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

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Showing 391 - 400 of 525 results

Status:
Possibly Marketed Outside US
Source:
Ciba 10870 by Ciba Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Aturban (phenglutarimide) is a neuropsychiatric agent, was used as therapeutic drug for parkinsonism. Phenglutarimide hydrochloride possesses parasympatholytic activity and has been available as an antiparkinson agent since its preparation by Tagman, Sury & Hoffmann (1952). Phenglutarimide is a muscarinic acetylcholine receptor antagonist. There are three subtypes of enantiomers of phenglutarimide. The affinity of the enantiomers of phenglutarimide at three muscarinic receptor subtypes was examined in vitro using field-stimulated rabbit vas deferens (M1 receptors) and guinea pig atria (M2 alpha receptors) and ileum (M2 beta receptors). Extremely high stereoselectivity was observed and higher affinities (up to 6000-fold) were found for the (+)-S-enantiomer. The stereoselectivity ratios were different at the three subtypes, and the stereochemical demands made by the muscarinic receptors were most stringent at M1 receptors. (+)-(S)-Phenglutarimide was found to be a potent M1-selective antagonist (pA2 at M1 = 8.53). Its receptor selectivity profile is qualitatively similar to that of pirenzepine. (-)-(R)-Phenglutarimide showed no comparable discriminatory properties.
Status:
Possibly Marketed Outside US
Source:
NCT02307396: Phase 4 Interventional Completed Schizophrenia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Zuclopenthixol is indicated the management of the manifestations of schizophrenia and other mental illnesses with disturbances in thinking, emotional reactions and behaviour. It is also used to treat the manic phase of manic depressive illness. Zuclopenthixol, a thioxanthene derivative, has high affinity for both dopamine D1 receptors and dopamine D2 receptors. Zuclopenthixol also has high affinity for α1-adrenergic and 5-HT2 receptors. Zuclopenthixol (CLOPIXOL®) is avavilable in the form of tablets and solution for intramuscular injections.
Status:
Possibly Marketed Outside US
Source:
NCT04589143: Phase 4 Interventional Completed Major Depressive Disorder
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Agomelatine behaves both as a potent agonist at melatonin MT1 and MT2 receptors and as a neutral antagonist at 5-HT2C receptors. Accumulating evidence in a broad range of experimental procedures supports the notion that the psychotropic effects of agomelatine are due to the synergy between its melatonergic and 5-hydroxytryptaminergic effects. Agomelatine is indicated for the treatment of major depressive episodes.
Status:
Possibly Marketed Outside US
Source:
NCT02682758: Phase 4 Interventional Completed Anesthesia
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Xenon is a noble gas used as an anesthetic agent. Xenon can associate with amino acid side chains of the active site of enzymes such as serine proteinases (including elastases and collagenases); these enzymes can form a specific binding cavity for single xenon atom without inducing major changes in protein structure. It has been demonstrated that xenon binds within the heme cavity of cytochrome P-450 monooxygenases and is capable of inhibiting the catalytic activity of some enzymes in vitro. Current evidence suggests that inhibition of N-methyl-D-aspartate (NMDA) receptor signaling is the mechanism by which xenon induces anesthesia. Although approved for use in anesthesia in Russia in 2000, it was unavailable for use in western countries until October 2005 when approval for its use was granted in Germany.
Status:
Possibly Marketed Outside US
Source:
NCT00853866: Phase 4 Interventional Completed Cerebral Stroke
(2009)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Reboxetine is a selective noradrenergic reuptake inhibitor that acts by binding to the norepinephrine (NE) transporter and blocking reuptake of extracellular NE back into terminals. This compound has low affinity for other transporters and receptors. Reboxetine is used in acute treatment of depressive illness / major depression. Very common side effects are: difficulties to sleep (insomnia); dizziness; dry mouth; constipation; nausea (feeling sick); sweating. Based on studies conducted primarily outside the US, the FDA granted a preliminary letter of approval in 1999. However, more recent clinical studies conducted in the US and Canada, prompted by the FDA, resulted in a letter of non-approval.
Status:
Possibly Marketed Outside US
Source:
OLCADIL by Sankyo
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Cloxazolam is an agonist of GABA-A receptor that was developed in Japan for the treatment of anxiety-disorders. The drug was marketed in Europe under the names Sepazon, Olcadil, Akton and Lubalix.
cis-Dosulepin is a stereoisomer of Dothiepin (trade name Prothiaden, Dothep, Thaden, and Dopress; Dosulepin (INN, BAN) a tricyclic antidepressant that is used in several European and South Asian countries, as well as Australia, South Africa, and New Zealand. Dosulepin is used for the treatment of the major depressive disorder and neuropathic pain. Dosulepin is only Therapeutic Goods Administration and Medicines and Healthcare products Regulatory Agency approved for the treatment of the major depressive disorder. Dothiepin is not used in the United States. The central action of cis-dosulepin was compared with that of its antidepressant stereoisomer trans-dosulepin, cis-dosulepin exerted weaker anti-reserpine, anti-tetrabenazine, and 3H-5-HT (serotonin) uptake inhibiting actions than trans-dosulepin, but cis-dosulepin's inhibition of 3H-dopamine and 3H-norepinephrine uptake was slightly more potent than that of trans-dosulepin. On the other hand, cis-dosulepin exhibited extremely potent anticholinergic action in oxotremorine induced tremor, isolated ileum and the 3H-quinuclidinyl benzilate binding test. It also showed potent apomorphine enhancing the action and shortened the period of immobility in the forced swimming test in animals.
Status:
Possibly Marketed Outside US
Source:
Japan:Nifenazone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Nifenazone is a drug that has been used as an analgesic for a number of rheumatic conditions. Later it was shown that nifenazone is not of significant value in the therapy of the chronic rheumatic disorders and that side-effects may be expected to occur, particularly in those patients who give a history of abnormal reactions to phenylbutazone and oxyphenbutazone.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Dipyrocetyl (2,3-diacetyloxybenzoic acid) is a drug used as an analgesics and antipyretics. Besides, was shown, that it may be useful in the treatment of acute lung injury (ALI) associated with acute respiratory distress syndrome (ARDS). Dipyrocetyl possesses the anticoagulation properties, which may contribute directly to improve tissue integrity as well as indirectly by the prevention of activation of pro-inflammatory cytokines. In addition, was made a suggestion, that the drug may function as an MMP inhibitor.
Status:
Possibly Marketed Outside US
Source:
DORMONOCT by Roussel Laboratories
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Loprazolam is a hypnotic drug which stimulates GABA-A receptors. Due to its hypnotic activity the drug is used to treat short-term sleep disordes.

Showing 391 - 400 of 525 results