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

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Showing 30921 - 30930 of 34777 results

Status:
Investigational
Source:
NCT00163085: Phase 2 Interventional Completed Parkinson's Disease
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Traxoprodil (CP-101,606) is a potent, selective N-Methyl-D-aspartate (NMDA) receptor (NR2B subunit) antagonist under development by Pfizer for its potential as a neuroprotectant in head injury and neurodegenerative disease. It is in phase II trials in the US and in phase I in Japan for the potential treatment of head injury, such as, Depressive Disorder, Major and Parkinson's Disease. CP-101,606 does not protect against glutamate-induced neurotoxicity in cultured cerebellar neurons, up to a dose of 10 uM. These results are consistent with CP-101,606 being a potent NMDA antagonist, selective for the type of NMDA receptor associated with the hippocampus. Some further investigation revealed that CP-101,606 was associated with a dose-related dissociation and amnesia. These results support the hypothesis that glutamate antagonists may be useful antidyskinetic agents. However, future studies will have to determine if the benefits of dyskinesia suppression can be achieved without adverse cognitive effects.
Status:
Investigational
Source:
NCT00069511: Phase 2 Interventional Unknown status Hepatitis C
(2003)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

UT-231B is an iminosugar that was under development by United Therapeutics Corporation as an oral drug for the treatment of hepatitis C virus (HCV). UT-231B completed acute and chronic Phase I dosing studies in early 2003. A Phase II proof-of-concept study for UT-231B in patients infected with hepatitis C who have failed conventional therapies was started, but the development of drug seemed to be discontinued.
Status:
Investigational
Source:
INN:pimilprost
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Pimilprost (SM-10902) and its free acid, SM-10906 are new stable 3-oxa-methano prostaglandin (PG) I1 analogs, SM-10902 is a prodrug of SM-10906. SM-10906, but not SM-10902 was demonstrated to be an agonist for IP receptors. SM-10906 was shown to exert its anti-platelet and vasodilatory activities through the increase of the cAMP level. Pimilprost was being developed by Dainippon Sumitomo Pharma (formerly Sumitomo Pharmaceuticals) in Japan for the treatment of skin ulcers. In Japan, an NDA was filed for pimilprost and was awaiting registration. However, development appears to have been discontinued.
Status:
Investigational
Source:
J Zoo Wildl Med. Sep 2016;47(3):834-843.: Not Applicable Veterinary clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Etorphine was the first potent opiate agonist employed primarily for use in non-domestic and wild species. Etorphine was 500 times as potent as morphine, with a very rapid onset and short duration of action. In morphine-dependent subjects, etorphine suppressed abstinence but for a shorter period than morphine. Etorphine is a full opiate agonist and binds to multiple opiate sites in the central nervous system. It is believed to produce its clinical effects through binding the µ-, δ-, and κ- opiate sites. It has a potent effect on depressing the respiratory centers of the CNS thus resulting in apnea being commonly seen in immobilized animals. Etorphine revolutionized the ability of biologists and veterinarians to safely capture and restrain many species that previously could not be handled. Etorphine is not currently commercially available due to lack of production by the manufacturer.
Status:
Investigational
Source:
INN:berupipam [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Berupipam (also known as NNC 22-0010), a dopamine antagonist with a high affinity and selectivity for D1 receptor has been studied for patients with psychotic disorders. Berupipam participated in phase I clinical trials; however, further development of this drug was discontinued
Status:
Investigational
Source:
NCT02471196: Phase 2 Interventional Completed Alzheimer's Disease
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Juvantia Pharma and Orion developed ORM-12741, also known as ORM-10921, a novel selective antagonist of alpha-2C adrenoceptors for the treatment of depression and Alzheimer's disease. ORM-12741 participated in phase II clinical trial where was evaluated the safety and efficacy of the drug in patients with Alzheimer's disease. In spite of the successfully completed phase II, further study of the drug for this disease was discontinued. In addition, ORM-12741 participated in clinical trial phase II to prove the concept that this drug could prevent blood vessel spasms for Raynaud's phenomenon. Raynaud's phenomenon is a disorder of the digital blood vessels resulting in episodic impairment of blood flow. However, this study was terminated because of the recommendation by study Data and Safety Monitoring Committee to the sponsor following the interim analysis of 8 subjects.
Status:
Investigational
Source:
NCT00405119: Phase 2 Interventional Completed Gastroesophageal Reflux Disease
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

LAVOLTIDINE, also known as loxtidine, is a highly potent and selective histamine H2-receptor antagonist. It is a member of triazoles. It produces gastric carcinoid tumors in rodents that is why its clinical development was discontinued.
Status:
Investigational
Source:
NCT00197145: Phase 3 Interventional Terminated Infection, Human Immunodeficiency Virus I
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Aplaviroc (GW873140) is a small-molecule noncompetitive allosteric CCR5 antagonist or HIV entry inhibitor (EI) that binds specifically to human CCR5 and exhibits potent anti-HIV activity in vitro in the nanomolar or subnanomolar range. Aplaviroc has exhibited potent in vivo antiviral activity (1.66 log decrease in viral load at nadir) following 10 days of monotherapy. In vitro studies of antiviral activity demonstrate that aplaviroc is active against HIV isolates from a variety of clades as well as those resistant to current HIV therapies targeting RT, PR, and gp41. However, GlaxoSmithKline has decided to terminate Phase III trials of aplaviroc after encountering additional cases of liver damage in patients taking the drug.
Status:
Investigational
Source:
NCT00275197: Phase 2 Interventional Completed Depressive Disorder, Major
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Elzasonan (CP 448187) is a serotonin 1B/1D receptor antagonist. Elzasonan was primarily metabolized via oxidative N‐demethylation, N‐oxidation, and aryl hydroxylation. Pfizer was developing elzasonan for the treatment of anxiety and affective disorders however development has been discontinued.
Status:
Investigational
Source:
INN:nalmexone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Nalmexone is an opioid partial agonist or mixed agonist-antagonist with both analgesic and narcotic antagonist properties. In preclinical models parenteral nalmexone was a moderately active antagonist and therefore might have low abuse potential. At the same time, early work in man indicated analgesic activity in doses above 20 mg.

Showing 30921 - 30930 of 34777 results