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

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Showing 981 - 990 of 13268 results

Status:
Investigational
Source:
NCT03850301: Not Applicable Interventional Recruiting Multiple Sclerosis
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Emapunil acts as a selective agonist at the peripheral benzodiazepine receptor (TSPO). At the cellular level, the selective TSPO ligand XBD173 potentiated the amplitude and duration of GABA-mediated inhibitory postsynaptic currents in mouse medial prefrontal cortical neurons, which was prevented by finasteride. In animal and human trials, XBD173 produced rapid anxiolytic and anti-panic effects probably via newly synthesized neurosteroids, without producing sedation or withdrawal symptoms, and may represent a promising target for the development of fast-acting anxiolytics with a more favourable side-effect profile than benzodiazepines.
Status:
Investigational
Source:
INN:divaplon
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Divaplon is one of a series of imidazopyrimidine derivatives, which are benzodiazepine receptor ligands. This compound exhibits anxiolytic and anticonvulsant activity but little or no sedative/myorelaxant effects. Divaplon occupied a large percentage of benzodiazepine receptors, as measured with an in vivo binding technique, without inducing any deficit in a rotating drum task in mice, and it is suggested that divaplon is a partial agonist at GABA receptors. No significant anticonvulsant tolerance was seen with the divaplon.
Status:
Investigational
Source:
INN:moguisteine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Moguisteine is a non-narcotic antitussive compound. Moguisteine demonstrated inhibitory effect on rapidly adapting irritant receptors that could account for the antitussigenic effect of this compound. Furthermore, it is possible that ATP-sensitive K(+) channels may be involved in the anti-tussive effect of peripherally acting non-narcotic moguisteine. The drug did not show any toxic effect on the dams and their fetuses, nor did it have any teratogenic effect in either of the tested species. Finally, moguisteine had no adverse effects, either on parturition or on peri-and postnatal survival and/or development of the offspring. It was reported that moguisteine to be effective in reducing cough frequency in chronic cough of bronchitis and COPD. It was recommended for the short-term symptomatic relief of coughing. Preregistration of moguisteine in Italy is discontinued.
Status:
Investigational
Source:
INN:ethyl dirazepate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Ethyl dirazepate is an anticonvulsant compound.
Status:
Investigational
Source:
USAN:ROSARAMICIN PROPIONATE [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Proadifen is an inhibitor of drug metabolism and cytochrome P450 enzyme system activity. It stimulated the release of prostacyclin (PGI2) from the rabbit aorta, bovine aorta and human umbilical vein in vitro, but had no effect on cultured smooth muscle from the bovine aortic media. In human platelets, proadifen inhibited prostaglandin and thromboxane production induced by A23187, thrombin, and ADP. Proadifen might thus constitute the prototype of a new class of antiplatelet drugs.
Pravadoline is the anti-nociceptive agent, which has analgesic efficacy against postoperative pain in humans. Pravadoline inhibits the enzyme cyclooxygenase, but in contrast to cyclooxygenase-inhibiting NSAIDs does not produce gastrointestinal irritation. Pravadoline inhibited the synthesis of prostaglandins in mouse brain both in vitro and ex vivo. Pravadoline demonstrated only weak anti-inflammatory activity relative to its anti-nociceptive potency. Single doses of pravadoline were safe and effective in humans, without serious adverse events. Single oral administration of pravadoline maleate induced acute tubular necrosis in male and female beagle dogs.
Status:
Investigational
Source:
NCT00612508: Not Applicable Interventional Completed Contraceptive Usage
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dofamium is the antiseptic agent. It was used for the water sterilization.
Status:
Investigational
Source:
INN:oxabrexine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxabrexine was developed as a diuretic; however, this compound has never been marketed. Information about the current use of this compound is not available.
Status:
Investigational
Source:
USAN:Amindocate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Information in the scientific papers related to the biological and/or pharmacological application of amindocate is absent.