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

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Showing 4161 - 4170 of 4343 results

Status:
US Previously Marketed
Source:
Centrine by Bristol
(1953)
Source URL:
First approved in 1953
Source:
Centrine by Bristol
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)



Aminopentamide is a potent antispasmodic agent. As a cholinergic blocking agent for smooth muscle, its action is similar to atropine. Aminopentamide hydrogen sulfate is marketed under the brand name Centrine indicated in the treatment of acute abdominal visceral spasm, pylorospasm or hypertrophic gastritis and associated nausea, vomiting and/or diarrhea of the dogs and cats. Centrine effectively reduces the tone and amplitude of colonic contractions to a greater degree and for a more extended period than does atropine. Centrine effects a reduction in gastric secretion, a decrease in gastric acidity and a marked decrease in gastric motility. Aminopentamide is a nonselective muscarinic cholinergic .
Status:
US Previously Marketed
Source:
Quertine by Abbott
(1953)
Source URL:
First approved in 1953
Source:
Quertine by Abbott
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Quercetin is a unique bioflavonoid that has been extensively studied by researchers over the past 30 years. Quercetin, the most abundant of the flavonoids (the name comes from the Latin –quercetum, meaning oak forest, quercus oak) consists of 3 rings and 5 hydroxyl groups. Quercetin is a member of the class of flavonoids called flavonoles and forms the backbone for many other flavonoids including the citrus flavonoids like rutin, hesperidins, Naringenin and tangeritin. It is widely distributed in the plant kingdom in rinds and barks. The best described property of Quercetin is its ability to act as antioxidant. Quercetin seems to be the most powerful flavonoids for protecting the body against reactive oxygen species, produced during the normal oxygen metabolism or are induced by exogenous damage [9, 10]. One of the most important mechanisms and the sequence of events by which free radicals interfere with the cellular functions seem to be the lipid peroxidation leading eventually the cell death. To protect this cellular death to happen from reactive oxygen species, living organisms have developed antioxidant line of defense systems [11]. These include enzymatic and non-enzymatic antioxidants that keep in check ROS/RNS level and repair oxidative cellular damage. The major enzymes, constituting the first line of defence, directly involved in the neutralization of ROS/RNS are: superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx) The second line of defence is represented by radical scavenging antioxidants such as vitamin C, vitamin A and plant phytochemicals including quercetin that inhibit the oxidation chain initiation and prevent chain propagation. This may also include the termination of a chain by the reaction of two radicals. The repair and de novo enzymes act as the third line of defence by repairing damage and reconstituting membranes. These include lipases, proteases, DNA repair enzymes and transferases. Quercetin is a specific quinone reductase 2 (QR2) inhibitor, an enzyme (along with the human QR1 homolog) which catalyzes metabolism of toxic quinolines. Inhibition of QR2 in plasmodium may potentially cause lethal oxidative stress. The inhibition of antioxidant activity in plasmodium may contribute to killing the malaria causing parasites.
Status:
US Previously Marketed
Source:
Centrine by Bristol
(1953)
Source URL:
First approved in 1953
Source:
Centrine by Bristol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Aminopentamide is a potent antispasmodic agent. As a cholinergic blocking agent for smooth muscle, its action is similar to atropine. Aminopentamide hydrogen sulfate is marketed under the brand name Centrine indicated in the treatment of acute abdominal visceral spasm, pylorospasm or hypertrophic gastritis and associated nausea, vomiting and/or diarrhea of the dogs and cats. Centrine effectively reduces the tone and amplitude of colonic contractions to a greater degree and for a more extended period than does atropine. Centrine effects a reduction in gastric secretion, a decrease in gastric acidity and a marked decrease in gastric motility. Aminopentamide is a nonselective muscarinic cholinergic .
Status:
US Previously Marketed
Source:
Centrine by Bristol
(1953)
Source URL:
First approved in 1953
Source:
Centrine by Bristol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Aminopentamide is a potent antispasmodic agent. As a cholinergic blocking agent for smooth muscle, its action is similar to atropine. Aminopentamide hydrogen sulfate is marketed under the brand name Centrine indicated in the treatment of acute abdominal visceral spasm, pylorospasm or hypertrophic gastritis and associated nausea, vomiting and/or diarrhea of the dogs and cats. Centrine effectively reduces the tone and amplitude of colonic contractions to a greater degree and for a more extended period than does atropine. Centrine effects a reduction in gastric secretion, a decrease in gastric acidity and a marked decrease in gastric motility. Aminopentamide is a nonselective muscarinic cholinergic .
Status:
US Previously Marketed
Source:
Aminopterin Sodium by Lederle
(1952)
Source URL:
First approved in 1952
Source:
Aminopterin Sodium by Lederle
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Aminopterin is a synthetic derivative of pterins with antineoplastic and immunosuppressive properties. As a folate analog, aminopterin competes for the folate binding site of the enzyme dihydrofolate reductase, thereby blocking tetrahydrofolate synthesis, and resulting in depletion of nucleotide precursors and inhibition of DNA, RNA and protein synthesis. Aminopterin was marketed by Lederle Laboratories (Pearl River, New York) in the United States from 1953 to 1964 for the indication of pediatric leukemia. The closely related antifolate methotrexate was simultaneously marketed by the company during the same period. Aminopterin was discontinued by Lederle Laboratories in favor of methotrexate due to manufacturing difficulties of the former. During the period Aminopterin was marketed, the agent was used off-label to safely treat over 4,000 patients with psoriasis in the United States, producing dramatic clearing of lesions. The use of aminopterin in cancer treatment was supplanted in the 1950s by methotrexate due to the latter's better therapeutic index in a rodent tumor model. Now in a more pure preparation and supported by laboratory evidence of superior tumor cell uptake in vitro, aminopterin is being investigated in clinical trials in leukemia as a potentially superior antifolate to methotrexate.
Edrophonium is a short and rapid-acting cholinergic drug. Chemically, edrophonium is ethyl (m-hydroxyphenyl) dimethylammonium. Edrophonium is used for the differential diagnosis of myasthenia gravis and as an adjunct in the evaluation of treatment requirements in this disease. It may also be used for evaluating emergency treatment in myasthenic crises. Because of its brief duration of action, it is not recommended for maintenance therapy in myasthenia gravis. It is also useful whenever a curare antagonist is needed to reverse the neuromuscular block produced by curare, tubocurarine, gallamine triethiodide or dimethyl-tubocurarine. It is not effective against decamethonium bromide and succinylcholine chloride. It may be used adjunctively in the treatment of respiratory depression caused by curare overdosage.
Status:
US Previously Marketed
Source:
Evans Blue by Parke Davis
(1951)
Source URL:
First approved in 1951
Source:
Evans Blue by Parke Davis
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Evans Blue (EBD) is an azo dye which has a very high affinity for serum albumin. It can be useful in physiology in estimating the proportion of body water contained in blood plasma. Evans Blue Dye is widely used to study blood vessel and cellular membrane permeability as it is non-toxic, it can be administered as an intravital dye and it binds to serum albumin – using this as its transporter molecule. The EBD–albumin conjugate (EBA) can be: (i) identified macroscopically by the striking blue colour within tissue; (ii) observed by red auto-fluorescence in tissue sections examined by fluorescence microscopy; and (iii) assessed and quantified by spectrophotometry for serum samples, or homogenised tissue. has recently been utilised in mdx mice to identify permeable skeletal myofibres that have become damaged as a result of muscular dystrophy. EBD has the potential to be a useful vital stain of myofibre permeability in other models of skeletal muscle injury and membrane-associated fragility. Evans Blue is a potent inhibitor of L-glutamate uptake into synaptic vesicles. It also inhibits AMPA and kainate receptor-mediated currents (IC50 values are 220 and 150 nM respectively). P2X-selective purinoceptor antagonist.
Pregnenolone is an endogenous steroid and precursor the biosynthesis of most of the steroid hormones, including the progestogens, androgens, estrogens, glucocorticoids, and mineralocorticoids. In addition, pregnenolone is a precursor of neurosteroid pregnenolone sulfate, which is positive modulator of NMDA receptors and negative modulator of GABAA. Pregnenolone itself is a negative allosteric modulator of cannabinoid receptors. Pregnenolone is available as a dietary supplement, and is being investigated in clinical trials agains schizophrenia, bipolar disorder, major depressive disorder, marijuana dependency and other conditions.
Pregnenolone is an endogenous steroid and precursor the biosynthesis of most of the steroid hormones, including the progestogens, androgens, estrogens, glucocorticoids, and mineralocorticoids. In addition, pregnenolone is a precursor of neurosteroid pregnenolone sulfate, which is positive modulator of NMDA receptors and negative modulator of GABAA. Pregnenolone itself is a negative allosteric modulator of cannabinoid receptors. Pregnenolone is available as a dietary supplement, and is being investigated in clinical trials agains schizophrenia, bipolar disorder, major depressive disorder, marijuana dependency and other conditions.

Showing 4161 - 4170 of 4343 results