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

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Showing 631 - 640 of 4697 results

Status:
Investigational
Source:
INN:iganidipine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Iganidipin is a new dihydropiridynic derivative of calcium antagonist. It is the only currently available calcium antagonist in the form of ophthalmic solution. Its topical administration increases ipsilateral optic nerve head blood flow in rabbits and monkeys and inhibits the contraction of blood vessels induced by endothelin -1. Iganidipin is also used for treat Angina pectoris and Hypertension.
Status:
Investigational
Source:
INN:lozilurea [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Lozilurea (N' -3-chlorobenzyl-N'-ethylurea, ITA 312) has shown marked anti-ulcer activity. It has shown itself to be active against chemically and neurogenically induced gastric and duodenal lesions in various experimental animal models. It has no major anti-secretory action. The experimental data obtained suggest that the mechanism of action of lozilurea consists in increasing the protective function of the mucus barrier. It increased gastric levels of hexosamines and mucoproteins. In the screening trials carried out in order to detect the side effects of lozilurea, it has shown sedative, antipyretic and vasodilatory actions.
Status:
Investigational
Source:
INN:cinflumide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Cinflumide is a cinnamamide derivative manufactured by Burroughs Wellcome Co. It is claimed to be a CNS voluntary muscle relaxant.
Status:
Investigational
Source:
INN:tetronasin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tetronasin is a furanone derivative patented by Imperial Chemical Industries Ltd. as antibiotic and feed additive for ruminants. Tetronasin acts as divalent antiporter that binds preferentially with Ca2+ or Mg2+ and inhibits anaerobic fungi and Gram-negative bacteria in vitro.
Status:
Investigational
Source:
JAN:MAFOPRAZINE MESILATE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Mafoprazine is a phenylpiperazine derivative exerting postsynaptic dopamine D2 receptor blocking activity and alpha-adrenergic activity (alpha 1 receptor blocking activity and alpha 2 receptor stimulating activity). In animal models, mafoprazine demonstrated antipsychotic, aggression-inhibiting and cataleptogenic actions.
Rubitecan [Orathecin™] is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral compound being developed for the treatment of pancreatic cancer and other solid tumours by SuperGen. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks.
Status:
Investigational
Source:
NCT00505076: Phase 2 Interventional Completed Schizophrenia
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

MK 0777 is a selective GABAA α2/3 receptor partial agonist, for potential use in the treatment of Schizophrenia, Anxiety Disorder, and Generalized Anxiety Disorder. MK-0777 is functionally selective for the α2 and α3 subunits, with virtually no activity for the α1 and α5 subunits. Therefore, MK-0777 cause less sedation, interact less with alcohol, and exhibit less abuse potential and physical dependence than benzodiazepines. Unfortunately, in clinical trials, MK-0777 has little benefit for cognitive impairments in people with schizophrenia and anxiety disorder.
Status:
Investigational
Source:
INN:ormaplatin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Ormaplatin (NSC 363812, tetraplatin) is a stable platinum (IV) analog. Ormaplatin alkylates DNA, forming both inter- and intra-strand platinum-DNA crosslinks, which result in inhibition of DNA replication and transcription and cell-cycle nonspecific cytotoxicity. Ormaplatin showed marked antitumor activity both in vitro and vivo. The severe, cumulative and irreversible peripheral neurotoxicity observed in phase I studies resulted in termination of further clinical development of ormaplatin.
Status:
Investigational
Source:
JAN:ECABAPIDE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Ecabapide (DQ 2511) is a compound with antiulcer and gastroprokinetic activity. Evidence from basic studies in animal models suggests that the drug acts on peripheral mechanisms of neural control. In the stomach, ecabapide acts to suppress firing in vagal afferent nerves and thereby reduce the flow of sensory information into the dorsal vagal complex. The mechanism of action of ecabapide in suppressing discharge in vagal afferent terminals appears to mimic that of nitric oxide by stimulating formation of cGMP and activation of an inhibitory transduction cascade in the sensory fibres. In this respect the mechanism of its pro-kinetic action differs from other promoter agents. Ecabapide development has been discontinued.
Status:
Investigational
Source:
INN:pincainide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pincainide is a new beta-amino anilide with local anesthetic properties. It has been shown to be 3 times more potent than lidocaine as a local anaesthetic on desheathed frog sciatic nerve. It was found to be effective against arrhythmias induced in guinea-pigs by ouabain infusion or by administration of adrenaline and chloroform. Pincainide not only inhibited the influx of Ca 2+ and increased 45Ca efflux, thus reducing the contractile responses induced in rat aorta by noradrenaline and high K +, but it also inhibited other effects related to the noradrenaline-induced release of intracellular Ca 2+ stores. Further studies, however, must be performed in experimental models of arrhythmias before the effectiveness of pincainide as an antiarrhythmic drug can be established.