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

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Showing 9391 - 9400 of 10822 results

Status:
Investigational
Source:
INN:rocastine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Rocastine (AHR-11325) is a potent, nonsedating antihistamine with a rapid onset of action. This H1-antagonist effectively protected guinea pigs challenged with a lethal dose of histamine. It has also been mentioned in patents as a candidate to treat eye conditions and cough/cold mixtures (in which the lack of sedative effects from a non-sedating antihistamine would be especially useful in children, because daytime sedation is especially undesirable in this group). However, information on current use is not available and other second-generation, non-sedative antihistamines are available.
Status:
Investigational
Source:
Vet Res Commun. Jan 2008;32(1):75-92.: Not Applicable Veterinary clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

(E)-Tetrachlorovinphos is an (E)- isomer of Tetrachlorovinphos. Tetrachlorovinphos is an organophosphate cholinesterase inhibitor that is used as an insecticide. Tetrachlorvinphos was introduced and first used commercially in 1966 in the USA. Tetrachlorvinphos was originally registered for use on various food crops, livestock, pet animals. Tetrachlorvinphos is applied dermally to livestock to control flies and mites. It is used as an oral larvicide in cattle, hog, goats and horses; in cattle ear tags to control flies; in cattle feedlots; in poultry dust boxes to control poultry mites; and in poultry houses. Tetrachlorvinphos also is used in pet sleeping areas and pet flea collars and to control flies around refuse sites, recreational areas, and for general outdoor treatment. Tetrachlorvinphos can cause cholinesterase inhibition in humans; that is, it can overstimulate the nervous system causing nausea, dizziness, confusion, and at very high exposures (e.g., accidents or major spills), respiratory paralysis and death. In 2014, the Natural Resources Defense Council (NRDC) filed a lawsuit against the United States Environmental Protection Agency (EPA) seeking EPA to respond to NRDC’s 2009 petition to ban tetrachlorvinphos in common pet flea treatment products. Tetrachlorvinphos is reportedly registered for use in Canada, South Africa, and Australia.
Status:
Investigational
Source:
NCT00697879: Phase 1 Interventional Completed Solid Tumor
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02423408: Phase 2 Interventional Completed Tension-Type Headache
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

ISOMETHEPTENE, (R)- is an antimigraine drug candidate, which development was discontinued in 2016. It is a potent agonist of the imidazoline-1-receptor.
Status:
Investigational
Source:
NCT00932126: Phase 1 Interventional Terminated Advanced Solid Tumors
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



PF-3758309 was developed as an ATP-competitive inhibitor of PAK4. In cells, PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM). PF-3758309 blocks the growth of multiple human tumor xenografts, with a plasma EC50 value of 0.4 nM in the most sensitive model. PF-3758309 is antiproliferative and induces apoptosis in an HCT116 tumor model.
Status:
Investigational
Source:
NCT01052012: Phase 3 Interventional Completed Postoperative Pain
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Lambda-cyhalothrin (λ-cyhalothrin), a mixture of isomers of cyhalothrin belongs to a class of insecticides known as synthetic pyrethroids. Synthetic pyrethroids are often preferred to the real thing as an active ingredient because they offer the added bonus of remaining effective for longer period. λ-cyhalothrin was the most commonly used pyrethroid insecticide for vegetable farming in Benin. Experiments have shown that λ-cyhalothrin residues in lettuce and cabbage from farms and markets in Parakou and Cotonou were relatively safe for consumption.
Status:
Investigational
Source:
NCT04017546: Phase 1 Interventional Completed AML
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:niguldipine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

S-(+)-niguldipine is a more active enantiomer and is a selective antagonist for the and α1A-adrenoceptor. In addition, it can be used for discriminating of alpha 1A- from alpha 1B-adrenoceptors. There were made attempts to investigate the antidepressant action of S-(+)-niguldipine on rats, but that studies were unsuccessful.
Status:
Investigational
Source:
INN:pranolium chloride
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


Pranolium (UM-272) is propranolol derivative. It can reduce the extent of myocardial injury sustained during severe ischemia. UM-272 lacks significant beta-adrenergic blocking activity but retains the negative chronotropic, negative inotropic and antiarrhythmic effects common to both d- and l-propranolol. The protective effects of UM-272 during myocardial ischemia cannot be due to metabolic effects of the beta-adrenergic blockade but may be due to effects on oxygen consumption or to effects on myocardial membrane properties that are related to its antiarrhythmic and myocardial depressant activity. The ability of UM-272 to enhance blood flow to subendocardial myocardium may also play a role in its beneficial effects during ischemia. UM-272 may protect the ischemic heart through direct effects on myocardial Ca++ regulating mechanisms. UM-272 has kinetically similar use-dependent inhibitory action of the fast sodium channels of cardiac muscles as other Class Ia antiarrhythmic drugs like quinidine or procainamide. Pranolium was investigated as an antiarrhythmic agent.
Status:
Investigational
Source:
INN:pranolium chloride
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


Pranolium (UM-272) is propranolol derivative. It can reduce the extent of myocardial injury sustained during severe ischemia. UM-272 lacks significant beta-adrenergic blocking activity but retains the negative chronotropic, negative inotropic and antiarrhythmic effects common to both d- and l-propranolol. The protective effects of UM-272 during myocardial ischemia cannot be due to metabolic effects of the beta-adrenergic blockade but may be due to effects on oxygen consumption or to effects on myocardial membrane properties that are related to its antiarrhythmic and myocardial depressant activity. The ability of UM-272 to enhance blood flow to subendocardial myocardium may also play a role in its beneficial effects during ischemia. UM-272 may protect the ischemic heart through direct effects on myocardial Ca++ regulating mechanisms. UM-272 has kinetically similar use-dependent inhibitory action of the fast sodium channels of cardiac muscles as other Class Ia antiarrhythmic drugs like quinidine or procainamide. Pranolium was investigated as an antiarrhythmic agent.

Showing 9391 - 9400 of 10822 results