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

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Showing 121 - 130 of 993 results

Status:
Investigational
Source:
NCT01519557: Early Phase 1 Interventional Completed Schizophrenia
(2011)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist. Dihydrexidine was shown to stimulate cyclic AMP synthesis just as well or better than dopamine. It was the first dopamine D1 receptor agonist that had potent antiparkinsonian activity in a primate model of Parkinson's disease. Dihydrexidine produces hypothermia. Dihydrexidine has been shown to alleviate cognitive deficits or enhance cognitive performance in a number of animal models of cognition. It is under investigation for the improving the cognitive and working memory deficits in schizophrenia and schizotypal disorder.
Status:
Investigational
Source:
NCT03418714: Phase 1/Phase 2 Interventional Completed Drug Effect
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Salvinorin A has been reported to be the most potent naturally occurring hallucinogen, with an effective dose in humans in the 200- to the 1,000-μg range when smoked; it has been reported to induce an intense hallucinatory experience in humans, with a typical duration of action being several minutes to an hour or so. Salvinorin A is a highly selective agonist of the kappa-opioid receptor (KOR) with few off-target effects. It is a potent and selective dilator of the cerebral vasculature, exhibits rapid penetration through the blood-brain barrier, has potent anti-inflammatory properties, and has the ability to preserve neurovascular unit integrity. As such, salvinorin A is an ideal compound for the prevention and treatment of cerebral vasospasm following subarachnoid hemorrhage.
Status:
Investigational
Source:
NCT01188967: Phase 2 Interventional Completed Nicotine Dependence
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02294266: Phase 1 Interventional Completed Amphetamine-Related Disorders
(2014)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Mephedrone (4-methylmethcathinone) is a β-ketoamphetamine belonging to the family of synthetic cathinones, an emerging class of designer drugs known for their hallucinogenic and psychostimulant properties as well as for their abuse potential. Mephedrone is a stimulant of dopamine (DA) release and blocks its reuptake through its interaction with the dopamine transporter. Furthermore, it has some affinity for various 5-hydroxytryptamine (5-HT) receptor subtypes. Neurotoxic effect of mephedrone on 5-HT and DA systems remains controversial. Although some studies in animal models reported no damage to DA nerve endings in the striatum and no significant changes in brain monoamine levels, some others suggested a rapid reduction in 5-HT and DA transporter function. Persistent serotonergic deficits were observed after binge like treatment in a warm environment and in both serotonergic and dopaminergic nerve endings at high ambient temperature. Oxidative stress cytotoxicity and an increase in frontal cortex lipid peroxidation were also reported. Despite the re-classification of mephedrone as a Class B restricted substance by the United Kingdom and restrictive legislation by the United States, international policy regarding mephedrone control is still developing and interest in synthetic amphetamine-like drugs could drive the development of future mephedrone analogues.
Status:
Investigational
Source:
INN:ordopidine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ordopidine (also known as ACR-325) is a dopaminergic stabilizer that acts as dopamine D2 receptor antagonists with low affinity. Ordopidine under the development of NeuroSearch participated in phase I trials for the treatment of Parkinson's disease and bipolar disorder. Information about the current study of this drug is not available.
Status:
Investigational
Source:
INN:savoxepin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Savoxepine (also known as cipazoxapine), a tetracyclic compound, possesses a potent neuroleptic-like effects. This compound acts via dopamine D(2)-receptor blockade. Savoxepine was studied in phase II clinical trials in Europe for the treatment of patients with psychotic disorders; however, these studied were discontinued.
Status:
Investigational
Source:
INN:naxagolide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Naxagolide (MK-458; L 647,339; (+)-PHNO) is a dopamine D2/D3-receptor agonist, which was studied for the treatment of patients with Parkinson's disease, but further study was discontinued. In addition, was discovered, that Naxagolide C-11 ([(11)C]-(+)-PHNO) was a potential radiotracer for imaging the high-affinity state of dopamine D2 receptors with positron emission tomography (PET) in human subjects. This radiotracer is a suitable for imaging the agonist binding sites (denoted D(2HIGH) and D(3)) of these receptors. PET studies in nonhuman primates documented that, in vivo, [(11)C]-(+)-PHNO displays a relative selectivity for D(3) compared with D(2HIGH) receptor sites and that the [(11)C]-(+)-PHNO signal is enriched in D(3) contribution compared with conventional ligands such as [(11)C] raclopride. Recently was published article reflects the relationship between social attachment and dopamine D2/3 receptor availability in the brains of healthy humans using [11C]-(+)-PHNO.
Status:
Investigational
Source:
INN:trepipam [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Trepipam is a benzazepine derivative. It is a D1-dopamine antagonist. Trepipam significantly reduced aggression in behaviorally disturbed adolescents and in acute schizophrenics without producing concomitant sedation. Trepipam specifically reduces aggressive and hyperactive behaviors in a wide range of laboratory tests in various species, without producing signs of overt CNS depression or neurological impairment. The drug is effective in reducing many forms of aggression including brain stimulated emotional behavior. Trepipam actually had little effect on gross behavior in mice or rats and only produced ataxia at lethal doses.
Status:
Investigational
Source:
INN:solypertine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Solypertine (WIN-18413-2) is an antiadrenergic drug. Solypertine selectively blocked the conditioned avoidance response in rats. Solypertine potentiated hexobarbitone sleeping time, caused hypothermia and afforded protection from amphetamine toxicity inaggregated mice.
Status:
Investigational
Source:
INN:levofenfluramine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


LEVOFENFLURAMINE is a levorotatory enantiomer of fenfluramine, a substituted amphetamine which was formerly used to treat obesity. LEVOFENFLURAMINE has dopamine-antagonistic properties and, at high doses, increases dopamine concentrations in rat striatal dialysates. It is essentially inactive to reduce food intake in human subjects.