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

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Showing 111 - 120 of 816 results

Status:
Investigational
Source:
INN:stilonium iodide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Stilonium Iodide (also known as MG 624) is a trimethylethanaminium derivative with ganglionic-blocking action. Stilonium Iodide acts as α7-nicotinic receptor antagonist and Stilonium Iodide inhibits transmission between preganglionic and postganglionic neurons in the Autonomic Nervous System. Stilonium Iodide inhibits nicotine-induced proliferation and angiogenesis in human microvascular endothelial cells of the lung. Stilonium Iodide displayed anti-angiogenic activity in Matrigel, rat aortic ring and rat retinal explant assays. Furthermore, MG624 suppressed angiogenesis of NCI-H69 human SCLC tumors in vivo in both the chicken chorioallantoic membrane (CAM) and nude mice model.
Status:
Investigational
Source:
NCT01400477: Phase 2 Interventional Completed Schizophrenia
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


GTS-21 (also known as DMBX-A), a selective alpha-7 nicotinic acetylcholine receptor agonist that has demonstrated memory and cognition enhancement activity in human clinical trials. GTS-21 has been studied in Phase II in patients with schizophrenia and in patients with Alzheimer disease. However, these studies were discontinued. GTS-21 was also involved in phase II to reduce negative affect, improve cognition and/or reduce smoking relapse in healthy adult men and women who are chronic cigarette smokers. However, this study was withdrawn. Besides, GTS-21 has participated in phase II to investigate safety and efficacy in adults with attention-deficit hyperactivity disorder.
Status:
Investigational
Source:
NCT01466088: Phase 2 Interventional Completed Alzheimer's Disease
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


ISPRONICLINE is a partial agonist at the a4b2 subtype of nicotinic acetylcholine receptors (nAChRs) without interaction with other nAChRs or other receptor systems. It has antidepressant, nootropic, and neuroprotective effects. It progressed to phase II clinical trials for the treatment of dementia and Alzheimer's disease but is no longer under development.
Status:
Investigational
Source:
INN:namoxyrate [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Xenbucin is an antihyperlipidemic agent. Information about the current use of this agent is not available.
Status:
Investigational
Source:
NCT00490516: Phase 2 Interventional Completed Schizophrenia
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

ACP-104 or N-Desmethylclozapine (NDMC), or norclozapine is a major metabolite of clozapine, which was developed like a small molecule drug candidate by ACADIA for treatment schizophrenia. ACP-104 combines M1 muscarinic agonist, 5-HT2A inverse agonist, and D2 and D3 dopamine partial agonist in a single compound and, therefore, uniquely addresses what ACADIA believed are the three most promising target mechanisms for treating schizophrenia. Then drug was discontinued, because the study did not meet its primary endpoint of antipsychotic efficacy or any of the secondary endpoints. Neither dose of ACP-104 demonstrated improved efficacy as compared to placebo. The most common adverse events in the treatment arms relative to placebo were increased salivation, tachycardia, and dyspepsia, which were noted to be dose-related. There was no clinically significant decrease in neutrophil counts in the study drug arms.
Status:
Investigational
Source:
INN:vedaclidine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Vedaclidine [LY 297802, NNC 101053, NNC 111053, butylthio[2.2.2]], a quinuclidine, is a muscarinic receptor agonist being developed by Novo Nordisk and Eli Lilly as an analgesic drug. Vedaclidine is a muscarinic receptor ligand which is equiefficacious to morphine in producing antinociception. In vitro, Vedaclidine had high affinity for muscarinic receptors in brain homogenates, but had substantially less or no affinity for several other neurotransmiter receptors and uptake sites. Its pharmacological profile suggests that it may have clinical utility in the management of pain as an alternative to opioids.
Status:
Investigational
Source:
NCT00996034: Phase 2 Interventional Completed Nicotine Dependence
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Vanoxerine, also known as GBR-12909, is a piperazine derivative exhibiting potent selective inhibition of sodium-dependent dopamine reuptake transporters. Vanoxerine has been in clinical trials for Parkinsonism, depression and cocaine addiction but lacked efficacy. Vanoxerine has also been observed as a potent blocker of the following channels: cardiac hERG/IKr potassium channel, Calcium channel, voltage-dependent, L type, alpha 1C subunit (also known as Cav1.2) and voltage-gated sodium channel Nav 1.5. Vanoxerine was studied as a potential treatment for atrial fibrillation. However, phase III clinical trials for this condition were terminated because of cardiac safety concerns. Research also indicates that vanoxerine may have additional mechanisms of action including antagonist action at nicotinic acetylcholine receptors (nAChRs).
Status:
Investigational
Source:
INN:metocinium iodide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Metocinium iodide, a spasmolytic agent, is an antagonist of muscarinic acetylcholine receptors. The drug is used in patients with irritable bowel syndrome.
Status:
Investigational
Source:
NCT00277810: Phase 2/Phase 3 Interventional Completed Alzheimer Disease
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LECOZOTAN, a benzodioxanylpiperazine derivative, is a selective serotonin 1A receptor antagonist. It was in development for the symptomatic treatment of cognitive deficits in Alzheimer's disease.

Showing 111 - 120 of 816 results