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

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Showing 81 - 90 of 100 results

Status:
Possibly Marketed Outside US
Source:
Canada:TRICHLORFON
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Trichlorfon (Metrifonate), the organophosphorous cholinesterase inhibitor, O,O-dimethylhydroxy-2,2,2-trichlorethyl-phosphonate, has been used sporadically in the treatment of human schistosomiasis for a decade. It has selective and variable schistosomicidal activity against S. haematobium that results from its partial metabolism to a highly active anti-cholinesterase, dichlorvos. Schistosomal cholinesterase is more susceptible to this metabolite than that of the human host, but transient reductions in both plasma and erythrocyte cholinesterase activity are demonstrable at therapeutic dosage. However, despite early concerns about its potential toxicity, metrifonate is well tolerated and has been used effectively and extensively in large-scale control programmes. Its potential to enhance central nervous system cholinergic neurotransmission led to clinical trials for the treatment of people with Alzheimer's disease (AD).
Status:
Possibly Marketed Outside US
Source:
Unknown by Wheeler, H.L.|McFarland, D.F.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Methylthiouracil is an orally active thyroid enzyme activity inhibitor. Methylthiouracil was introduced in the mid-1940s for the treatment of hyperthyroidism. Methylthiouracil is no longer in clinical use in most countries, although it may be used to a limited degree in some eastern European countries. Methylthiouracil possess anti-inflammatory effects in vitro and in vivo and was found effective in a murine model of sepsis.
Status:
Possibly Marketed Outside US
Source:
NCT02683863: Phase 4 Interventional Completed Multiple Sclerosis
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Niridazole is used (but not officially recommended) for the treatment of schistosomiasis, dracunculiasis and tungiasis. The mode of action of niridazole is not fully understood. The major action of niridazole seems to be on the glycogen metabolism of the helminths. The drug also case structural damage to the reproductive system of female schistosomes. Another possible mechanism of action of niridazole involves the inhibition of DNA synthesis in schistosomes. It is metabolized in the liver. The most serious side effects were those connected with the nervous area (convulsion, hallucination, etc.).
Status:
Possibly Marketed Outside US
Source:
Marlate by Elbs, K.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Methoxychlor is a contact and stomach insecticide effective against a wide range of pests encountered in agriculture, households, and ornamental plantings. It was registered for use on fruits, vegetables, forage crops and on shade trees. Methoxychlor was also registered for veterinary use as a poison to kill parasites on dairy and beef cattle. Exposure to methoxychlor may occur during its manufacture or use as a pesticide. In an acute oral study in animals, changes in the liver were reported. Dermal contact with methoxychlor is slightly irritating to the skin. The use of methoxychlor as a pesticide was banned in the United States in 2003 and in the European Union in 2002.
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.
mixture
Status:
Other

Class:
MIXTURE

Trypan blue (trade name MembraneBlue, VisionBlue) is a vital stain used to selectively color dead tissues or cells blue. Live cells or tissues with intact cell membranes are not colored. Since cells are very selective in the compounds that pass through the membrane, in a viable cell trypan blue is not absorbed; however, it traverses the membrane in a dead cell. Hence, dead cells are shown as a distinctive blue color under a microscope. Since live cells are excluded from staining, this staining method is also described as a dye exclusion method. This dye may be a cause of certain birth defects such as encephalocele. Trypan blue is commonly used in microscopy (for cell counting) and in laboratory mice for assessment of tissue viability. The method cannot distinguish between necrotic and apoptotic cells. Trypan blue is also used in ophthalmic cataract surgery to stain the anterior capsule in the presence of a mature cataract, to aid in visualization, before creating the continuous curvilinear capsulorhexis.
Cyclophosphamide (the generic name for Cytoxan, Neosar, Revimmune), also known as cytophosphane, is a nitrogen mustard alkylating agent, from the oxazophorines group. It is used to treat various types of cancer and some autoimmune disorders. It is a "prodrug"; it is converted in the liver to active forms that have chemotherapeutic activity
Medroxyprogesterone acetate (INN, USAN, BAN), also known as 17α-hydroxy-6α-methylprogesterone acetate, and commonly abbreviated as MPA, is a steroidal progestin, a synthetic variant of the human hormone progesterone. Medroxyprogesterone acetate (MPA) administered orally or parenterally in the recommended doses to women with adequate endogenous estrogen, transforms proliferative into secretory endometrium. Androgenic and anabolic effects have been noted, but the drug is apparently devoid of significant estrogenic activity. While parenterally administered MPA inhibits gonadotropin production, which in turn prevents follicular maturation and ovulation, available data indicate that this does not occur when the usually recommended oral dosage is given as single daily doses. MPA is a more potent derivative of its parent compound medroxyprogesterone (MP). While medroxyprogesterone is sometimes used as a synonym for medroxyprogesterone acetate, what is normally being administered is MPA and not MP. Used as a contraceptive and to treat secondary amenorrhea, abnormal uterine bleeding, pain associated with endometriosis, endometrial and renal cell carcinomas, paraphilia in males, GnRH-dependent forms of precocious puberty, as well as to prevent endometrial changes associated with estrogens. Progestins diffuse freely into target cells in the female reproductive tract, mammary gland, hypothalamus, and the pituitary and bind to the progesterone receptor. Once bound to the receptor, progestins slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH surge.

Showing 81 - 90 of 100 results