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

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Showing 51 - 60 of 100 results

Status:
US Previously Marketed
Source:
21 CFR 310.502(a) certain drugs 1,1,1-trichloroethane
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

1,1,1-trichloroethane (methyl chloroform) is a colorless liquid or vapour with a sharp sweet smell. It dissolves in water and other chemicals and easily evaporates into the air. TCE is non-flammable. Trichloroethane is used as a solvent and degreasing agent in industry. It is an ingredient in consumer products such as household cleaners, glues, and aerosol sprays. Methyl chloroform is also used as a chemical intermediate in the production of vinylidene chloride. It was formerly used as a food and grain fumigant. Excessive absorption of this substance through the lungs or gastrointestinal tract produces central nervous system (CNS) depression proportional to the amount absorbed. Mild liver and kidney dysfunction may occur transiently following recovery from CNS depression. The consumption of trichloroethane has been banned by the 1987 Montreal Protocol because of its ozone-depleting potential.
Trichloroacetic acid (TCA; TCAA) is a chemical used in skin peel formulations. It is more frequently used for lighter skin and is less used on darker skin because of the higher risks of scarring, as well as post-peel dyschromias. Low concentrations, 10-35% is preferred for skin peel formulations so that it only reaches the upper papillary dermis. Topical TCA is an efficacious treatment of internal anal high-grade squamous intraepithelial lesions (HSIL). Advantages of TCA for this recurrent disease process include low cost, no requirement for special equipment beyond that for high-resolution anoscopy, and painless application procedure.
Status:
US Previously Marketed
Source:
21 CFR 310.502(a) certain drugs vinyl chloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Vinyl Chloride, a gas, is produced as a combustion product in tobacco smoke. Vinyl Chloride is used to produce polyvinyl chloride (PVC) and was workers exposed to vinyl chloride were at carcinogenic risk.
Cholesterol is a sterol (a combination steroid and alcohol) and a lipid found in the cell membranes of all body tissues, and transported in the blood plasma of all animals. The high level of cholesterol in the blood is a marker of hypercholesterolemia, also called dyslipidemia. As a part of homeopathic product, it helps to support general liver and gallbladder health, and is used for temporary relief of symptoms related to adrenal glands such as fatigue and low energy. Cholesterol binds to and affects the gating of a number of ion channels such as the nicotinic acetylcholine receptor (nAChR) Inwardly-rectifying K+ channels (Kir); Transient receptor potential vanilloid 1 channels (TRPV1) and Large-conductance Ca2+-sensitive voltage-gated K+ channels (BK). It was shown the new mechanistic insights into the role of cholesterol in the regulation of nAChR, showing that cholesterol regulates the channels by two distinct mechanisms: stabilization of the channels in a resting state that depends on specific lipid-protein interactions and facilitation of the transitions between uncoupled and coupled states that depends on the hydrophobic thickness of the membrane
Status:
US Previously Marketed
First approved in 1962

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Uramustine (INN) or uracil mustard is a chemotherapy drug which belongs to the class of alkylating agents. It is used in lymphatic malignancies such as non-Hodgkin's lymphoma. Uracil Mustard selectively inhibits the synthesis of deoxyribonucleic acid (DNA). The guanine and cytosine content correlates with the degree of Uracil Mustard-induced cross-linking. At high concentrations of the drug, cellular RNA and protein synthesis are also suppressed. After activation, it binds preferentially to the guanine and cytosine moieties of DNA, leading to cross-linking of DNA, thus inhibiting DNA synthesis and function. The DNA damage leads to apoptosis of the affected cells. Chemically it is a derivative of nitrogen mustard and uracil.
Status:
US Previously Marketed
Source:
Beta-Prone by Forest
(1959)
Source URL:
First approved in 1959
Source:
Beta-Prone by Forest
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Propiolactone (or beta-propiolactone) is a disinfectant used in vapor form to sterilize vaccines, grafts, blood plasma, surgical instruments. It has been used against bacteria, fungi, and virus. Propiolactone was first commercially available in the United States in 1958 but then was withdrawn because it was discovered that compound was a human carcinogen. The results have shown the generation of tumors in several tissues and from different administration routes. Propiolactone is a direct-acting alkylating agent that reacts with polynucleotides and DNA, mainly at N7 of guanine and N1 of adenine, to form carboxyethyl derivatives.
Status:
US Previously Marketed
Source:
Tricofuron by Eaton
(1957)
Source URL:
First approved in 1957
Source:
Tricofuron by Eaton
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Furazolidone is a nitrofuran derivarive with broad antibacterial, antiprotazoal properties. It was used for the treatment of bacterial or protozoal enteritis and diarrhea, but now the drug is no longer prescibed in the US. The mechanism of furazolidone action is supposed to be mediated by its binding to bacterial DNA.
Status:
US Previously Marketed
Source:
METATENSIN #2 by SANOFI AVENTIS US
(1982)
Source URL:
First approved in 1954

Class (Stereo):
CHEMICAL (ABSOLUTE)



Reserpine is an alkaloid, isolated from the Rauwolfia serpentina plant and developed by Ciba pharma. Reserpine was approved by FDA for the treatment of hypertension and psychotic disorders. The drug exerts its effect by blocking two vesicular monoamine transporters, VMAT1 and VMAT2. The blockade results in vesicles that lose their ability to store neurotransmitter molecules. Neurotransmitters, thus retained in cytosol, are then neutralized by MAO.
Status:
US Previously Marketed
First approved in 1951
Source:
Kwell by Reed & Carnrick
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Lindane is an isomer of hexachlorocyclohexane that has been used both as an agricultural insecticide and as a pharmaceutical. As a shampoo, lindane is used for treamtment lice infestation. Lindane lotion is used for treatment of scabies. Due to toxicities, associated with lindane, it is used only in patients who cannot tolerate or have failed first-line treatment with safer medication. Lindane exerts its parasiticidal action by being directly absorbed into the parasites and their ova, where it interferes with GABA neurotransmitter function by interacting with the GABAA channel complex at the picrotoxin binding site.