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

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Showing 3301 - 3310 of 3582 results

Denatonium, usually available as denatonium benzoate (trade names Bitrex) is the most bitter chemical compound known, with bitterness thresholds of 0.05 ppm for the benzoate and 0.01 ppm for the saccharide. Scientists at Macfarlan Smith, Ltd. of Edinburgh, Scotland discovered Bitrex during research on derivatives of the anesthetic lidocaine. The extremely bitter taste proved effective in reducing ingestion by humans and animals. Denatonium is commonly included in placebo medications used in clinical trials to match the bitter taste of certain medications. Denatonium activates bitter taste receptor, mainly, TAS2R4, TAS2R8, TAS2R10, TAS2R13 on many cell types and plays important roles in chemical release, ciliary beating and smooth muscle relaxation through intracellular Ca(2+)-dependent pathways.
Chlorprothixene (Taractan, Tarasan, Truxal) is a thioxanthine derivative developed by Lundbeck for the treatment of psychotic disorders. The drug exerts its activity by binding to and inhibiting serotonin receptors, dopamine receptors, muscarinic acetylcholine receptor, histamine H1 receptor and alpha1-adrenergic receptor.
Status:
US Previously Marketed
Source:
Monase by Upjohn
(1961)
Source URL:
First approved in 1961
Source:
Monase by Upjohn
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

ETRYPTAMINE (MONASE®), similar to the hallucinogenic tryptamines, is an inhibitor of monoamine oxidase, introduced for use as an antidepressant. It was withdrawn from the market due to problems with agranulocytosis and other side effects. However, it's activity is still under scientific investigation.
Status:
US Previously Marketed
First approved in 1959
Source:
Laverna by Winthrop
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Oxyphenisatin is a stimulant laxative that has been used by mouth and as an enema. Oxyphenisatin was introduced as Lavema by Winthrop in US in 1959. Oxyphenisatin was used as a cleansing enema apart from x-ray studies and prior to urinary, gastro-intestinal and cholecystography x-ray examination. Oxyphenisatin was also used for preoperative preparation of the large intestine and colon. May be mixed with barium for x-ray examination of the large intestine. Oxyphenisatin may cause jaundice. Oxyphenisatin-induced liver damage usually occurs when the drug has been taken for at least six months and usually two years. Oxyphenisatin was withdrawn in most countries in the early 1970s.
Status:
US Previously Marketed
First approved in 1958
Source:
Madribon by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfadimethoxine is a sulfonamide antibacterial used to treat many infections including treatment of respiratory, urinary tract, enteric, and soft tissue infections. It is most frequently used in veterinary medicine, although it is approved in some countries for use in humans. Sulfadimethoxine inhibits bacterial synthesis of folic acid (pteroylglutamic acid) from para-aminobenzoic acid. Sulfadimethoxine is approved in Russia for use in humans, including children, and has been successfully used there for more than 35 years and is available as an over-the-counter drug manufactured by a number of Russian pharmaceutical companies. In USA and Europe sulfadimethoxine is approved in a veterinary medicinal products. ANADA was approved by FDA in US in 1997 as an Over the Counter medicine for treatment of bovine respiratory disease complex (shipping fever complex) and bacterial pneumonia associated with Pasteurella Spp. Sensitive to sulfadimethoxine; necrotic pododermatitis (foot rot) and calf diphtheria caused by Fusobacterium necrophorum (Sphaerophorus necrophorus) sensitive to sulfadimethoxine. Bioequivalence for this generic animal drug, Sulfadimethoxine Injection 40%, was established by demonstration of chemical equivalence to the pioneer product, Hoffmann-La Roche's Albon® Injection 40% (NADA 041-245).
Status:
US Previously Marketed
Source:
PACATAL 25MG by WC
(1961)
Source URL:
First approved in 1957
Source:
Pacatal by Warner/Chilcott
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

PECAZINE is a phenothiazine derivative that was used as an antipsychotic. It is also an allosteric inhibitor of MALT1 paracaspase activity.
Status:
US Previously Marketed
Source:
DARTAL 100MG by SEARLE
(1961)
Source URL:
First approved in 1957
Source:
Dartal by Searle
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


THIOPROPAZATE, a phenothiazine derivative, is a typical antipsychotic. It is a prodrug to perphenazine.
Status:
US Previously Marketed
Source:
Bauer and Black Foot Powder by Bauer & Black
(1956)
Source URL:
First approved in 1956
Source:
Bauer and Black Foot Powder by Bauer & Black
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Novobiocin (also known as streptonivicin) is an aminocoumarin antibiotic, active against Staphylococcus epidermidis. Novobiocin and other aminocoumarin antibiotics act as a potent competitive inhibitor of DNA gyrase B. The oral form of the drug was withdrawn from the market in 1999 due to safety or effectiveness reasons. Later it was discovered that novobiocin inhibited Hsp90 and topoisomerase II, and novobiocin was investigated in clinical trials against metastatic breast cancer and non-small cell lung cancer. Topical form of novobiocin was investigated in combination with nalidixic acid for treatment of psoriasis.
Status:
US Previously Marketed
Source:
Provell Maleate by Lilly
(1953)
Source URL:
First approved in 1953
Source:
Provell Maleate by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Protoveratrine A, the principal alkaloid of Veratrum album, has been used in the treatment of hypertension but has largely been replaced by drugs with fewer adverse effects.

Showing 3301 - 3310 of 3582 results