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

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Showing 901 - 910 of 39119 results

Enrasentan is an orally active mixed endothelin A/B receptor antagonist with a 100-fold greater affinity for the endothelin A receptor. In an animal model of hypertension and cardiac hypertrophy the drug has reduced blood pressure, prevented cardiac hypertrophy and preserved myocardial function. In rats with hyperinsulinemia and hypertension enrasentan normalized blood pressure and prevented cardiac and renal damage. In rats with stroke the drug reduced the ischemic area in the brain. Enrasentan had been in phase II clinical trial for the treatment of heart failure but the results suggested that enrasentan does not appear to have favorable effects on ventricular remodeling.
Status:
Investigational
Source:
INN:etersalate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Etersalate is a derivative of aspirin exerting antiplatelet, analgesic, anti-inflammatory and antipyretic properties. Etersalate has potential to prevent oligomerization of amyloid beta (Aβ) peptides.
Status:
Investigational
Source:
INN:cefcanel daloxate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefcanel is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcanel is active against the species E. coli, K. aerogenes and Proteus mirabilis; H. influenzae and M. catarrhalis has reasonable susceptibility. Cefcanel inhibits 90% of S. aureus strains at 2 µg/ml, irrespective of the presence of a β-lactamase. Cefcanel binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
Status:
Investigational
Source:
INN:livoletide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Livoletide (AZP-531) is an analog of unacylated ghrelin, a naturally occurring hormone that is thought to counteract the effects of acylated ghrelin. The drug was designed to improve glycaemic control and reduce weight. Livoletide participated in pivotal phase 2b/3 clinical study for the treatment of Prader-Willi syndrome. In addition, the drug was studied in patients with type 2 diabetes mellitus (T2D). Its pharmacokinetic profile, suitable for once daily dosing, and metabolic effects support further clinical development for T2D.
Status:
Investigational
Source:
INN:meseclazone [INN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Meseclazone (W-2395) is a non-steroidal anti-inflammatory drug. It exerts anti-inflammatory, analgesic and antipyretic activity. Meseclazone inhibits in vitro and ex vivo platelet aggregation initiated by the release reaction. It inhibits bradykinin-induced bronchospasm.
Status:
Investigational
Source:
INN:palmoxiric acid
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
JAN:OMECAMTIV MECARBIL HYDROCHLORIDE HYDRATE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure (in Phase 2 of development). Omecamtiv mecarbil is an inotropic agent that prolongs systolic ejection time and increases ejection fraction through myosin ATPase activation.
Status:
Investigational
Source:
INN:cemadotin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Cemadotin (LU103793) is a cytotoxic water-soluble pentapeptide analogue of dolastatin 15. The dolastatin peptides were originally isolated from the shell-less mollusc Dolabella auricularia. Cemadotin blocks cells at mitosis. It exerts its antitumor activity by suppressing spindle microtubule dynamics through a distinct molecular mechanism by binding at a novel site in tubulin. Cemadotin was in phase II clinical trials as a promising cancer chemotherapeutic agent. However, this agent appears to be inactive in the treatment of advanced non-small-cell lung cancer and other tumors and this research has been discontinued.
Status:
Investigational
Source:
INN:fasobegron [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Fasobegron is an agonist of β3-adrenoreceptor.
Status:
Investigational
Source:
INN:ciadox
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ciadox is Quinoxaline 1,4-dioxide derivative with antimicrobial and promoting activities. Cyadox supplied as premix in the final feed in Eastern Europe and may be used in pigs up to four months of age. Some evidence demonstrated that the mechanism of Ciadox for improving pig growth performance was correlated with several metabolic hormones and growth factors. Cyadox also did not show any adverse effects in carcinogenicity tests with rats and long-term toxicity tests with mice and rats. Cyadox subchronic oral toxicity evaluation shows mild toxicity in non-rodents animals. Metabolic transformation of Ciadox leads to three major metabolites, including 1,4-bisdesoxycyadox, 4-desoxycyadox, and quinoxaline-2-carboxylic acid. Ciadox and metabolites shows virtually no toxic effects in the acute and subchronic oral toxicity study and no mutagenic, carcinogenic activivt.