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

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Showing 1191 - 1200 of 2699 results

Status:
Possibly Marketed Outside US
Source:
Unknown by Kalvinš, I.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Meldonium (3-(2,2,2-trimethylhydrazinium)propionate; MET-88; quaterine, trade-named as Mildronate) is an antiischemic drug developed at the Latvian Institute of Organic Synthesis. It is a clinically used in the treatment of heart failure, myocardial infarction, arrhythmia, atherosclerosis, and diabetes. Mechanism of action is based on the regulation of energy metabolism pathways through l-carnitine lowering effect. L-Carnitine biosynthesis enzyme γ-butyrobetaine hydroxylase and carnitine/organic cation transporter type 2 (OCTN2) are the main known drug targets of meldonium, and through inhibition of these activities, meldonium induces adaptive changes in the cellular energy homeostasis. Since L-carnitine is involved in the metabolism of fatty acids, the decline in its levels stimulates glucose metabolism and decreases concentrations of l-carnitine related metabolites, such as long-chain acylcarnitines and trimethylamine-N-oxide. Meldonium is used in neurological clinics for the treatment of brain circulation disorders. It appears to improve patients' mood; they become more active, their motor dysfunction decreases, and asthenia, dizziness, and nausea become less pronounced. CNS effects of Meldonium could be mediated by stimulation of the nitric oxide production in the vascular endothelium by modification of the gamma-butyrobetaine and its esters pools. It is hypothesized that mildronate may increase the formation of the gamma-butyrobetaine esters. Meldonium was on the World Anti-Doping Agency’s (WADA) list of drugs being monitored until September 2015, when it was added to the list of banned substances, effective January 1, 2016.
Status:
Possibly Marketed Outside US
Source:
ASTOMIN by Yamanouchi Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Dimemorfan is a nonnarcotic antitussive drug. The antitussive action of dimemorfan appears to be directly on the cough center in the medulla.
Benproperine (Cofrel) is a cough suppressant. It is used for symptomatic relief of cough. Cofrel is 2-4 times as potent as codeine in suppressing cough in animals. It acts peripherally by blocking afferent sensory nerve impulses originating from receptors in the lungs and pleura.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Magnesium glycerophosphate is a magnesium salt that is available as a tablet, capsule, liquid solution or liquid suspension for oral use. Magnesium glycerophosphate is a bioavailable well tolerated source of magnesium. The organic glycerophosphoric anion, by itself, offers very significant nutritional advantages (a source of phosphorus, permeation enhancer). Adverse effects are: diarrhea, abdominal pain.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Piperaquine is a bisquinoline antimalarial drug that was first synthesized in the 1960s and used extensively in China and Indochina as prophylaxis and treatment during the next 20 years. Usage declined in the 1980s as piperaquine-resistant strains of P. falciparum arose and artemisinin-based antimalarials became available. However, during the next decade, piperaquine was rediscovered by Chinese scientists as one of a number of compounds suitable for combination with an artemisinin derivative. The rationale for such artemisinin combination therapies (ACTs) was to provide an inexpensive, short-course treatment regimen with a high cure rate and good tolerability that would reduce transmission and protect against the development of parasite resistance. Piperaquine is characterized by slow absorption and a long biological half-life, making it a good partner drug with artemisinin derivatives which are fast acting but have a short biological half-life.
Calcium glycerophosphate (brand name Prelief) is a relatively new mineral complex primarily used to neutralize acidic foods when consumed and to protect teeth. Prelief is AkPharma's brand name has a number of important uses. As a palliative in interstitial cystitis, prostatitis, overactive bladder. As a symptoms reducer in irritable bowel syndrome. Through a mechanism not fully elucidated, but it appears to reduce cellular inflammation in the urinary bladder.
Status:
Possibly Marketed Outside US
Source:
ABLAVAR by Massachusetts General Hospital
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Gadofosveset trisodium is an intravenous contrast agent used with magnetic resonance angiography (MRA), which is a non-invasive way of imaging blood vessels. The agent allows for the vascular system to be imaged more clearly by the MRA. In this way, gadofosveset trisodium is used to help diagnose certain disorders of the heart and blood vessels. Gadofosveset binds reversibly to endogenous serum albumin resulting in longer vascular residence time than non-protein binding contrast agents. The binding to serum albumin also increases the magnetic resonance relaxivity of gadofosveset and decreases the relaxation time (Tl) of water protons resulting in an increase in signal intensity (brightness) of blood. The extended acquisition time and increased relaxivity of gadofosveset allows for longer steady-state acquisition times, and potentially submillimeter voxels. Overlay of veins in steady-state MR angiography is less of a problem in multiplanar reformats with this level of resolution. This is particularly promising for MR evaluation of the peripheral vasculature. In the United States, gadofosveset is FDA-approved only for use in aortoiliac disease, with other uses being off-label. It currently does not have a role in hepatic imaging.
Status:
Possibly Marketed Outside US
Source:
Atrinositol sodium by Perstorp (Sweden)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Atrinositol antagonizes the effect of neuropeptide Y (NPY) in guinea pig basilar arteries. Atrinositol molecule derived from phytic acid. It seems to exert potent protective effects on some of the manifestations associated with diabetes in rats. Atrinositol inhibits glucose-stimulated insulin secretion by a direct effect on the pancreatic islets. Atrinositol appears to modulate fatty acid desaturases and aldose reductase in platelets and delay by a few weeks the development of cataract in this acute model of diabetes. It normalizes platelet aggregation in diabetic animals after long-term administration in vivo.
Sodium glycerol 2-phosphate (Disodium beta-glycerophosphate) is used for the preparation of thermo-sensitive chitosan hydrogen as a scaffold to construct tissue engineered injectable nucleus pulposus (NP). Since Sodium glycerol 2-phosphate (6 g/day) reduced the lithogenic index of bile in human subjects with cholesterol gallstones in a short-term study and facilitated dissolution of cholesterol gallstones in mice, Sodium glycerol 2-phosphate may have potential to help dissolve cholesterol gallstones in man. Sodium glycerol 2-phosphate is an alkaline phosphate inhibitor. Sodium β-glycerophosphate pentahydrate is used as a phosphatase inhibitor. It promotes bone matrix mineralization while delivering to osteoblasts by providing a source of phosphate ions. It is used in the development of hydrogels and scaffolds, which finds applications in tissue engineering and cell growth. It is used as an additive in isolation mediums by providing phosphate ions to isolate. It is utilized to promote mineralization in vitro by modulating bone cell metabolic activity.

Showing 1191 - 1200 of 2699 results