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

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Showing 15681 - 15690 of 16236 results

Adiphenine is a ternary amino ligand. It is used as a local anesthetic that reduces the frequency of acetylcholine-induced single-channel currents. It was originally introduced as a spasmolytic agent. Adiphenine reduced the muscle tone of the gastrointestinal tract, bile duct and gallbladder, bronchi, bladder. It affects the tone of the muscles of the eye, causing the pupil dilated (mydriasis), increased intraocular pressure, and paralysis of accommodation. Influences on the cardiovascular system, causing tachycardia and improving AV-conduction. Adiphenine side effects are: nausea, vomiting, heartburn, dizziness, headache. Adiphenine has not been widely used clinically.
Status:
US Previously Marketed
Source:
NEOMERSYL MERSALYL by CENTRAL PHARCA
(1961)
Source URL:
First marketed in 1935

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

MERSALYL (Mersal) is an organomercury compound, mercurial diuretics that superseded by safer diuretics such as thiazides, and is hardly used anymore. Due to the idiosyncratic nature of mercury toxicity, the risk of severe disease and sudden death are unpredictable and frequently show no warning signs. Mercurial diuretics cause diuresis by reducing the reabsorption sodium in the ascending loop of Henle, thus causing more water being delivered to the distal convoluted tubule. Unfortunately, earlier physicians misconstrued hallmark symptoms of mercury poisoning such as excessive salivation as signs of mercury's efficacy, including up until the early 1960s when the use of mercurial diuretics was halted in medicine.
Status:
US Previously Marketed
Source:
ACR-ALLANTOMIDE AMINACRINE HYDROCHLORIDE by NATIONAL DRUG
(1961)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Aminacrine has long been known to be a potent frameshift mutagen in viruses and bacteria. It is one in a general class of aminoacridine dyes that bind to DNA and possess mutagenic activity. Aminacrine is used clinically as a topical antiseptic. A part from therapeutic use, aminacrine is also introduced as a matrix for negative mode matrix-assisted laser desorption/ionization (MALDI).
Status:
US Previously Marketed
Source:
hexobarbital
(1933)
Source URL:
First marketed in 1933
Source:
hexobarbital
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Hexobarbital or hexobarbitone, (sold both in acid and sodium salt, brand name Evipan, and Tobinal), is a barbiturate derivative having hypnotic and sedative effects. It was used in the 1940s and 1950s as an agent for inducing anesthesia for surgery, as well as a rapid-acting, short-lasting hypnotic for general use, and has a relatively fast onset of effects and short duration of action. It was also used to murder women prisoners at Ravensbruck Concentration Camp. Modern barbiturates (such as Thiopental) has largely supplanted the use of hexobarbital as an anesthetic, as they allow for better control of the depth of anesthesia. Hexobarbital is still used in some scientific research. Hexobarbital binds at a distinct binding site associated with a Cl- ionophore at the GABA-A receptor, increasing the duration of time for which the Cl- ionophore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
Status:
US Previously Marketed
Source:
amobarbital
(1923)
Source URL:
First marketed in 1923

Class (Stereo):
CHEMICAL (ACHIRAL)



AMOBARBITAL is a barbiturate derivative with hypnotic and sedative properties. In an in vitro study in rat thalamic slices amobarbital worked by activating GABAA receptors, which decreased input resistance, depressed burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increased both the amplitude and decay time of inhibitory postsynaptic currents. Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high.
Status:
US Previously Marketed
Source:
DL-alpha tocopheryl acetate
(1921)
Source URL:
First marketed in 1921
Source:
DL-alpha tocopheryl acetate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



dl-α-tocopheryl phosphate has a growth acceleration effect on domestic fowl. Also was confirmed, that in all investigated animals dl-α-tocopheryl phosphate has an ability to being converted into vitamin E.
Status:
US Previously Marketed
Source:
GENTIA-JEL APPLICATORS by WESTWOOD
(1961)
Source URL:
First marketed in 1921
Source:
gentian violet
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Gentian violet ((GV) hexamethyl pararosaniline, also known as crystal violet, methyl violet) is a triphenylmethane dye with anti-bacterial, anti-fungal, anti-helminithic, anti-trypanosomal, anti-angiogenic and anti-tumor properties. GV has a lengthy history and has been used successfully as monotherapy and an adjunct to treatment in a variety of diseases. Gentian violet interacts with negatively charged components of bacterial cells including the lipopolysaccharide (on the cell wall), the peptidoglycan and DNA. A similar cell penetration and DNA binding process is thought to take place for fungal cells as well. Because Gentian violet is a mutagen and mitotic poison, cell growth is consequently inhibited. A photodynamic action of gentian violet, apparently mediated by a free-radical mechanism, has recently been described in bacteria and in the protozoan T. cruzi. Evidence also suggests that gentian violet dissipates the bacterial (and mitochondrial) membrane potential by inducing permeability. This is followed by respiratory inhibition. This anti-mitochondrial activity might explain gentian violet's efficacy towards both bacteria and yeast with relatively mild effects on mammalian cells.
Silver iodide is an inorganic compound with the formula AgI. It is used as a photosensitive agent in photography, as a local antiseptic, as a chemical intermediate, and in cloud seeding for rain-making. The major hazards encountered in the use and handling of silver iodide stem from its toxicologic properties. Effects from exposure may include skin rashes, conjunctivitis, argyria (a permanent ashen-gray discoloration of skin, conjunctiva, and internal organs), headache, fever, hypersensitivity, laryngitis, and bronchitis.
Status:
US Previously Marketed
Source:
1,2-ethanedisulfonic acid
(1921)
Source URL:
First marketed in 1921
Source:
1,2-ethanedisulfonic acid
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Sodium 1,2-ethanedisulfonate dihydrate is salt of ethanedisulfonic acid. Ethanedisulfonic acid is used in pharmaceutical formulations of some antipsychotic compounds to form salts with the active ingredients, known as edisylates.
Status:
US Previously Marketed
Source:
Sparteine Sulphate U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Sparteine Sulphate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Sparteine is a class 1a antiarrhythmic agent; a sodium channel blocker. It is the predominant alkaloid in Lupinus mutabilis, and is thought to chelate the bivalents calcium and magnesium. It is not FDA approved for human use as an antiarrhythmic agent. It is also used as a chiral base in organic chemistry, and as a ligand in organic chemical synthesis. Marketed under the brand name Spal in Taiwan and Sparteine in Brazil.

Showing 15681 - 15690 of 16236 results