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

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Showing 1001 - 1010 of 2546 results

Itopride is a dopamine D2 receptor antagonist and inhibitor of acetylcholinesterase. It is indicated in the for the treatment of gastrointestinal symptoms caused by reduced gastrointestinal motility, such as functional non-ulcer dyspepsia (chronic gastritis), gastric fullness, rapid satiation, pain or discomfort in the upper abdomen, anorexia, heartburn, nausea, and vomiting. The drug is not approved in the USA or UK but is available in Japan and Western European countries.
Fendiline or Sensit (N-(3,3-diphenylpropyl)-(1-phenylethyl)-amine), is a diphenylalkylamine blocker of L-type calcium channels. Fendiline is an anti-anginal agent for the treatment of coronary heart disease. Pharmaco-dynamically, it exerts the typical calcium as well as calmodulin antagonistic actions: inhibition of the transmembrane calcium current, smooth muscle relaxation, negative inotropism, cardioprotection, inhibition of calmodulin-activated myosin light-chain kinase and phosphodiesterase. Pharmacokinetics reveal slow onset of action and a long half-life. The anti-anginal and anti-ischaemic efficacy of fendiline has been proven in several placebo-controlled, double-blind trials. Fendiline is an FDA-approved, albeit now clinically obsolete. Additionally, fendiline is a specific inhibitor of K-Ras plasma membrane localization that also inhibits K-Ras signal output and blocks the proliferation of K-Ras-transformed tumor cells.
Status:
Possibly Marketed Outside US
Source:
Foridon by Dubur, G.Y. et al.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Riodipine is the blocker of calcium channels of L-type. Riodipine is indicated for the treatment of arterial hypertension, prevention of attacks of angina pectoris. Antiepileptic effect of riodipine was manifested by a decreased frequency and amplitude of interictal discharges and a less frequent appearance of ictal discharges. Riodipine increased latency to first convulsive episodes and delayed the development of generalized tonic-clonic seizures. Detected side effects are: arterial hypotension, tachycardia, hypostasis of shins, increase of a daily urine. Allergic reactions to the drug are possible. Nitrates, tricyclic antidepressants, and other anti-hypertensive drugs are able to potentiate of riodipine effects.
Status:
Possibly Marketed Outside US
Source:
CLEBOPRIDE by Prieto, J. et al.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Clebopride is a dopamine antagonist drug. It is used to treat functional gastrointestinal disorder such as nausea or vomiting. Unchanged parent drug was the most abundant compound in human urine. Major metabolites included the hydroxylation at benzyl group to yield carbinolamine and its further N-dealkylation product, and the piperidine ring hydroxylation/oxidation metabolite (a lactam).
Status:
Possibly Marketed Outside US
Source:
NCT04589143: Phase 4 Interventional Completed Major Depressive Disorder
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Agomelatine behaves both as a potent agonist at melatonin MT1 and MT2 receptors and as a neutral antagonist at 5-HT2C receptors. Accumulating evidence in a broad range of experimental procedures supports the notion that the psychotropic effects of agomelatine are due to the synergy between its melatonergic and 5-hydroxytryptaminergic effects. Agomelatine is indicated for the treatment of major depressive episodes.
Status:
Possibly Marketed Outside US
Source:
Bromopan by Soc. d'Etudes Sci. de l'Ile-de-France
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Bromopride is a dopamine D2 receptor blocker. Bromopride exerts is a gastrointestinal prokinetic exploited clinically for the management of motor disorders of the upper gastrointestinal tract, including functional dyspepsia, gastric stasis of various origins and emesis.
Status:
Possibly Marketed Outside US
Source:
Spasmium by Derkosch, J.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Caroverine is a spasmolytic drug used in tinnitus treatment improves mechanosensitivity and mechanotransduction phenomenon and otoneuroprotective agent. Caroverine acts as an N-type calcium channel blocker, competitive AMPA receptor antagonist, and non-competitive NMDA receptor antagonist. When excessive glutamate binds to NMDA receptors, the receptor opens and allows calcium and sodium to enter the neuron, abnormal levels of calcium disturbs ionic balance causing spontaneous depolarization state. Pathological spontaneous depolarization state is reversed back to physiological polarization state by antagonistic property of Caroverine.
Status:
Possibly Marketed Outside US
Source:
REDUCDYN by Degussa
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Citiolone (N-acetylhomocysteine thiolactone) is an antioxidant drug used in the treatment of liver diseases.
Status:
Possibly Marketed Outside US
Source:
NCT00357019: Phase 4 Interventional Completed Keratoconjunctivitis, Vernal
(2001)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Spaglumic acid (NAAG) is the β-aspartyl isoform of N-Acetyl-l-aspartylglutamate (isospaglumic Acid is N-(N-Acetyl-l-α-aspartyl)-l-glutamic acid). In eye drops, spaglumic acid is either a magnesium or sodium salt of N-Acetyl-l-aspartylglutamate. Spaglumic acid is a mast cell stabilizer. Thus it is used in allergic conditions such as allergic conjunctivitis. Specifically spaglumic acid is approved in Portugal under the brand name Naabak and in Greece under the brand name Naaxia for use in patients with allergic conjunctivitis. Spaglumic Acid is a peptide neurotransmitter and the third-most-prevalent neurotransmitter in the mammalian nervous system. It is a weak activator of NMDA receptors and a highly selective agonist for mGlu3 receptors. Spaglumic Acid is neuroprotective under non-hydrolysing conditions in vivo.
Status:
Possibly Marketed Outside US
Source:
NCT03509922: Phase 4 Interventional Completed Peripheral Artery Disease, PAD
(2018)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Sarpogrelate (brand name Anplag; former developmental code names MCI-9042, LS-187,118) is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. It blocks serotonin-induced platelet aggregation and has applications in the treatment of many diseases including diabetes mellitus, Buerger's disease, Raynaud's disease, coronary artery disease, angina pectoris, and atherosclerosis.

Showing 1001 - 1010 of 2546 results