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

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Showing 621 - 630 of 21518 results

Status:
Investigational
Source:
INN:lotucaine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Lotucaine is a local anesthetic.
Status:
Investigational
Source:
INN:clemeprol [INN]
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Clemeprol is an antidepressant drug of the 3,3-diraylpropyl-amine type. It exhibits antireserpine activity in animal tests, inhibits the neuronal uptake of noradrenaline. The drug was used in the clinic for the treatment of depression in the 1980s, but no development was reported since.
Status:
Investigational
Source:
INN:tigestol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tigestol is an Estrene derivative patented by Organon Laboratories Ltd. as an anabolic, androgenic, and progestative agent.
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: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:
NCT01108913: Phase 2 Interventional Completed Chronic Obstructive Pulmonary Disease
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Bimosiamose, discovered by Encysive Pharmaceutical and presently being developed by Revotar Biopharmaceuticals, is an 863 g/mol molecular weight dimer with minimal carbohydrate content and is, to date, the leading selectin inhibitor in clinical development. It was developed as anti-inflammatory drug fir the treatment of acute chronic inflammatory disorders including COPD. This compound has shown promise in a phase IIa 'proof of concept' trial in patients with asthma, reducing airway recruitment of eosinophils after intravenous administration. In acute lung injury, neutrophils (a type of white blood cells, thus belonging to the group of cells of the body’s defence system-the immune system) are drawn to the small lung bloodvessels and migrate into the air sacs (alveoli). There they release substances, which cause the inflammation leading to further destruction of the lung tissue. Bimosiamose disodium is expected to hinder the migration of these neutrophils into the alveoli.
Status:
Investigational
Source:
INN:betacetylmethadol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Betacetylmethadol is a synthetic narcotic analgesic under international control according to the UN Single Convention 1961.
Status:
Investigational
Source:
NCT01591655: Phase 3 Interventional Completed Cataract
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Mapracorat (BAY-865319, BOL-303242-X or ZK-245186) is a selective non-steroid glucocorticoid receptor agonist exerting anti-inflammatory activity. Mapracorat showed partial attenuation of the classical NF-κB pathway, consistent with traditional steroids. However, mapracorat uniquely potentiated a novel anti-inflammatory mechanism through rapid upregulation of RelB, an anti-inflammatory member of the NF-κB alternative pathway. Mapracorat was being studied in the treatment of ocular and skin inflammatory diseases.
Status:
Investigational
Source:
NCT03348527: Phase 2 Interventional Completed Prostate Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Hydroxyflutamide is the major active metabolite of flutamide. Flutamide undergoes extensive first-pass metabolism by CYP1A2 to its metabolite hydroxyflutamide and its hydrolysis product, 3-trifluoromethyl-4-nitroaniline. Hydroxyflutamide is a more powerful antiandrogen in vivo, with higher affinity for the receptor than that of flutamide. Hydroxyflutamide is in phase II clinical trials for the treatment of prostate cancer. However, a drug resistance problem appears after about one year's treatment. Per-residue free energy decomposition analyses indicate that N705, T877, and M895 androgen receptor mutations are vital residues in the agonist/antagonist mechanism of hydroxyflutamide.
Status:
Investigational
Source:
INN:pytamine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Pytamine is a nitrosamine derivative patented by Hercules Powder Co. as antioxidants, stabilizers, rubber additives, insecticides, fungicides, bactericides, and pharmaceutical intermediates. In preclinical trials Pytamine shows potent psychotropic effects associated modulation of GABAA receptors.