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

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Showing 1191 - 1200 of 1447 results

Status:
US Previously Marketed
First approved in 1955
Source:
Vanquin by Parke-Davis
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pyrvinium (Viprynium) is an anthelmintic effective for pinworms. Pyrvinium is used in the treatment of enterobiasis caused by Enterobius vermicularis (pinworm). Pyrvinium has being shown to be a potent inhibitor of Wnt signaling (EC(50) of ∼10 nM). Pyrvinium binds all casein kinase 1 (CK1) family members in vitro at low nanomolar concentrations and pyrvinium selectively potentiates casein kinase 1α (CK1α) kinase activity. Pyrvinium pamoate (PP) is a potent noncompetitive inhibitor of the androgen receptor (AR). A noncompetitive AR inhibitor pyrvinium has significant potential to treat CRPC, including cancers driven by ligand-independent AR signaling.
Status:
US Previously Marketed
Source:
CYSTOKON by MALLINCKRODT
(1961)
Source URL:
First approved in 1953

Class (Stereo):
CHEMICAL (ACHIRAL)



Acetrizoic acid (trade names Gastrografina, Urografina in Portugal) is a palatable lemon-flavored water-soluble iodinated radiopaque X-ray contrast medium for oral or rectal administration only. Acetrizoic acid is indicated for radiographic examination of segments of the gastrointestinal tract (esophagus, stomach, proximal small intestine, and colon). The preparation is particularly indicated when a more viscous agent such as barium sulfate, which is not water-soluble, is not feasible or is potentially dangerous. Administration of hypertonic Gastrografin solutions may lead to hypovolemia and hypotension due to fluid loss from the intestine.
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.
Pregnenolone sulfate is an endogenous neurosteroid with excitatory effects in the brain, acting as a potent negative allosteric modulator of the GABAA receptor, a positive allosteric modulator of the NMDA receptor, and activator of transient receptor potential cation channel TRPM1 and TRPM3. In the model of schizophrenia, treatment with pregnenolone sulfate normalized the hyperlocomotion and stereotypic bouts, and rescued the PPI deficits of dopamine transporter knockout mice. Promnesic properties of pregnenolone sulfate were demonstrated in rat models of spatial memory performance.
Pregnenolone sulfate is an endogenous neurosteroid with excitatory effects in the brain, acting as a potent negative allosteric modulator of the GABAA receptor, a positive allosteric modulator of the NMDA receptor, and activator of transient receptor potential cation channel TRPM1 and TRPM3. In the model of schizophrenia, treatment with pregnenolone sulfate normalized the hyperlocomotion and stereotypic bouts, and rescued the PPI deficits of dopamine transporter knockout mice. Promnesic properties of pregnenolone sulfate were demonstrated in rat models of spatial memory performance.
Status:
US Previously Marketed
Source:
Profenil by Smith Pharmacal
(1947)
Source URL:
First approved in 1947
Source:
Profenil by Smith Pharmacal
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Alverine is a smooth muscle relaxant used for the treatment irritable bowel syndrome. Alverine may increase calcium influx during action potentials due to inhibition of the inactivation of L-type calcium channels, but may also suppress evoked activity by inhibiting the sensitivity of contractile proteins to calcium.
Status:
US Previously Marketed
Source:
Profenil by Smith Pharmacal
(1947)
Source URL:
First approved in 1947
Source:
Profenil by Smith Pharmacal
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Alverine is a smooth muscle relaxant used for the treatment irritable bowel syndrome. Alverine may increase calcium influx during action potentials due to inhibition of the inactivation of L-type calcium channels, but may also suppress evoked activity by inhibiting the sensitivity of contractile proteins to calcium.
Status:
US Previously Marketed
Source:
Profenil by Smith Pharmacal
(1947)
Source URL:
First approved in 1947
Source:
Profenil by Smith Pharmacal
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Alverine is a smooth muscle relaxant used for the treatment irritable bowel syndrome. Alverine may increase calcium influx during action potentials due to inhibition of the inactivation of L-type calcium channels, but may also suppress evoked activity by inhibiting the sensitivity of contractile proteins to calcium.
Status:
US Previously Marketed
Source:
Synkayvite by Hoffmann-La Roche
(1941)
Source URL:
First approved in 1941
Source:
Synkayvite by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Menadiol diphosphate is given as a vitamin K supplement to prevent bleeding caused by vitamin K deficiency. Vitamin K is normally obtained from the diet; for example it is found in green leafy vegetables, root vegetables, cereals and dairy products. Although it cannot be made by the human body itself, a certain amount of vitamin K is also made by bacteria that live in the gut. The body normally produces bile to help it absorb fats from the gut. In conditions where there is a problem with the production of bile, for example in certain liver diseases, or if there is a blockage of the bile duct, there can be problems absorbing fats. This can lead to vitamin K deficiency, decreased production of clotting factors and an increased risk of bleeding. In these situations, menadiol diphosphate is given as a vitamin K supplement to increase the production of clotting factors. It is water soluble so is readily absorbed from the gut. Also in 1974 was made attempt to develop tritiated derivatives of Synkavit (menadiol sodium diphosphate, MNDP) of high specific activity as a radioactive drug. Among the 203 evaluable treated cases, some form of response was observed in 23 out of 151 (15·2%) receiving the drug by intravenous injections and 13 out of 52 (25%) after intra-arterial injections. For the sites and types of malignant diseases which showed responses after either intravenous or intra-arterial administration among the 55 patients surviving at least 3 months after the first injection, some form of response was observed in 32 but only 5 of these showed either a "complete" or a "partial" response.It is concluded that further investigation is desirable. Kappadione is a Vitamin K derivative, was discontinued. It was manufactured by Eli Lilly and others Company.
Status:
US Previously Marketed
Source:
Synkayvite by Hoffmann-La Roche
(1941)
Source URL:
First approved in 1941
Source:
Synkayvite by Hoffmann-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Menadiol diphosphate is given as a vitamin K supplement to prevent bleeding caused by vitamin K deficiency. Vitamin K is normally obtained from the diet; for example it is found in green leafy vegetables, root vegetables, cereals and dairy products. Although it cannot be made by the human body itself, a certain amount of vitamin K is also made by bacteria that live in the gut. The body normally produces bile to help it absorb fats from the gut. In conditions where there is a problem with the production of bile, for example in certain liver diseases, or if there is a blockage of the bile duct, there can be problems absorbing fats. This can lead to vitamin K deficiency, decreased production of clotting factors and an increased risk of bleeding. In these situations, menadiol diphosphate is given as a vitamin K supplement to increase the production of clotting factors. It is water soluble so is readily absorbed from the gut. Also in 1974 was made attempt to develop tritiated derivatives of Synkavit (menadiol sodium diphosphate, MNDP) of high specific activity as a radioactive drug. Among the 203 evaluable treated cases, some form of response was observed in 23 out of 151 (15·2%) receiving the drug by intravenous injections and 13 out of 52 (25%) after intra-arterial injections. For the sites and types of malignant diseases which showed responses after either intravenous or intra-arterial administration among the 55 patients surviving at least 3 months after the first injection, some form of response was observed in 32 but only 5 of these showed either a "complete" or a "partial" response.It is concluded that further investigation is desirable. Kappadione is a Vitamin K derivative, was discontinued. It was manufactured by Eli Lilly and others Company.

Showing 1191 - 1200 of 1447 results