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

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Showing 791 - 800 of 11247 results

Status:
Investigational
Source:
INN:gemopatrilat
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Gemopatrilat is a vasopeptidase inhibitor, that was found to inhibit plasma and renal angiotensin converting enzyme (ACE), as well as renal neutral endopeptidase (NEP). Gemopatrilat is rapidly absorbed, and causes inhibition of circulating and renal ACE and renal NEP after a single oral dose for up to 48 hours in rats. Potentially, this is because the free sulfhydryl group of gemopatrilat forms reversible disulfide linkages with plasma and tissue proteins and is thus eliminated from the body at a very slow rate. Similar metabolism of the compound was found in rat, dog, and human. Gemopatrilat was evaluated for its potential in treatment of antihypertensive activity in hypertension (independent of age, renin and salt status or ethnic origin), as well as its potential as a new therapeutic modality for the treatment of congestive heart failure. The drug was never marketed. A phase II study for treatment of hypertension and heart failure has been discontinued.
Status:
Investigational
Source:
INN:prazocillin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Prazocillin is 6-aminopenicillanic acid derivative patented by Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt. as a bactericidal compound. The activity of Prazocillin against Staphylococcus aureus strains was the same as that of dikloxacillin, but Prazocillin was more active against Bacillus subtilis ATCC 6633. Prazocillin had a bactericidal effect on a penicillin-resistant S. aureus strain at concentrations of 1 μg/ml. Pyrazocillin inhibits bacterial penicillinase in vitro.
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:
NCT04905654: Not Applicable Human clinical trial Completed Migraine with Aura
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cromakalim is an ATP-sensitive potassium (KATP) channel opener, which was studied for the treatment of gastric ulcer, hypertension and preventing a cardiomyopathy. But the development of this drug was discontinued due to heart lesions found in monkey chronic toxicity studies.
Status:
Investigational
Source:
INN:suritozole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Suritozole (also known as MDL 26,479) is an aryldialkyltriazolethione derivative patented by Merrell Dow Pharmaceuticals, Inc as an antidepressant. Suritozole acts as negative modulator at the gamma-aminobutyric acid A (GABAA) receptor that enhances cholinergic function. In preclinical models, chronic treatment Suritozole produces a small but significant decrease in the average spontaneous firing rate of Purkinje neurons. Suritozole attenuated a scopolamine-induced acquisition deficit in a T-maze reinforced alternation task, suggesting that the compound may have memory enhancing potential.
Status:
Investigational
Source:
INN:deramciclane [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Deramciclane is camphor derivative. It is an anxiolytic agent that binds with high affinity to 5-HT2A/2C receptor. Deramciclane showed significant evidence of efficacy for the treatment of generalized anxiety disorder in adult patients. A single dose of deramciclane was rapidly absorbed with peak plasma concentrations being reached after about 3 h. Deramciclane has a half-life of around 27 h. The most commonly reported adverse event was headache. In the in vitro studies deramciclane concentration-dependently inhibited NMDA evoked spreading depression.
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:
NCT00491543: Phase 2 Interventional Completed Diabetes
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

ALT-2074 (SYI 2074) is small molecule organoselenium compound which acts as a glutathione peroxidase mimetic. Like native glutathione peroxidase, ALT-2074 catalyzes the reduction of hydroperoxides to less toxic species using glutathione (GSH) as the reducing agent. The hydroperoxides could otherwise lead to the formation of free radicals, which can cause tissue damage. ALT-2074 also down-regulates the gene transcription which leads to the production of a wide array of inflammatory mediators. GPx mimics such as BXT-51072 behave as potent antagonists of TNF-alpha and interleukin-1 through the downregulation of endothelial proinflammatory responses. ALT-2074 was investigated for use/treatment in cardiovascular disorders, diabetes mellitus type 1 and 2, plaque psoriasis, ulcerative colitis.
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:
Am J Surg. Nov 1978;136(5):600-5.: Not Applicable Human clinical trial Completed Urethral Stricture
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

3-Aminopropionitrile (beta-aminopropionitrile, BAPN) is a poisonous substance found in Lathyrus spp. (wild peas), for example, Lathyrus hirsutus (wild winter pea), sometimes sown with grasses to provide early-spring grazing. BAPN is a specific and irreversible inhibitor of LOX activity. It has been shown to reduce body weight gain and improve the metabolic profile in diet-induced obesity in rats. The administration of beta-aminopropionitrile has been proposed for pharmacological control of unwanted scar tissue in human beings. BAPN has been shown to have preventive effect in the development of fibrosis by decreasing tissue damage in an experimental model of corrosive esophagitis in rats. BAPN is FDA approved for the treatment of tendinitis of the superficial digital flexor tendon (SDFT) in horses where there is sonographic evidence of fiber tearing.