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:
Unknown by Topchiev, A.V.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Hydrocotarnine is a crystalline alkaloid, obtained from opium and also formed by the reduction of cotarnine. It is a non-narcotic opium alkaloid. Hydrocotarnine is supposed to potentiate the analgesic effect of oxycodone with unknown mechanism.
Status:
Possibly Marketed Outside US
Source:
Unknown by Topchiev, A.V.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Hydrocotarnine is a crystalline alkaloid, obtained from opium and also formed by the reduction of cotarnine. It is a non-narcotic opium alkaloid. Hydrocotarnine is supposed to potentiate the analgesic effect of oxycodone with unknown mechanism.
Status:
Possibly Marketed Outside US
Source:
Unknown by Eykman, J.F.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



α-Asarone is a phytochemical compound with neuroprotective, anti-oxidative, anticonvulsive and cognitive enhancing action, isolated from the Chinese medicinal herb Acorus tatarinowii. Numerous clinical studies in China had indicated the effectiveness of α-asarone against respiratory disorders and epilepsy. Asarone tablets have been clinically used as bronchial asthma and bronchitis prescription drug in China. Unfortunately, toxic and genotoxic studies of a-asarone have indicated that this compound may pose a risk to human health, including embryotoxicity and maternal toxicity in rats, hepatotoxicity in rat-cultivated hepatocytes, and in vivo and in vitro genotoxic damage in mammalian cells.
Fenproporex is a central and indirect-acting sympathomimetic. It was developed as an anorectic drug. Their anorectic effects are believed to be a result of adrenergic activation. Fenproporex has never been approved by the US Food and Drug Administration (FDA) for sale in the US due to lack of efficacy and safety data. There is a paucity of randomized, placebo-controlled trials on Fenproporex. These studies suggest that Fenproporex is modestly effective in promoting weight loss. Data from these studies are insufficient to determine the risk-benefit profile of Fenproporex. Abuse potential and amphetamine-like adverse effects are causes for concern. Adverse effect most frequently reported are: insomnia, anxiety, depression, irritability, dry mouth.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Casopitant (GW679769) is a novel substituted piperidine derivative that competitively binds with NK1 receptors. The full occupancy of the receptor by their piperidine compound inhibits its binding with tachykinin neurotransmitters, including SP. Casopitant, in a series of in vitro and in vivo experimentations, has exhibited a potent NK1 receptor antagonism. On 29 May 2008, GlaxoSmithKline announced the submission of a new drug application to the FDA for intravenous and oral formulations of casopitant mesylate. This drug was proposed for the prevention of chemotherapy-induced nausea and vomiting as an add-on therapy to the standard dual therapy of 5-HT3 receptor antagonists + dexamethasone. The submission also included a proposed indication for postoperative nausea and vomiting prevention. Rezonic™ is the proposed trade name for casopitant mesylate in the United States; Zunrisa™ is the proposed trade name for casopitant mesylate for GlaxoSmithKline’s global group of companies. In September 2009, GlaxoSmithKline decided to discontinue all regulatory filings for casopitant based on an estimate of the amount of additional safety data.
Laquinimod is a new orally available carboxamide derivative, which is currently developed for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases. The mechanism of action of laquinimod is not fully elucidated because the molecular target is not known. Treatment with laquinimod led to a significant and persistent increase in brain-derived neuroprotective factor (BDNF) serum levels compared to placebo treatment. In human studies, a decrease of pro-inflammatory and an increase of anti-inflammatory cytokines have been measured. After commercial launch the unexpected severe cardiac adverse events (AEs) such as serositis, pericarditis, and myocardial infarction were detected.
Menthyl lactate is derived from menthol, a compound that comes from peppermint oil, or is made synthetically. Menthol has a natural cooling effect, which makes it useful as a topical analgesic to treat skin irritation, pain, itching or sunburn. Despite its cooling benefits, menthol can be a skin irritant. Like menthol, menthyl lactate is cooling, but it causes less skin irritation than menthol. Menthyl lactate also has a refreshing, minty taste. For this reason, some manufacturers use it as a flavoring ingredient. The compound is recommended for use as a flavor in concentrations of 0.005% to 0.2% and in cosmetic and other external products in concentrations ranging from 0.2% to 2.0%. Menthyl lactate is a known compound available e.g. from Haarmann & Reimer GmbH (Germany) under the name FRESCOLAT, Type ML.