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

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Showing 61 - 70 of 816 results

Status:
Investigational
Source:
NCT00686933: Phase 2 Interventional Completed Attention-Deficit/Hyperactivity Disorder
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Pozanicline is an alpha4-beta2 neuronal nicotinic receptor partial agonist. It had been in phase II clinical trials for the treatment of attention hyperactivity disorder and Alzheimer’s disease. It was tested for the treatment of schizophrenia too. All these studies were discontinued. Modulation of hippocampal learning and memory using Pozanicline in animal model was effective as novel therapeutic strategies for nicotine addiction. However future clinical trial was terminated.
Status:
Investigational
Source:
INN:revatropate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Revatropate is a muscarinic antagonist with selectivity for M1 and M3 receptor subtypes. Significant improvement in airway function was shown in horses with heaves after inhalation of revatropate, and it was found to be a safe and effective bronchodilator. Early clinical studies in chronic obstructive airway disease (COAD) patients also showed that inhaled revatropate was an effective bronchodilator, and well tolerated.
Alvameline is a partial agonist of the M1 mAChR that also displays M2/M3 antagonist effects. It readily crosses the blood-brain barrier. It has an effect profile that makes it of interest to test its ability to counteract bladder overactivity in humans. Behaviorally, alvameline has been shown to significantly improve Morris water maze (MWM) performance in both young and ageimpaired rats. It failed to improve cognition in patients with mild to moderate Alzheimer's disease.
ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine] is a potent cholinergic neuronal nicotinic acetylcholine receptor (nAChR) ligand with analgesic properties. ABT-594 binds alpha-4/ beta-2 neuronal nAChRs acting as an agonist. ABT-594 is studying for the treatment of diabetic peripheral neuropathic pain.
Status:
Investigational
Source:
NCT00387946: Phase 3 Interventional Completed Smoking Cessation
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Dianicline binds with high affinity to the rat and human alpha4beta2 nicotinic acetylcholine receptor (nAChR) subtypes and displays selectivity for the alpha4beta2 nAChR. Electrophysiological experiments indicate that dianicline is a partial agonist at the human alpha4beta2 nAChR subtype. Pretreatment with dianicline reduces the dopamine-releasing and discriminative effects of nicotine. Dianicline shows activity in animal models of nicotine dependence at doses devoid of unwanted side effects typically observed with nicotine. Dianicline did not increase cigarette smoking abstinence rates beyond the initial phase of treatment. However, self-reported craving and nicotine withdrawal symptoms were reduced. The most common adverse event for subjects receiving dianicline was nausea. Other gastrointestinal disorders also tended to be more frequent in the dianicline group, including diarrhea.
AE-37 (ANAVEX2-73, Tetrahydro-N, N-dimethyl-2, 2-diphenyl-3-furanemethanamine) is an orally available drug candidate developed to potentially modify Alzheimer’s disease rather than temporarily address its symptoms. It has a clean Phase 1 data profile and shows a reversal of memory loss (anti-amnesic properties) and neuroprotection in several models of Alzheimer’s disease. This drug is in Phase II trials for Alzheimer's disease, phase I trials for epilepsy, and in preclinical trials for amyotrophic lateral sclerosis, Parkinson's disease, Rett syndrome, stroke. AE-37 may function as a pro-drug for ANAVEX19-144 and acts as a muscarinic receptor and a moderate sigma1 receptor agonist.
Status:
Investigational
Source:
NCT01458197: Phase 2 Interventional Completed Overactive Bladder
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Tarafenacin (also known as SVT-40776) was developed as muscarinic M3 receptor antagonist for the treatment of overactive bladder. The drug participated in phase II clinical trial in patients suffering from overactive bladder, where both dose levels of tarafenacin were well tolerated. However, information about the further development of tarafenacin is not available.
Status:
Investigational
Source:
INN:velufenacin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:emraclidine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03645434: Phase 2 Interventional Completed Chronic Obstructive Pulmonary Disease
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)