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

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Status:
Possibly Marketed Outside US
Source:
Artilide fumarate by Upjohn (Pharmacia)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Artilide fumarate was developed as a drug for the treatment of cardiac arrhythmias
Status:
Possibly Marketed Outside US
Source:
NCT01744236: Phase 4 Interventional Completed Type 2 Diabetes
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tilarginine is L-N-monomethyl arginine (L -NMMA), a non-selective inhibitor of nitric oxide synthase (NOS), which has been studied in the treatment of septic shock and cardiogenic shock complicating myocardial infarction. Despite strong evidence that excessive nitric oxide (NO) production plays a pivotal role in the pathogenesis of septic shock and may contribute to the pathogenesis of cardiogenic shock complicating myocardial infarction, outcome studies in these two disorders have proved disappointing. Tilarginine therapy was associated with an excess mortality, particularly at doses > 5 mg/(kg h), in septic shock, whereas the effects of a lower dose (1 mg/(kg h)) in cardiogenic shock complicating myocardial infarction were neutral. The excess mortality in patients with septic shock was almost certainly the result of unfavorable hemodynamic changes induced by Tilarginine (decreased cardiac output, increased pulmonary vascular resistance and reduced tissue oxygen delivery) whereas the lack of benefit in patients with cardiogenic shock complicating myocardial infarction may have been because the dose of Tilarginine was too low.
Oxantel is a narrow-spectrum anthelmintic effective against whipworms in dogs and cats. It is ineffective against other roundworms, flukes, tapeworms or external parasites. Oxantel acts on the nervous system of the worms as inhibitors of acetylcholinesterase. Oxantel, a cholinergic anthelmintic and fumarate reductase inhibitor, significantly inhibited biofilm formation by P. gingivalis and disrupted established biofilms at concentrations below its MIC against planktonic cells. Oxantel was more effective against P. gingivalis in biofilm than metronidazole, a commonly used antibiotic for periodontitis. When oxantel was administrated to human beings for the treatment of trichuriasis, no drug reaction or side effects were reported, and the results of hematologic, biochemical and urinary examinations didn’t reveal any significant drug-related changes.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxetorone is an antimigraine drug used for the disease-modifying treatment of migraines and marketed in several European countries. It works by non-selective inhibition of serotonin receptors and antihistamine agent. The therapeutic effects of oxetorone are primarily linked to antiserotonergic and also antihistamine and anti-adrenergic properties. Antidopaminergic properties are also suspected because hyperprolactinemia and extrapyramidal reactions have been observed. Adverse effects are: hypertonia, drowsiness at the start of treatment, diarrhoea and lymphocytic colitis. Acute intoxications by oxetorone, although uncommon, are potentially severe poisonings.
Status:
Possibly Marketed Outside US
Source:
Japan:Monosodium Fumarate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



3-Aminopropionitrile (Beta-amino-propionitrile, BAPN) is a toxic constituent from lathyrus plants. BAPN found in lathyrus odoratus (our more common garden sweet pea plant) is thought to be responsible for osteolathyrism due to irreversible inhibition of lysyl oxidase (LOX), an enzyme necessary for the covalent cross-linking of tropocollagen molecules during the maturation of mature collagen. BAPN demonstrated in antimetastatic and antimyelofibrotic activity in vivo due to inhibition of LOX.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

TILIDINE is a low to medium potency opioid analgesic. It is metabolized to its active metabolites, nortilidine and bisnortilidine. Its analgesic activity is largely exerted through nortilidine which is a potent agonist at Mu opioid receptors.
Status:
Possibly Marketed Outside US
Source:
NCT04274673: Phase 4 Interventional Unknown status Chronic Pain, Acute Pain, Cotinine, Hysterectomy
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cotinine is a product formed after the chemical nicotine enters the body. Measuring cotinine in people’s blood is the most reliable way to determine exposure to nicotine for both smokers and nonsmokers exposed to environmental tobacco smoke. Cotinine is safe, non-addictive and has pharmacokinetic properties adequate for therapeutic use. Research has shown that cotinine has antipsychotic, anxiolytic, and antidepressant properties and modulates the serotonergic, cholinergic and dopaminergic systems. Cotinine behaves as a positive allosteric modulator of the nicotinic acetylcholine receptors and has anti-inflammatory effects. Cotinine is under investigation as an agent for the treatment of depression, PTSD, schizophrenia, Alzheimer's disease and Parkinson's disease.
Status:
Withdrawn

Class (Stereo):
CHEMICAL (RACEMIC)

Aminorex is an anorectic stimulant drug. Aminorex inhibits norepinephrine and dopamine transporters with IC50 of 0.33 and 0.85 uM. It was briefly available as an appetite suppressant in the 1960s in Switzerland, Germany, and Austria, but was found to cause pronounced vasoconstriction in the pulmonary vasculature, and was withdrawn from the market in 1972 due to several cases of fatal and life-threatening pulmonary hypertension. In the USA aminorex is an illegal schedule I drug.