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

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Showing 13871 - 13880 of 14117 results

Alpha-ketoglutarate (AKG), an endogenous intermediary metabolite in the Krebs cycle, is a molecule involved in multiple metabolic and cellular pathways. As an intermediate of the tricarboxylic acid cycle, AKG is essential for the oxidation of fatty acids, amino acids, and glucose. Extracellular AKG is a significant source of energy for cells of the gastrointestinal tract. As a precursor for the synthesis of glutamate and glutamine in multiple tissues (including liver, skeletal muscle, heart, brain, and white adipose tissue), AKG bridges carbohydrate and nitrogen metabolism for both conservation of amino acids and ammonia detoxification. Additionally, emerging evidence shows that AKG is a regulator of gene expression and cell signaling pathways (including the mammalian target of rapamycin and AMPactivated protein kinase). Thus, AKG is an attractive dietary supplement in animal and human nutrition to improve cellular energy status, immunity, and health.AKG can decrease protein catabolism and increase protein synthesis to enhance bone tissue formation in the skeletal muscles and can be used in clinical applications. In addition to these health benefits, a recent study has shown that AKG can extend the lifespan of adult Caenorhabditis elegans by inhibiting ATP synthase and TOR. Orally, AKG is used for kidney disease, gastrointestinal disorders, bacterial overgrowth, intestinal toxemia, liver dysfunction, and chronic candidiasis. It is also used for improving peak athletic performance, improving amino acid metabolism in hemodialysis patients, and cataracts. Intravenously, AKG is used for preventing ischemic injury during heart surgery, improving renal blood flow after heart surgery, and preventing muscle protein depletion after surgery or trauma.
Status:
Possibly Marketed Outside US
Source:
NCT01091337: Phase 4 Interventional Completed Asthma
(2006)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Procaterol is a beta2-adrenoreceptor agonist. It is a bronchodilator that may be administered orally or by aerosol inhalation for the treatment of dyspnea caused by bronchial asthma, chronic bronchitis, and pulmonary emphysema. The drug is not approved in the USA, but is available in Japan, Indonesia, and other countries worldwide.
Status:
Possibly Marketed Outside US
Source:
VASCULAT by Boehringer Ingelheim
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Bamethan (butyl-sympatol or vasculat) is an adrenaline derivative developed by C. H. Boehringer Sohn. Bamethan shows a depressor action on peripheral blood vessels as a result of the peripheral vasodilating action caused by stimulation of adrenergic beta-receptor. Bamethan has been used abroad in the treatment of certain peripheral vascular and circulatory disturbances, such as vasospastic conditions, arteriosclerotic peripheral vascular disease, Raynaud's syndrome, occlusive vascular disease of the legs, the post-thrombotic syndrome, degenerative muscular disorders, and other conditions involving peripheral vascular insuffciency.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Azacosterol (Ornitrol, 20,25-diazacholesterol dihydrochloride, SC 12937) is a cholesterol-lowering drug (hypocholesteremic) which was marketed previously but has since been discontinued. Azacosterol is a sterol derivative of cholesterol with two nitrogen atoms replacing two carbon atoms that acts as a hypocholesteremic agent by blocking delta-24-reductase. Azacosterol has the unintended side effect of causing myotonia. It is an avian contraceptive compound, which reduces fertility by inhibiting cholesterol synthesis. Azacosterol is also useful in the control of rodent populations.
Status:
Possibly Marketed Outside US
Source:
NCT02380053: Phase 4 Interventional Completed Chronic Obstructive Pulmonary Disease
(2016)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Celiprolol is beta blocker, used to treat high blood pressure. Celiprolol is a selective β1 receptor antagonist, β2 receptor partial agonist. Celiprolol is not approved by the FDA, but is available worldwide under brand names Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm. It is used to treat mild to moderate hypertension and angina prectoris. In 2010 celiprolol has demonstrated positive results in the prevention of vascular complications of Ehlers-Danlos syndrome. Celiprolol has fewer CNS-related side effects than other beta blockers presumably because of limited penetration through blood-brain barrier because of its solubility.
Status:
Possibly Marketed Outside US
Source:
NCT01263002: Phase 4 Interventional Completed Hepatitis B Associated Hepatocellular Carcinoma
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Clevudine (also known as L-FMAU) is a nucleos(t)ide reverse transcriptase inhibitor, which inhibits the DNA synthesis activity of the hepatitis B virus polymerase. The drug was approved in Korea and Philippines and is being marketed under the names Levovir and Revovir. The drug is indicated in patients with chronic hepatitis B virus infection. Upon administration, clevudine is metabolized to the active metabolite, clevudine triphosphate, which is responsible for the inhibition of viral polymerase.
Status:
Possibly Marketed Outside US
Source:
NCT00199004: Phase 4 Interventional Completed Adult Acute Lymphocytic Leukemia
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Vindesine (desacetyl vinblastine amide sulfate) is a synthetic derivative of vinblastine. Vindesine acts by causing the arrest of cells in metaphase mitosis through its inhibition tubulin mitotic funcitoning. Vindesine is an anti-neoplastic drug for intravenous use which can be used alone or in combination with other oncolytic drugs. Information available at present suggests that Eldisine as a single agent may be useful for the treatment of: acute lymphoblastic leukaemia of childhood resistant to other drugs; blastic crises of chronic myeloid leukaemia; malignant melanoma unresponsive to other forms of therapy; advanced carcinoma of the breast, unresponsive to appropriate endocrine surgery and/or hormonal therapy. Adverse effects associated with the use of vindesine include cellulitis and phlebitis, gastrointestinal bleeding, chills, and fever. It may increase the neuropathy associated with Charcot-Marie-Tooth syndrome. Vindesine may interact with mitomycin-C (brand name Mutamycin), causing acute bronchospasm within minutes or hours following administration. Phenytoin (brand name Dilantin) may also interact with vindesine, leading to decreased serum levels of phenytoin.
Cefsulodin is a third-generation of cephalosporin antibiotic with a narrow spectrum of activity. It has a specific activity against Pseudomonas aeruginosa. Cefsulodin’s targets are bacterial penicillin binding proteins. Drug is indicated for the treatment of infections of lower respiratory tract, skin and skin structures, urinary tract, bone and joint; treatment of gynecological infections; treatment of intra-abdominal infections; treatment of septicemia and CNS infections including meningitis caused by susceptible strains of specific microorganisms. Cefsulodin appears to be well tolerated and relatively free of any significant toxicity except for nausea and vomiting.
Status:
Possibly Marketed Outside US
Source:
Japan:Etilefrine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Etilefrine is a cardiac stimulant used as an antihypotensive. Intravenous infusion of this compound increases cardiac output, stroke volume, venous return and blood pressure in man and experimental animals, suggesting stimulation of both α and β adrenergic receptors. However, in vitro studies indicate that etilefrine has a much higher affinity for β1 (cardiac) than for β2 adrenoreceptors. Intravenous etilefrine increases the pulse rate, cardiac output, stroke volume, central venous pressure and mean arterial pressure of healthy individuals. Marked falls in pulse rate, cardiac output, stroke volume and peripheral bloodflow, accompanied by rises in mean arterial pressure, occur when etilefrine is infused after administration of intravenous propranolol 2,5 mg. These findings indicate that etilefrine has both β1 and α1 adrenergic effects in man. The French Health Products Agency concluded that etilefrine and heptaminol have an unfavourable harm-benefit balance, and also placed restrictions on the use of midodrine.
Status:
Possibly Marketed Outside US
Source:
JAMA Netw Open. May 2024;7(5):e248661.: Phase 4 Human clinical trial Completed Vaginosis, Bacterial
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dequalinium is a quaternary ammonium cation commonly available as the dichloride salt. Dequalinium chloride has an antiseptic effect against a wide range of bacteria, yeasts, and some fungi and viruses. It kills the micro-organisms associated with various mild infections of the mouth and throat. Also, Dequalinium chloride is active against the bacteria which cause bacterial vaginosis. Dequalinium Chloride (DECA) is a PKC inhibitor and high-affinity blocker CNGA1 channel, and nearly as effective on heteromeric CNGA1+CNGB1 channels. Common side effects are: vaginal discharge; vaginal itching or vaginal burning; vaginal yeast infection (thrush); tender tongue.

Showing 13871 - 13880 of 14117 results