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

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Showing 3011 - 3020 of 3069 results

Status:
Possibly Marketed Outside US
Source:
Canada:CLOROPHENE
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Chlorophene is a halogenated phenolic compound that functions as a biocide and preservative in cosmetics. In Europe, the maximum authorized concentration allowed for Chlorophene is 0.2%. The glucuronic acid conjugate, the sulfate ester conjugate, and two other minor metabolites of Chlorophene were profiled in rat urine during pharmacokinetic tests. Chlorophene is incompletely absorbed through rat skin. In several anumal species these chemicals exhibited low oral toxicity. Some evidence of toxicity was found in short-term oral toxicity studies in mice and rats with nephropathy as the principal finding. Rats and mice dosed with Chlorophene for 2 years had a dose-related and sex-related increase in the severity of nephropathy. In another set of animal tests Chlorophene was found to be an ocular irritant. There was no readily available inhalation profile for Chlorophene. Chlorophene was severely irritating to rabbits in most dermal irritation studies. Chlorophene was found to be mutagenic in four in-vitro mammalian test systems. However, neoplasms were not observed in rats treated with Chlorophene for 2 years but, in mice treated similarly a significant incidence of neoplasms was observed. A 1-year National Toxicology Program (NTP) study concluded that Chlorophene was a cutaneous irritant and a weak skin tumor promoter but had no activity as an initiator or complete carcinogen. Some reactions to Chlorophene occurred in some, but not all, clinical dermal sensitization tests.
Hexoprenaline is a selective beta2-adrenoreceptor agonist indicated for use in the treatment of bronchospasm associated with obstructive airways diseases, including asthma, bronchitis and emphysema. In many countries the drug is used as tocolytic agent (under the trade name gynipral).
Octopamine is an organic chemical closely related to norepinephrine. In many types of invertebrates it functions as a neurotransmitter. Octopamine is known to exert adrenergic effects in mammals although specific octopamine receptors have been cloned only in invertebrates. It has been shown that octopamine can stimulate alpha(2)-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha(2)-ARs. Octopamine stimulates lipolysis through beta(3)-rather than beta(1)-or beta(2)-AR activation in white adipocytes from different mammalian species. Octopamine activates only beta(3)-ARs and is devoid of alpha(2)-adrenergic agonism. Thus, octopamine could be considered as an endogenous selective beta(3)-AR agonist. In humans Octopamine is a trace amine found endogenously in the human brain where it interacts with signalling of catecholamines; it is structurally similar to synephrine and tyramine, being a metabolite of the latter (via dopamine β-hydroxylase) and substrate for the synthesis of the former (via phenethanolamine N-methyltransferase[3]) while being perhaps the closest in structure to noradrenaline. Octopamine is found in the bitter orange similar to many biogenic amines related to L-tyrosine that are used as dietary supplements, this includes synephrine and hordenine. p-Octopamine HCl (Norphen) was studied in the late 1960’s and 1970’s as a drug for the treatment of hypotensive regulatory and circulatory disorders. Octopamine was used as a nootropic. All optical isomers (enantiomers) of octopamine are on the World Anti-Doping Agency (WADA) 2014 list of substances prohibited in competition.
Status:
Possibly Marketed Outside US
Source:
Japan:Difeterol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (MIXED)


Conditions:

Antihistamine agent
Ximelagatran (Exanta or Exarta, H 376/95) is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy. In 2006, its manufacturer AstraZeneca announced that it would withdraw pending applications for marketing approval after reports of hepatotoxicity (liver damage) during trials, and discontinue its distribution in countries where the drug had been approved (Germany, Portugal, Sweden, Finland, Norway, Iceland, Austria, Denmark, France, Switzerland, Argentina and Brazil). Ximelagatran is a prodrug that is rapidly converted after oral administration to the active compound melagatran. Melagatran is able to inhibit thrombin activity directly and quickly. The melagatran molecule binds to the arginine side pocket of thrombin, inactivating the thrombin. Following oral administration of ximelagatran, oral bioavailability (measured as melagatran) is 18% to 25%. Peak melagatran levels after a ximelagatran dose of 48 mg twice daily are achieved within approximately 2 hours. Ximelagatran is rapidly and extensively converted to melagatran in the liver and other tissues. This conversion is achieved by ester hydrolysis and reduction via two intermediate metabolites, hydroxymelagatran, and ethylmelagatran. The predominant compound in plasma is the active drug, melagatran. The elimination half-life of melagatran after an oral dose of ximelagatran is 2.5 to 4.3 hours.
Status:
Possibly Marketed Outside US
Source:
NCT02143765: Phase 4 Interventional Completed Type 2 Diabetes Mellitus
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Mitiglinide is a drug for the treatment of type 2 diabetes currently marked under tradename Glufast. Glufast® is available as the tablet for oral use, containing 5 mg or 10 mg of Mitiglinide calcium hydrate. The recommended dose is 10 mg three times daily just before each meal (within 5 minutes). Mitiglinide was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on January 29, 2004, and is currently co-marketed in Japan by Kissei and Takeda. Mitiglinide is a rapid-acting insulin secretion-stimulating agent, its belongs to the meglitinide (glinide) class of blood glucose-lowering drugs. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) (K(ATP)) channels in pancreatic beta-cells.
Cyamemazine (Tercian), also known as cyamepromazine, is a typical antipsychotic drug of the phenothiazine class used primarily in the treatment of schizophrenia and psychosis-associated anxiety. Cyamemazine actually behaves like an atypical antipsychotic, due to its potent anxiolytic effects and lack of extrapyramidal side effects. Cyamemazine is used for the treatment of chronic psychotic states, anxiety, major depression.
Ifenprodil (marketed under the brands Vadilex; Dilvax; Creocral; Cerocral) is a selective NMDA receptor (glutamate) antagonist. Additionally, ifenprodil inhibits GIRK channels, and interacts with alpha1 adrenergic, serotonin, and sigma receptors. Ifenprodil acts as a vasodilator. Ifenprodil is a medicine available in a number of countries worldwide, but not in US.
Mebhydrolin (INN) or mebhydroline is a histamine H1-receptor antagonist. It is not available in the United States, but it is available in various other countries under the brand names Bexidal and Diazolin. It is used for symptomatic relief of allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis.
Status:
Possibly Marketed Outside US
Source:
NCT01224756: Phase 4 Interventional Completed Pain
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tinoridine is a non-steroidal anti-inflammatory and analgesic agent. This agent has been proved pharmacologically to show antiedematous and analgesic actions. The mechanism of the anti-inflammatory action of Tinoridine is attributed to its biomembrane stabilizing action particularly on the lysosomes which are related to cell or tissue damage at the time of inflammation through the release of hydrolytic enzymes. Tinoridine may produce gastrointestinal disorders (nausea, loss of appetite, diarrhea, and constipation), vertigo drowsiness, dry mouth and itching.

Showing 3011 - 3020 of 3069 results