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

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Showing 481 - 490 of 13315 results

Status:
Investigational
Source:
INN:theophylline ephedrine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Theophylline ephedrine is a pharmacologically active salt useful for the treatment of obstructive ventilatory disorders. Theophylline / Ephedrine is used for Wheezing, Shortness of breath, Chest tightness, Interruption of breathing in newborns, Mild and chronic bronchial asthma, Low blood pressure and other conditions.
Status:
Investigational
Source:
NCT02138812: Phase 1 Interventional Terminated Medical Oncology
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Empesertib (previously known as BAY-1161909) was developed as a selective inhibitor of the serine/threonine monopolar spindle 1 (Mps1) kinase for the treatment of cancer. Empesertib participated in phase I clinical trials in combination with paclitaxel in subjects with advanced malignancies. The studies were terminated because another more successful Mps1 inhibitor was being developed in parallel.
Status:
Investigational
Source:
NCT02648178: Not Applicable Interventional Completed Nicotine Dependence, Other Tobacco Product
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT01638403: Phase 3 Interventional Completed Treatment of Excessive Daytime Sleepiness in Narcolepsy
(2010)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Diclobutrazol is the active ingredient of a broad-spectrum systemic fungicide for use on cereals. Diclobutrazol sprays appear promising for the control of coffee rust, apple mildew and scab, grape powdery mildew and various other crop diseases. Diclobutrazol has a systemic action and is translocated mainly acropetally. It eradicative action, increased by vapour effect, is very strong. Diclobutrazol is of low toxicity to mammals and other animals. It is also of low toxicity to birds, fish and invertebrates. Diclobutrazol inhibited spore germination and mycelia growth of a wide range of fungi. Stereoselective inhibition of human CYP3A4 and Candida albicans CYP51 was observed with enantiomers of the azole antifungal compound diclobutrazol. The RR(+) configuration at its asymmetric carbon center was most active.
Status:
Investigational
Source:
NCT01460420: Phase 1/Phase 2 Interventional Completed Hematologic Malignancies
(2011)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

(±)-quinuclidinyl benzilate (3-quinuclidinyl benzilate), is a specific muscarinic cholinergic receptor antagonist. It binds potently but reversibly to the muscarinic cholinergic receptors of mammalian brain and peripheral tissues. 3-quinuclidinyl benzilate was invented by Hoffmann-La Roche Inc in 1951, while investigating antispasmodic agents resembling tropine for the treatment of gastrointestinal conditions. In the 1960s 3-quinuclidinyl benzilate, was developed and weaponized as a new chemical agent for battlefield use as a psychochemical. Assigned the NATO code BZ it is classified as a hallucinogenic chemical warfare agent that affects both the peripheral and central nervous systems (CNS). It is one of the most potent anticholinergic psychomimetics known, with only small doses necessary to produce incapacitation. The primary route of absorption is through the respiratory system but absorption also can occur through the skin or gastrointestinal tract. BZ is odorless and is usually disseminated as an aerosol. Data regarding the health effects of BZ in humans following inhalation exposure are limited to military application studies. Pharmacologic activity of 3-quinuclidinyl benzilate is similar to other anticholinergic drugs (eg, atropine) but with a much longer duration of action. It was shown that I[3H]-3-quinuclidinyl benzilate accumulated in various brain regions after intravenous injection. The specific binding of [3-3H]3-quinuclidinyl-benzilate and [125I]3-quinuclidinyl-(3-iodo-4-hydroxy-benzilate) to rat brain subcellular fractions is parallel in myelin, synaptic plasma membrane and mitochondrial fractions with a 3-4-fold enrichment observed in synaptic plasma membrane over crude mitochondrial fractions. These findings suggested the use of 3-quinuclidinyl benzilate as a binding probe useful in assaying low levels of muscarinic receptor in tissue culture and other biological sources including labeling the receptor in vivo for autoradiographic studies. M2 muscarinic acetylcholine receptor (M2 receptor), essential for the physiologic control of cardiovascular function through activation of G protein-coupled inwardly-rectifying potassium channels, was shown to bind 3-quinuclidinyl benzilate with high affinity in vitro.
Status:
Investigational
Source:
INN:posovolone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02808390: Phase 2 Interventional Terminated Ulcerative Colitis
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02207439: Phase 2 Interventional Completed Head and Neck Squamous Cell Carcinoma
(2014)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Fluoromisonidazole (FMISO) is a small, water-soluble molecule with a molecular weight of 189.14 Daltons. It has an octanol:water partition coefficient of 0.41, so that it would be expected to reflect plasma flow as an inert, freely-diffusible tracer immediately after injection, but later images should reflect its tissue partition coefficient in normoxic tissues. Fluoromisonidazole is used as a positron emission tomography (PET) radiotracer for imaging hypoxia when labeled with fluorine-18. It is the most widely used nitroimidazole imaging agent for use as a non-invasive way to localize and quantify hypoxia.
Status:
Investigational
Source:
J Rheumatol. Oct 1996;23(10):1719-24.: Not Applicable Human clinical trial Completed Lupus Nephritis/metabolism
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03599284: Phase 2 Interventional Completed Coronary Artery Disease
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)