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

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Showing 11771 - 11780 of 13362 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Veradoline is an analgesic agent.
Status:
Possibly Marketed Outside US
Source:
Canada:PENICILLIN G BENZATHINE
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Mitoguazone is a guanylhydrazone derivative with potential antineoplastic activity. Mitoguazone inhibits S-adenosyl-L-methionine decarboxylase (SAMD), an enzyme involved in the synthesis of polyamines, resulting in a decreased proliferation of tumor cells, antimitochondrial effects, and p53-independent apoptosis. In the 1960s the drug was investigated in clinical trials. Despite the responses in acute leukemia, chronic myelogenous leukemia, lymphoma, multiple myeloma, head and neck cancer, esophageal cancer and other types of cancer, the development of the drug was discontinued because of marked myelosuppression and mucositis. Using a weekly schedule of administration, mitoguazone had minimal toxicity and showed limited activity in patients with lymphoma, esophageal cancer, prostate cancer, and other types of tumors.
Levormeloxifene (INN) is an experimental selective estrogen receptor modulator (SERM) that was being developed as an alternative to estrogen replacement therapy for the treatment and prevention of postmenopausal bone loss. Levormeloxifene is the levorotatory enantiomer of non-hormonal, non-steroidal oral contraceptive -- ormeloxifene (trade names Novex-DS, Centron, and Sevista). The development of Levormeloxifene was stopped because of a high incidence of gynecologic adverse events during clinical trials.
Status:
Possibly Marketed Outside US
Source:
NCT03237182: Phase 4 Interventional Terminated Tuberculosis, Multidrug-Resistant
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Protionamide is a thioamide derivative with antitubercular activity, usually involving to treat MDR TB and leprosy. It has the same active substances and cross-resistance with ethionamide. Prothionamide is part of a group of drugs thioamides. The side effects of prothionamide are similar to ethionamide. Prothionamide is most commonly associated with nausea and vomiting. It may cause depression and hallucinations. Rarely, prothionamide will cause jaundice, menstrual disturbances and peripheral neuropathy. Prothionamide has received approval in Germany for the treatment of TB and drug resistant TB. While prothionamide is widely used to treat MDR TB, there is little published evidence demonstrating safety and efficacy. Protionamide forms a covalent adduct with bacterial nicotinamide adenine dinucleotide (NAD), PTH-NAD, which competitively inhibits 2-trans-enoyl-ACP reductase (inhA), an enzyme essential for mycolic acid synthesis. This results in increased cell wall permeability and decreased resistance against cell injury eventually leading to cell lysis. Mycolic acids, long-chain fatty acids, are essential mycobacterial cell wall components and play a key role in resistance to cell injury and mycobacterial virulence.
Status:
Possibly Marketed Outside US
Source:
NCT03120299: Phase 4 Interventional Completed Type 2 Diabetes Mellitus
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dihomo-gamma-linolenic acid (DGLA) is an n-6 polyunsaturated fatty acid that is mainly metabolized to an anti-inflammatory eicosanoid, prostaglandin (PG) E1, via the cyclooxygenase (COX) pathway. DGLA exists widely in the human body and daily animal-source foods. Concentrations of DGLA in the serum of atopic dermatitis patients are lower than those in healthy volunteers. DGLA suppressed clinical severity of skin lesions dose-dependently, with an increase in DGLA contents in phospholipids of skin, spleen, and plasma. Discontinuation of DGLA administration resulted in the onset of dermatitis and a decrease in DGLA contents in skin, spleen, and plasma. These findings indicate that oral administration of DGLA effectively prevents the development of atopic dermatitis in NC/Nga mice. DGLA may have an anti-atherosclerotic effect in apoE-deficient mice via PGE1 formation. As dihomo-γ-linolenic acid and arachidonic acid compete for processing by these oxidation enzymes, introduction of dihomo-γ-linolenic acid to platelets is correlated to suppression of arachidonic acid metabolites and promotion of dihomo-γ-linolenic acid metabolites such as PGE1, which produces an antithrombotic effect.
Status:
Possibly Marketed Outside US
Source:
NCT02237937: Phase 4 Interventional Unknown status Major Depression
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Amitriptylinoxide (amitriptyline N-oxide, Amioxid, Ambivalon) is a tricyclic antidepressant, which was introduced in Europe in the 1970s for the treatment of depression. Amitriptylinoxide (AMINO) produces similar effects to the drug Amitriptyline (AMI), which makes sense because it is a metabolite of Amitriptyline. AMINO and AMI potentiate the depletion of 5-hydroxytryptamine (5-HT) induced by p-chloroamphetamine in the rat brain and it may be considered as evidence that both drugs do not inhibit 5-HT uptake in vivo. Neither AMINO nor AMI affects the rat brain level of 5-HT but at higher doses they elevate the 5-hydroxy-indoleacetic acid concentrations. AMINO antagonizes the head twitch reaction induced by 5-hydroxytryptophan in mice and tryptamine convulsions in rats. The hyperthermia induced by fenfluramine (in rats at a high ambient temperature) as well as the stimulation of the hind limb flexor reflex in spinal rats, induced by fenfluramine or LSD, are also inhibited. AMINO antagonizes the 5-HT-induced increase in blood pressure in pithed rats. All the above effects are similar to those induced by AMI, only the active doses of AMINO are higher. The results presented indicate that AMINO, like AMI, inhibits NA uptake and is a 5-HT antagonist. Amitriptylinoxide is considered to work more quickly with fewer side effects than Amitriptyline and is regarded as being equal in terms of efficacy. The way the drug works is nearly identical to Amitriptyline, except it affects the Alpha-1 receptors to a significantly lesser extent (60x less) and has among the weakest effects on acetylcholine receptors. Half maximal inhibition of acetylcholine receptor binding occurred for amitriptylinoxide at 18 mumol/l (amitriptyline: 0.32 mumol/l). Comparing all studied antidepressants for muscarinic acetylcholine receptor binding, amitriptylinoxide had the weakest affinity of all tested tricyclic compounds. Also the affinity of amitriptylinoxide for alpha-receptor binding was about 60 fold less than that of amitriptyline. For all antidepressants investigated, the lowest affinities were found for benzodiazepine, opiate and beta-receptor binding. The weak affinities of amitriptylinoxide for various receptors may be responsible for its reduced side-effects, while it still retains potent antidepressant properties by stabilising the amitriptyline-level in the brain.
Carnidazole (trade name Spartrix) is an antiprotozoal drug of the nitroimidazole class used in veterinary medicine. Spartrix (Carnidazole) is indicated for oral treatment of trichomoniasis (canker) in ornamental and homing (non-food) pigeons.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Mitoguazone is a guanylhydrazone derivative with potential antineoplastic activity. Mitoguazone inhibits S-adenosyl-L-methionine decarboxylase (SAMD), an enzyme involved in the synthesis of polyamines, resulting in a decreased proliferation of tumor cells, antimitochondrial effects, and p53-independent apoptosis. In the 1960s the drug was investigated in clinical trials. Despite the responses in acute leukemia, chronic myelogenous leukemia, lymphoma, multiple myeloma, head and neck cancer, esophageal cancer and other types of cancer, the development of the drug was discontinued because of marked myelosuppression and mucositis. Using a weekly schedule of administration, mitoguazone had minimal toxicity and showed limited activity in patients with lymphoma, esophageal cancer, prostate cancer, and other types of tumors.
Status:
Possibly Marketed Outside US
Source:
Xipranolol hydrochloride by ZYF Pharm Chemical
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

XIPRANOLOL is a beta-adrenoceptor antagonist with antiarrhythmic properties.

Showing 11771 - 11780 of 13362 results