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

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Showing 101 - 110 of 816 results

Status:
Investigational
Source:
NCT00741910: Phase 2 Interventional Completed Crohn's Disease
(2003)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Semapimod (CNI-1493) is a cytokine inhibitor and synthetic guanylhydrazone mitogen-activated protein kinase blocker, is being developed by Cytokine PharmaSciences as a potential treatment for Crohn's disease and other inflammatory conditions. As of December 2001, a phase I study demonstrating the safety of the compound had been completed and phase II trials for psoriasis and Crohn's disease were ongoing. In April 2003, preclinical and early clinical studies were underway for a variety of indications, including congestive heart failure and pancreatitis. Semapimod inhibits activation of p38 MAPK and NF-κB and induction of cyclooxygenase-2 by TLR ligands, but not by IL-1β or stresses. Semapimod inhibits TLR4 signaling (IC50 ≈0.3 umol) and acts by desensitizing cells to LPS; it fails to block responses to LPS concentrations of ≥5 ug/ml. Semapimod had been in phase II clinical trials by Ferring Pharmaceuticals for the treatment of Crohn's disease. However, this research has been discontinued. Semapimod is in phase I clinical trials for the treatment of autoimmune disorders and inflammation.
Status:
Investigational
Source:
INN:eucatropine
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


Conditions:

Eucatropine is known as an anticholinergic agent, which acts as antagonist of muscarinic cholinergic receptors.
Status:
Investigational
Source:
INN:tazomeline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tazomeline (also known as LY 287041), a neuropsychiatric agent, is a muscarinic M1 acetylcholine receptor agonist that was studied in patients with cognitive dysfunction. Tazomeline participated in clinical trials for the treatment of Alzheimer’s disease and dementia. However, all these studied were discontinued for unknown reasons.
Fonturacetam, also known as Phenylpiracetam, is marketed in Russia as Carphedon and Phenotropil. It is one of the first ever nootropic drugs and originally discovered in Russia. Fonturacetam acts on most neurotransmitter systems and has been used for its cognitive and physical enhancing properties, and also as an antidepressant.
Status:
Investigational
Source:
INN:pargeverine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Pargeverine (also known as a propinox) is an antispasmodic drug that was studied for the treatment of disorders of the gastrointestinal tract, the uterus, and the gallbladder. Pargeverine showed a dual mechanism of action, it binds to muscarinic and calcium receptors that can be related to its antispasmodic activity. The clinical trial has shown that pargeverine was an effective drug in the treatment of moderate to severe colic pain of biliary origin. In addition, its efficacy and tolerability were determined in patients with moderate-to-severe acute intestinal colic pain. As a result, no differences in blood pressure or heart rate were found among treatments. The incidence of mouth dryness was significantly more frequent with the 20 mg and 30 mg doses of propinox than with the placebo or the 10 mg dose. Information about the current development of this drug is not available.
Status:
Investigational
Source:
NCT01155531: Phase 1 Interventional Completed Obesity
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Telenzepine is a selective muscarinic M1 receptor antagonist that was studied for selective inhibition of gastric acid secretion. Telenzepine was used in clinical trials in patients with acute duodenal ulcer, where was found that once daily administration of 3 mg in the evening must be regarded as the optimal dosage regimen of telenzepine. However, the preregistration for peptic ulcer in Germany was discontinued. In addition, the drug was studied in patients with nocturnal asthma. It was shown that telenzepine via the oral route at a dose of up to 5 mg was not effective in preventing nocturnal asthma.
Status:
Investigational
Source:
INN:nanofin [INN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


Nanofin is a ganglion blocker alkaloid having nicotinic acetylcholine receptor antagonist action. It has an antihypertensive effect used for mild to moderate hypertension. It was also used for the treatment of eczema and neurodermatitis.
Status:
Investigational
Source:
INN:espatropate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Espatropate (UK 88060) is an antagonist of M3 muscarinic receptors. Espatropate is a bronchodilator with anticholinergic activity. It was undergoing preclinical development with Pfizer for the treatment of asthma.
Esaprazole, also known as hexaprazole, was developed in the 1980s as a drug for the treatment of gastric and duodenal ulcers. Esaprazole exerts a dose-dependent cytoprotective effect on the gastric mucosa in man. It was shown to have a dose-dependent antisecretory activity, which was particularly evident on secretion volume and acid output. Esaprazole completed phase II clinical trials with only a few minor side effects being reported, but was shown to be less effective than Cimetidine and Ranitidine at healing ulcers. Esaprazole is a weak sigma opioid receptor and muscarinic acetylcholine receptors M3 and M5 ligand. Esaprazole analogs with many compounds showing neuroprotective properties.

Showing 101 - 110 of 816 results