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

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Showing 1191 - 1200 of 13268 results

Status:
Investigational
Source:
INN:pinokalant
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Pinokalant is the isoquinoline derivative. It is a broad-spectrum cation channel blocker which inhibits store-operated cation channels in human endothelial cells, mast cells, HL60 cells and in primary cultures of cortical and hippocampal neurons. Pinokalant inhibits voltage-operated calcium channels of the L- and N-subtypes in primary cultures of cortical neurons and shows some antagonism on the NMDA- and AMPA glutamate receptor subtypes. Pinokalant also acts as an antagonist at the delayed rectifier K+ channel in PC12 cells and cortical neurons. Pinokalant reduced in vivo lesion size as well as post mortem infarct size derived from 2,3,5-triphenyltetrazolium chloride-stained brain slices 24 hr after middle cerebral artery occlusion. Pinokalant has been evaluated as a potential neuroprotectant in rodent models of stroke.
Status:
Investigational
Source:
NCT00080015: Phase 2 Interventional Completed Small Cell Lung Cancer
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Diflomotecan is an E-ring modified camptothecin analogue, which possesses greater lactone stability in plasma compared with other topoisomerase I inhibitors. Diflomotecan was the first homocamptothecin to enter clinical studies. Phase I data are summarized for both the intravenous and oral schedules. The toxicity is primarily haematological while no severe gastrointestinal toxicity has been observed in contrast to other topoisomerase I inhibitors. Diflomotecan has a high oral bioavailability (72 - 95%) and the oral day 1 - 5 every 3 weeks regimen is recommended for Phase II testing because it is relatively well tolerated. Diflomotecan had been in Phase II clinical trials for the treatment of small cell lung cancer. However, this research has been discontinued.
Status:
Investigational
Source:
INN:glisentide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Glisentide (glypentide) is a hypoglycemic agent and part of the second-generation sulfonamide derivatives. Glisentide is used as an oral medication to control blood sugar levels in patients with diabetes mellitus type 2. Glisentide is patented by Uriach as Staticum®. This compound appears to decrease total lipid and cholesterol levels. Results of glisentide administration in humans showed that this oral hypoglycemic drug was well tolerated and had a similar, and in many instances superior, activity to other similar drugs such as glybenclamide and glipizide.
Status:
Investigational
Source:
INN:glisolamide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Glisolamide is a second-generation sulfonylurea with antihyperglycemic activity. Glisolamide is comparable to glyburide and gliquidone in controlling blood glucose levels. It is sold as Diabenor in several countries outside the US.
Status:
Investigational
Source:
INN:halopemide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Halopemide is a new psychotropic agent, a structural analog of the neuroleptics of the butyrophenone type but with different pharmacological and clinical properties. Preliminary clinical findings indicate that halopemide lacks the ability to induce parkinsonism and may be an effective drug in the treatment of psychosis characterized by autism, emotional withdrawal or apathy. However, the results from of the double-blind study showed no significant difference between the placebo phase and halopemide phase. Halopemide is phospholipase D2 inhibitor: PLD1 and PLD2. Halopemide may be used as a screen to identify inhibitors of human PLD2 using an in vitro biochemical assay. It is also inhibitory at benzodiazepine binding sites.
Status:
Investigational
Source:
INN:datelliptium chloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Datelliptium is a DNA-intercalating agent, an analog of a natural alkaloid ellipticine. The compound was active in vivo against a variety of murine solid tumors. In a phase I clinical trial no objective complete or partial responses were observed in patients with solid tumors or lymphoma treated with datelliptium.
Status:
Investigational
Source:
INN:cyclopyrronium bromide
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Cyclopyrronium bromide is an anticholinergic agent, discovered by Robins Company, Inc. Ex vivo study has demonstrated that the compound was effective in inhibiting gastrointestinal motility in isolated guinea pig ileum.
Status:
Investigational
Source:
NCT00203125: Phase 3 Interventional Completed Parkinson's Disease
(2000)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tyramine is a naturally occurring monoamine compound and trace amine derived from the amino acid tyrosine. Tyramine occurs widely in plants and animals, and is metabolized by the enzyme monoamine oxidase. Tyramine is an alpha-adrenergic agonist. Hypertension can occur, from ingestion of tyramine-rich foods in conjunction with monoamine oxidase inhibitors. The possibility that tyramine acts directly as a neurotransmitter was revealed by the discovery of a G protein-coupled receptor with high affinity for tyramine, called TAAR. It exhibits sympathomimetic effects by causing the release of endogenic norepinephrine. It has been used in mydriatic eyedrops. This has been said to reduce the intraocular pressure in rabbits and in some patients with open-angle glaucoma.
Status:
Investigational
Source:
INN:deterenol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Deterenol is a beta-adrenoceptor agonist. It is an effective nonmydriatic and nonmiotic hypotensive agent, which can be used in antiglaucoma treatment.
Status:
Investigational
Source:
INN:bepiastine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Showing 1191 - 1200 of 13268 results