U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 15901 - 15910 of 15963 results

Status:
Withdrawn

Class (Stereo):
CHEMICAL (RACEMIC)



Pronetalol (Pronethalol) is a nonselective beta-adrenoceptor antagonist that is structurally related to propranolol. Pronethalol displays a ∼125–150-fold lower affinity (140–830 nM) for beta-adrenoceptors than propranolol (1.1–5.7 nM). Pronethalol was the first beta-adrenoceptor antagonist used for the treatment of coronary heart disease and cardiac arrhythmias. Pronethalol is a cationic-amphiphilic agent that exhibits membrane-stabilizing effects that are unrelated to beta-adrenoceptor blockade. Pronetalol itself never came into widespread clinical use; it was found to produce thymic tumors in mice, and was discarded in favor of a similar, safer compound, ICI 45,520.
Status:
Withdrawn
Source:
Ganglioside GM1 [Germany]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ganglioside GM1 is a monosialo-glycosphingolipid belonging to the gangliotetrahexosyl series that abundant in neurons of all animal species and plays important roles in many cell physiological processes, including differentiation, memory control, cell signaling, neuronal protection, neuronal recovery, and apoptosis. Ganglioside GM1 in neurons helps to transfer information from the exterior to the interior of the cell, through specific recognition and binding of biologically active molecules (membrane receptors and ion channels), and has specific functions in nerve conduction and/or synaptic transmission. The mechanisms underlying the effects of Ganglioside GM1 remain unclear in many cases, but it appears that these effects are often due to specific interactions between Ganglioside GM1 and proteins involved in signaling processes, within Ganglioside GM1-enriched lipid rafts in the plasma membrane. Ganglioside GM1 is a major component of total ganglioside mixtures from mammalian brains, from which it can be extracted and purified in large amounts. Ganglioside GM1 was widely used in the past as a therapeutic drug for a wide variety of neurological disorders. Further studies have shown that Ganglioside GM1 has immunogenic properties and led to the production of antibodies that promoted peripheral neuropathies such as Guillain–Barré syndrome.
Status:
Withdrawn

Class (Stereo):
CHEMICAL (RACEMIC)


Mebanazine is an inhibitor of monoamine oxidase. It was introduced in the 1960s for the treatment of depression and was marketed under trade name Actomol. The drug was withdrawn from the market due to hepatotoxicity. In addition to its antidepressant effect, the drug was found to possess an anorexic action and in animal models, it potentiated the hypoglycemic response to insulin and delayed the recovery of blood glucose levels to normal.
Status:
Withdrawn
Source:
Diethylaminoethoxyhexestrol [Japan]
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Diethylaminoethoxyhexestrol is a coronary dilating agent, approved for the treatment of angina in 1958 and marketed under tradename Coralgil. Diethylaminoethoxyhexestrol was withdrawn from the market because of drug-related phospholipidosis in liver, spleen and other tissues. Studies indicate that lipidosis is caused by the accumulation of the drug in lysosomes and inhibition of phospholipase A.
Status:

Class (Stereo):
CHEMICAL (RACEMIC)

Sch 39304 is a new broad-spectrum orally active triazole antifungal agent that is active, orally and topically, against a broad range of fungal pathogens, including superficial Trichophyton mentagrophytes and vaginal Candida albicans infections. The mechanism of action of SCH-39304 appears similar to those of ketoconazole and fluconazole, involving inhibition of cell membrane ergosterol synthesis. SCH-39304 has two asymmetrical carbon atoms, and the formulation used in clinical trials has been a racemic mixture of two enantiomers, active SCH-42427 (RR (+)-) and inactive SCH-424264 (SS (–)-). Unfortunately, hepatocarcinomas associated with the use of SCH-39304 in animals have sharply restricted the development and use of this agent.
Cefprozil is a 2nd generation cephalosporin that is FDA approved for the treatment of mild to moderate infections of upper respiratory tract, lower respiratory tract, and uncomplicated skin and skin-structure infections. Cefprozil, like the penicillins, is a beta-lactam antibiotic. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Common adverse reactions include diarrhea, nausea, vomiting, dizziness, abdominal pain and vaginitis. Nephrotoxicity has been reported following concomitant administration of aminoglycoside antibiotics and cephalosporin antibiotics. Concomitant administration of probenecid doubled the AUC for cefprozil.
mixture
Status:
Investigational
Source:
NCT04325035: Phase 2 Interventional Completed Cardiogenic Shock
(2020)
Source URL:

Class:
MIXTURE



Istaroxime is a novel intravenous agent with luso-inotropic properties that acts by inhibition of Na( )/K( ) adenosine triphosphatase and stimulation of sarco/ endoplasmic reticulum calcium ATPase isoform 2. It is significantly decreased left ventricular end-diastolic pressure, pulmonary capillary wedge pressure, heart rate and increased systolic blood pressure and cardiac index with no change in neurohormones, renal function or troponin I. Istaroxime has successfully concluded phase II clinical trials in cardiac failure patients. Istaroxime induced apoptosis, affected the key proliferative and apoptotic mediators c-Myc and caspase-3 and modified actin cytoskeleton dynamics and RhoA activity in prostate cancer cells – this provides novel insights into the anti-cancer properties of istaroxime further supporting the development of this agent as a novel anti-cancer drug candidate.
mixture
Status:
US Approved Allergenic Extract (1994)

Class:
MIXTURE

alpha-Amyl cinnamaldehyde is a pale yellow liquid fragrance material with a floral smell used in allergenic testing.

Showing 15901 - 15910 of 15963 results