiinflammation effect by reducing adhesion molecule expression and immune cell infiltration after intracerebral hemorrhage (ICH).

INT-777 (S-EMCA) is a potent TGR5 agonist with an EC50 of 0.82 μM. INT-777 (S-EMCA) inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3 cAMP PKA signaling pathway after subarachnoid hemorrhage in rats.

HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt/β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

Carbetocin is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth.

ML351 is a potent and selective inhibitor of human 15-lipoxygenase-1 (15 LOX)(IC50: 200 nM).

Cytosporone B (Dothiorelone G) is a naturally occurring agonist for the nuclear receptor Nur77 (IC50 = 0.278 nM). Activation of Nur77 with cytosporone B induces the expression of Nur77-dependent genes, including the gene for Nur77 itself. Signaling through Nur77 induces apoptosis in cancer cells and retards xenograft tumor growth. It also induces genes related to gluconeogenesis and decreases atherosclerosis progression in mice fed a high fat and high cholesterol diet. Cytosporone B is brain penetrant and aggravates early brain injury in rats when given (13 mg/kg intraperitoneally) after experimentally-induced subarachnoid hemorrhage. Cytosporone B also has antibacterial properties.

Desmethylanethol trithione (ADT-OH) is a derivative of anethole dithiolethione (ADT) and synthetic hydrogen sulfide (H2S) donor. In the in vitro glucose-oxygen deprivation (OGD) model, Desmethylanethol trithione markedly attenuated tPA-enhanced Akt activation and VEGF expression in brain microvascular endothelial cells. Finally, Desmethylanethol trithione improved functional outcomes in mice subjected to MCAO and tPA infusion. H2S donors reduced tPA-induced cerebral hemorrhage by possibly inhibiting the Akt-VEGF-MMP9 cascade. Administration of H2S donors has potential as a novel modality to improve the safety of tPA following the stroke.

ESI-05 (NSC-116966) is a specific EPAC2 (exchange protein directly activated by cAMP 2) antagonist (IC50: 0.4 μM). ESI-05 inhibits cAMP-mediated activation of EPAC2, as well as EAPC2, mediated Rap1 activation.

Tirilazad, a nonglucocorticoid 21-aminosteroid, serves to inhibit lipid peroxidation. It mitigates the effects of trauma-induced brain or spinal cord injury, as well as damage resulting from stroke, ischemia, and reperfusion injury. Additionally, Tirilazad exhibits antiviral properties against nCoV and offers neuroprotection in cases of ischemic stroke. It is also utilized in subarachnoid hemorrhage research [1] [2] [3].

Potent and selective melanocortin 4 (MC4) receptor agonist (IC50 values are 0.58 and 55 nM for human MC4 and MC3 receptors respectively). Produces a rapid and dose dependent restoration of cardiovascular and respiratory function in hemorrhage-shocked rats

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.

Cimetidine sulfoxide (Cimetidine sulphoxide), a metabolite of Cimetidine, is a histamine H2-receptor antagonist with potential applications in treating peptic ulcer disease and upper gastrointestinal hemorrhage [1].

Fursultiamine (Alinamin F) is a disulfide derivative of thiamine, or an allithiamine. It has potential uses in the treatment of vitamin B1 deficiency.

6-Methylnicotinamide is a derivative of nicotinamide, an endogenous metabolite. 6-Methylnicotinamide is used to make co-crystals/salts. In the acute phase of cerebral hemorrhage (ICH), a sudden increase in 6-Methylnicotinamide exacerbates neurological damage.6-Methylnicotinamide can be used to make co-crystals/salts.6-Methylnicotinamide can be used to make co-crystals/salts.

piCRAC-1 is a powerful inhibitor of the photoinducible Ca2+ release-activated Ca2+ (CRAC) channel. It effectively alleviates thrombocytopenia and hemorrhage [1].

Sambutoxin, a new mycotoxin produced by toxic Fusarium isolates obtained from rotted potato tubers, it can cause toxic effects in rats, including body weight loss, feed refusal, hemorrhage in the stomach and intestines, and, finally, death when rats were

Carboprost (15(S)-15-Methyl Prostaglandin F2α) is a synthetic analogue of PGF2α with oxytocic properties, commonly used to restore uterine tone.

Carbetocin acetate is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth.

Tat-QFNP12 is a peptide that combines a transcriptional transactivator (Tat) transmembrane domain with an inhibitor targeting the interaction between N-Myc downstream regulated gene 2 (NDRG2) and protein phosphatase Mg2+/Mn2+ dependent 1A (PPM1A). This compound effectively mitigates blood-brain barrier endothelial tight junction disruption caused by elevated levels of matrix metalloproteinase-9 (MMP-9), alleviates cerebral edema, and promotes spontaneous activity along with symmetric limb movement in a mouse model of subarachnoid hemorrhage induced by endovascular puncture. These benefits are observed at a dosage of 20 mg/kg.

Carboprost tromethamine, a synthetic 15-methyl analogue of prostaglandin F2α, effectively promotes uterine contractions and significantly reduces bleeding during and post-delivery.

Edaravone, a novel and potent free radical scavenger, effectively prevents MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator. Its deuterium-labeled variant, Edaravone D5, retains the original compound's attributes while offering isotopic labeling benefits.