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

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Showing 641 - 650 of 13501 results

Ensaculin is related to naturally occurring benzopyranones like scoparone. The compound is a potent functional antagonist of excitatory amino acid-induced convulsions and mortality. In receptor-binding studies, Ensaculin showed high affinity to dopaminergic (D2, D3), serotoninergic (5-HT1A, 5-HT7), and adrenergic (A1a, A1b) receptors in the nanomolar range. Ensaculin antagonizes NMDA responses in a voltage-dependent manner. Various studies support the notion that this compound could indeed have a broad range of nootropic properties. Although few patients presented postural hypotension and dizziness after receiving ensaculin in phase I clinical trials, this drug candidate was further discontinued in phase III due to potential side effects.
Status:
Investigational
Source:
INN:etazepine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Etazepine (5,6-dihydro-5-methyl-11H-11-ethoxy-dibenzo[b,e]azepin-6-one) demonstrates anticonvulsant activity in rodents. Etazepine seems to exert its anticonvulsant effects by activating the GABAergic system.
Status:
Investigational
Source:
INN:vinpoline
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Vinpoline was studied as a central stimulant. Information about the further development of this agent is not available.
Status:
Investigational
Source:
INN:oxiperomide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxiperomide was developed as a dopamine-receptor antagonist. Clinical trials have shown that this drug decreased dyskinesia in patients with Parkinson's disease receiving levodopa or other dopamine agonists without necessarily increasing Parkinsonian symptoms. However, information about the further development of this drug is not available.
Status:
Investigational
Source:
INN:melizame [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Melizame is a sugar substitute for sweetening caloric or noncaloric materials.
Status:
Investigational
Source:
INN:pirtenidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pirtenidine is the antimicrobial agent. Pirtenidine was found to be highly efficacious against oral plaque-forming microorganisms. Adherence of Candida spp. to buccal epithelial cells in vitro was significantly reduced after both short- and long-term periods of yeast exposure to sub-inhibitory concentrations of pirtenidine. The drug was shown to cause extensive leakage of cytoplasmic contents from the Candida albicans cells which was correlated with morphological and ultrastructural changes in the yeast. Pirtenidine affects the lipids and sterol composition of C. albicans.
Status:
Investigational
Source:
INN:taltrimide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Taltrimide, a taurine derivative that was developed as an anticonvulsive agent. Taltrimide strongly inhibits the sodium-independent binding of taurine to synaptic membranes of the brain and it does not appear to bind to GABAA and benzodiazepine receptor. The drug was studied in phase II clinical trial Finland as an anticonvulsant agent to treat epilepsy. However, the further development of this drug was discontinued.
Status:
Investigational
Source:
INN:octabenzone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Octabenzone is a UV absorber/screener. It is used to protect polymers (e.g., polyethylene, polypropylene, polyvinylchloride) against damage by UV light.
Status:
Investigational
Source:
INN:libecillide
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Libecillide is a specific monovalent penicilloyl hapten inhibitor of allergic reactions to penicillin. A depression of skin hypersensitivity to PPL and/or penicillin and penicillin derivatives sometimes persisting for weeks and months was obvious in numerous allergic patients submitted to combined libecillide-penicillin treatment. A depressing effect on antipenicillin antibody titers detected by passive hemaglutination was also manifest in some patients. The overall tolerance of libecillide in allergic patients has been very good. Nevertheless, the major obstacle to a wider general use of libecillide at the present time appears to be the occurrence of positive skin reactions to that compound in approximately 5 percent of patients allergic to penicillin.
Status:
Investigational
Source:
NCT01429623: Phase 2 Interventional Completed Mild Cognitive Impairment
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LADOSTIGIL, a rasagiline derivative, is a reversible acetylcholinesterase and butyrylcholinesterase inhibitor with neuroprotective properties. It also acts as an irreversible brain monoamine oxidases inhibitor. It is under development for the treatment of neurodegenerative disorders like dementia and Alzheimer's disease.