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

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Showing 1851 - 1860 of 167129 results

Status:
Investigational
Source:
INN:femoxetine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Femoxetine is a selective serotonin re-uptake inhibitor. It was being studied in the treatment of narcolepsy, migraine, depressive states and eating disorder. Femoxetine development has been discontinued.
Status:
Investigational
Source:
INN:carsatrin [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Carsatrin (also known as RWJ 24517) is purinylpiperazine derivative patented by Ortho Pharmaceutical Corp. as cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+,K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbine, or prazosin
Status:
Investigational
Source:
INN:dibupyrone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dibupyrone is an analgesic agent.
Status:
Investigational
Source:
NCT00621270: Phase 2 Interventional Completed Major Depressive Disorder
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Coluracetam (code name BCI-540; formerly MKC-231) is a nootropic agent of the racetam family. It was initially developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer's disease. After the drug failed to reach endpoints in its clinical trials it was in-licensed by BrainCells Inc for investigations into major depressive disorder (MDD). Like most racetam compounds, Coluracetam increases choline uptake, but it also increases uptake in damaged neurons. Specifically, Coluracetam interacts with the HACU process, which is responsible for absorbing choline into the neurons. This increased uptake occurs during the Acetylcholine synthesis process. Since Coluracetam improves choline preservation during this process, a larger amount is converted into Acetylcholine. This results in increased memory, attention and alertness. It is important to note here, that these benefits were only seen in subjects with previously impaired neurons, not in subjects with normally functioning neurons. Coluracetam is also shown to improve AMPA potentiation, which is a process that triggers cognitive function and alertness. Although Coluracetam interacts with choline transporters as well, there isn’t enough evidence to explain why or how this interaction occurs, or what occurs after the interaction. Coluracetam has been in phase II clinical trials for the treatment of major depression and anxiety. However, this research has been discontinued.
Status:
Investigational
Source:
INN:lofendazam
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Lofendazam is partial benzodiazepine agonist. It has been widely tested as a psychotherapeutic drug. In particular, as an anxiety treatment agent.
Status:
Investigational
Source:
INN:dazepinil [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Dazepinil (HRP 543) is a 1,3-benzodiazepine antidepressant, developed by Hoerscht in the early 1980s. In mouse tests, dazepinil inhibited tetrabenazine-induced ptosis and potentiated yohimbine toxicity. In vitro, dazepinil inhibited norepinephrine and serotonin uptake into rat brain synaptosomes and lacked anticholinergic activity.
Status:
Investigational
Source:
INN:linopristin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Linopristin is a chemically modified form of quinupristin. It is an antibiotic of the streptogramin B class. It is one of the components of the antibiotic combination NXL103 (XRP 2868). NXL-103 is a combination of streptogramin A:streptogramin B components, initially developed in a 70:30 dose ratio. In multiple in vitro studies, NXL-103 demonstrated potent activity against different types of bacteria, such as Staphylococcus aureus (including MRSA), Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecium, Enterococcus faecalis, Haemophilus influenzae and Haemophilus parainfluenzae. In phase I clinical trials, NXL-103 achieved bactericidal levels in plasma and was generally well tolerated, with side effects primarily on the gastrointestinal system. The first phase II trial conducted to evaluate the efficacy of NXL-103 against community-acquired pneumonia revealed that the compound was comparable with amoxicillin. NXL-103 has promise to become an important agent in the treatment of community-acquired pneumonia and complex skin and soft tissue infections, pending further development.
Status:
Investigational
Source:
NCT00113893: Phase 2 Interventional Completed Bone Marrow Diseases
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Talmapimod is a p38 MAPK kinase inhibitor that inhibits p38 alpha with IC50 value of 9 nM which is 10-times lower then IC50 for p38 beta. Talmapimod was under clinical development for the treatment of Myelodysplastic Syndromes, Multiple Myeloma and Rheumatoid Arthritis (phase II), however, it seems to be discontinued as no longer presents in Janssen's pipeline.
Status:
Investigational
Source:
NCT01082471: Phase 3 Interventional Completed Postoperative Pain
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Morphine-6-glucuronide is a pharmacologically active metabolite of morphine that is being developed by CeNeS Pharmaceuticals as an alternative to morphine for the management of postoperative pain. Compared to morphine, Morphine-6-glucuronide has been reported to have6 and 86 times lower affinity for the human mu and kappa opioid receptors, respectively, and similar affinity for the delta opioid receptor. Morphine-6-glucuronide is was studied in phase III clinical trials for postoperative pain management. Unfortunately, Morphine-6-glucuronide failed to demonstrate superior safety compared to Morphine and further development was discontinued. Morphine-6-glucuronide accumulates after administration of morphine to patients with renal insufficiency, and analgesia can be obtained with lower doses of morphine compared to patients with normal renal function. More importantly, the dose should be reduced to avoid serious side-effects, although the simulations in this review did not account for side-effects.
Status:
Investigational
Source:
INN:levofuraltadone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levofuraltadone is the nitrofurane used for the treatment of trypanosomiasis. It has been shown to be effective in mice and polyneuritis, a serious side effect of nitrofurazone therapy, is less frequent with levofuraltadone. Nevertheless, levofuraltadone is a very toxic agent and it has never been commercially produced.

Showing 1851 - 1860 of 167129 results