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

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Showing 121 - 130 of 1114 results

Status:
Investigational
Source:
NCT00124696: Phase 1 Interventional Completed Cocaine-Related Disorders
(2002)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cocaethylene is the ethyl ester of benzoylecgonine. Cocaethylene is formed in the liver after concurrent use of cocaine and alcohol. Cocaethylene works by blocking the dopamine transporter on dopaminergic presynaptic nerve terminals in the brain. It increases dopamine synaptic content, provoking enhanced postsynaptic receptor stimulation, resulting in euphoria, reinforcement, and self-administration. Compared to cocaine, which is a methyl ether of benzoylecgonine, cocaethylene has three to five times larger half-life in plasma. Cocaethylene is associated with seizures, liver damage and compromised the functioning of the immune system. It carries an 18-25 fold increase in risk for immediate death compared to cocaine alone.
Status:
Investigational
Source:
INN:diflumidone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Diflumidone is a non-steroidal antiinflammatory drug. It inhibits the biosynthesis of prostaglandin by bovine seminal vesicle microsomes and arachidonic acid-induced aggregation of human platelets in a concentration-dependent manner. Diflumidone is a competitive inhibitor of prostaglandin synthetase. Diflumidone also inhibits equally the formation of PGE2 and PGF2a, which suggests blockade of endoperoxide formation. The relative topical efficacy of indomethacin and diflumidone for the suppression of ultraviolet-light-induced erythema has been compared in a randomized, double-blind, placebo-controlled study in man. At 24 h after application, the indomethacin-treated sites had significantly less erythema than did the diflumidone-treated sites.
Status:
Investigational
Source:
INN:osanetant
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Osanetant (SR-142801) is a NK3 receptor antagonist, it has a higher affinity for human and guinea pig NK3 receptors than for rat NK3 receptors. Osanetant was under development for the treatment of schizophrenia and other Central Nervous System (CNS) disorders. It was developed by Sanofi-Aventis (formerly Sanofi-Synthelabo). Sanofi was originally investigating its potential use as a treatment for psychosis and anxiety. Following phase IIa clinical trials, osanetant entered phase IIb development in February 2001. In a review of its R&D portfolio, the company announced in August 2005 that it would cease any further development of osanetant. This follows an earlier decision to discontinue development of eplivanserin for schizophrenia.
Status:
Investigational
Source:
INN:tulopafant
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tulopafant [RP 59227] is a platelet-activating factor (PAF) antagonist which was being developed by Rhône-Poulenc Rorer as an antiasthmatic agent. Double-blind, placebo-controlled clinicacl trial showed that RP 59227 attenuated the release of NCA and ECA after antigen challenge, and reduced the effect of exogenously added PAF in inducing eosinophil chemotaxis but did not protect against the antigen-induced early or late phase response in asthmatics. RP 59227 has also been shown to effectively reduce myocardial infarct size and the incidence of ischemia and reperfusion-induced arrhythmias in barbital-anesthetized dogs. Development of Tulopafant for asthma treatment has been discontinued.
Status:
Investigational
Source:
INN:triflumidate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Triflumidate is a fluoroalkanesulfonanilide. It had been identified for clinical trials. This non-steroidal compound is an anti-inflammatory agent.
Status:
Designated
Source:
FDA ORPHAN DRUG:865621
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)