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

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Showing 2771 - 2780 of 8583 results

Acetarsone is a pentavalent arsenical compound with antiprotozoal and antihelmintic properties. It was first discovered in 1921 at Pasteur Institute by Ernest Fourneau, and sold under the brand name Stovarsol (fourneau is the French word for stove). Before stovarsol was used in the treatment of congenital syphilis, it had already been used in other diseases : amoebiasis, acquired syphilis, yaws, trypanosomiasis and malaria, and a formidable list of toxic manifestations can be compiled from the literature. Bender (I927) recorded six cases of poisoning with malaise, fever, cedema, jaundice, diarrhoea, albuminuria, bronchitis, coryza and skin troubles, such as diffuse erythema, dryness and pruritus. Of 232 cases of amoebiasis treated by Brown (I935) without a death, thirteen (5.6%) had toxic erythemata, some of them so severe as to amount to exfoliative dermatitis. Although its mechanism of action is not fully known, acetarsone may bind to protein-containing sulfhydryl groups located in the parasite, thereby forming lethal As-S bonds. This may prevent their functioning and eventually kill the parasite.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Pirenoxine is an anti-cataract agent which is used in many asian countries under the name Catalin. Although its efficacy is not proved scientifically, the drug may play an important role in cataract prevention. It is supposed that the anti-cataract effect of pirenoxine results from inhibition of sulfhydryl combination of quinoid substances with lens proteins and the inhibition leads to the maintenance of lens transparency.
Status:
Possibly Marketed Outside US
Source:
Alizarin Sulfonate, Calcium by BASF|Perkin, W. H.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Alizarin is an anthraquinone is an organic compound that has been used as a red dye, principally for dyeing textile fabrics since ancient times. Historically it was derived from the roots of the madder plant Rubia tinctorum, in which it occurs combined with the sugars xylose and glucose. Laboratory methods of preparing alizarin from anthraquinone were discovered in 1868, and, upon commercial introduction of the synthetic dye in 1871, the natural product disappeared from the market for textile dyes. At present alizarin is commonly used in biomedical studies involving bone growth, osteoporosis, bone marrow, calcium deposits in the vascular system, cellular signaling, gene expression, tissue engineering, and mesenchymal stem cells. Alizarin precipitates free calcium, and tissue block containing calcium stain red immediately when immersed in alizarin. It is approved by FDA as a Calcium test system for clinical chemistry. Alizarin red, has been used for a quantitative sweat measure to characterize the sweat distribution in patients with syncope, anxiety, and POTS.
Status:
Possibly Marketed Outside US
Source:
Unknown
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Ethyl loflazepate (Lof) has been used widely as a sedative and anxiolytic agent for nearly 20 years. Ethyl loflazepate was designed to be a prodrug for descarboxyloflazepate, its active metabolite. It is the active metabolite which is responsible for most of the pharmacological effects rather than ethyl loflazepate. The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-ydroxydescarbethoxyloflazepate which are the benzodiazepine receptor agonists. Ethyl loflazeplate is commercialized in Mexico, under the trade name Victan. It is officially approved for the following conditions Anxiety: Post-trauma anxiety; Anxiety associated with severe neuropathic pain; Generalized anxiety disorder (GAD); Panic attack; Delirium tremens. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Accumulation of the active metabolites of ethyl loflazepate are not affected by those with renal failure or impairment. The symptoms of an overdose of ethyl loflazepate include sleepiness, agitation and ataxia. Hypotonia may also occur in severe cases. These symptoms occur much more frequently and severely in children. High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Nitarsone is an organoarsenic compound that is used in poultry production as a feed additive to increase weight gain, improve feed efficiency, and prevent blackhead disease. It is marketed as Histostat by Zoetis, a publicly traded subsidiary of Pfizer. Histostat is approved for the prevention of histomoniasis (blackhead disease) in turkeys and chickens, and is the only approved animal drug for this indication. Histomoniasis is a disease that occurs regionally and seasonally in turkeys, and causes significant mortality. Nitarsone is one of four arsenical animal drugs approved by the U.S. Food and Drug Administration for use in poultry, along with roxarsone, arsanilic acid, and carbarsone. Following the 2011 suspension of roxarsone sales in the United States, however, it is believed to be the only arsenical animal drug currently marketed in the U.S. In September 2013, the FDA announced that Zoetis and Fleming Laboratories would voluntarily withdraw current roxarsone, arsanilic acid, and carbarsone approvals, leaving only nitarsone approvals in place. When the withdrawals occurred, nitarsone was only arsenical approved for use in food animals in the U.S. In 2015 FDA withdrew the approval of using nitarsone in animal feeds. The ban came into effect at the end of 2015.
Nimetazepam (Erimin) is an intermediate-acting hypnotic drug which is a benzodiazepine derivative. It was first synthesized in 1962 in Japan. It does possess hypnotic, anxiolytic, sedative, and skeletal muscle relaxant properties. Nimetazepam is also an anticonvulsant. It is sold in 5 mg tablets known as Erimin. It is generally prescribed for the treatment of short-term severe insomnia in patients who have difficulty falling asleep or maintaining sleep. Nimetazepam is currently a Schedule IV drug under the international Convention on Psychotropic Substances of 1971. In Singapore, nimetazepam is a class C drug under the Misuse of Drugs Act. In Hong Kong, nimetazepam is regulated under Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance. Nimetazepam can only be used legally by health professionals and for university research purposes.
Status:
Possibly Marketed Outside US
Source:
NCT02931136: Phase 4 Interventional Not yet recruiting Mild Cognitive Impairment
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Huperzine A is a plant alkaloid derived from Club moss plant, Huperzine serrata, which is a member or the Lycopodium species. Huperzine-A is in phase III clinical trial in the USA (Alzheimer disease) and is available as a dietary supplement. It selectively and reversibly inhibits acetylcholinesterase. Huperzine A is also a NMDA receptor antagonist, which protects the brain against glutamate induced damage, and it increases nerve growth factor levels. Huperzine A is used for Alzheimer's disease, memory and learning enhancement, and age-related memory impairment. It is also used for treating a muscle disease called myasthenia gravis, for increasing alertness and energy, and for protecting against agents that damage the nerves such as nerve gases. It can cause some side effects including nausea, diarrhea, vomiting, sweating, blurred vision, slurred speech, restlessness, loss of appetite, contraction and twitching of muscle fibers, cramping, increased saliva and urine, inability to control urination, high blood pressure, and slowed heart rate. Various medications used for glaucoma, Alzheimer's disease, and other conditions (Cholinergic drugs) interacts with Huperzine A.
Status:
Possibly Marketed Outside US
Source:
NCT01456780: Phase 4 Interventional Completed Meibomian Gland Dysfunction
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Loteprednol (as the ester loteprednol etabonate) is a corticosteroid used to treat inflammations of the eye. It is marketed by Bausch and Lomb as Lotemax. It is a topical corticoid anti-inflammatory. It is used in ophthalmic solution for the treatment of steroid responsive inflammatory conditions of the eye such as allergic conjunctivitis, uveitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, and selected infective conjunctivitis’s. Lotemax is less effective than prednisolone acetate 1% in two 28-day controlled clinical studies in acute anterior uveitis, where 72% of patients treated with Lotemax experienced resolution of anterior chamber cells, compared to 87% of patients treated with prednisolone acetate 1%. Lotemax is also indicated for the treatment of post-operative inflammation following ocular surgery. Corticosteroids inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation. There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Corticosteroids are capable of producing a rise in intraocular pressure (IOP). Loteprednol etabonate is structurally similar to other corticosteroids. However, the number 20 position ketone group is absent. It is highly lipid soluble, which enhances its penetration into cells. Loteprednol etabonate is synthesized through structural modifications of prednisolone-related compounds so that it will undergo a predictable transformation to an inactive metabolite. Based upon in vivo and in vitro preclinical metabolism studies, loteprednol etabonate undergoes extensive metabolism to inactive carboxylic acid metabolites. Lotemax possesses some adverse reactions associated with ophthalmic steroids include elevated intraocular pressure, which may be associated with optic nerve damage, visual acuity and field defects, posterior subcapsular cataract formation, secondary ocular infection from pathogens including herpes simplex, and perforation of the globe where there is thinning of the cornea or sclera.
Status:
Possibly Marketed Outside US
Source:
Sera baktopur direct by Shimizu, M.|Takase, Y.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nifurpirinol, 6-hydroxymethyl-2-[2-(5-nitro-2-furyl)vinyl]pyridine, has been widely used as an antibacterial drug against diseases of fish. M. Shimizu and Y. Takase showed marked inhibitory activity against many species of bacteria, including several fish pathogens. They found minimum inhibitory concentrations (MIC's) of 0.1 to 0.3 ug of Nifurpirinol (P-7138) per ml of broth medium (ug/ml) for Vibrio anguilIarum, Aeromonas salmonicida, and Aeromonas liquefaciens. The first designation for this drug was "P-7138." Subsequently, "Furanace" was designated as the trade name, and "nifurpirinol" was selected as the generic name.
Status:
Possibly Marketed Outside US
Source:
DEPAS by Yoshitomi Pharmaceutical Industries
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Etizolam is an analogue of benzodiazepine that contains thienotriazolodiazepine group. The drug was developed and approved in Japan and now is used in Japan, Italy and India for the treatment of anxiety disorders. Etizolam exerts its action through activation of GABA A receptors, moreover, the agonistic behavior was shown on isolated neurons. There are several cases when etizolam dependence was reported. In many countries the drug is recognized as a psychoactive substance and its distribution is illegal there.

Showing 2771 - 2780 of 8583 results