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

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Showing 71 - 80 of 993 results

Metitepine, a psychotropic agent was developed as a non-selective antagonist of serotonin, dopamine, and adrenergic receptors. Metitepine has never been marketed.
Status:
Investigational
Source:
INN:sunepitron [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Sunepitron (CP-93,393) is an anxiolytic drug with highly selective serotonin 5-hydroxytryptamine 1A autoreceptor agonist, alpha2-adrenergic antagonist, and dopamine D2 agonist properties. Sunepitron hydrochloride had been in Phase III clinical trials by Pfizer for the treatment of anxiety disorder and depression. However, this research has been discontinued.
Status:
Investigational
Source:
INN:mesocarb [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Mesocarb (sydnocarb or 3-(beta-phenylisopropyl)-N-phenylcarbamoylsydnonimine) is a psychomotor stimulant N-alkylated amphetamine derivative. Mesocarb is a selective inhibitor of dopamine uptake, it potently blocks dopamine transporter. It is very likely that mesocarb is being used by drug addicts. Mesocarb is included in the World Anti-Doping Agency’s list of substances and methods that are prohibited in sports. It is used in Russia for the treatment of a variety of neuropsychiatric comorbidities.
Status:
Investigational
Source:
INN:nepicastat
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nepicastat (SYN-117) is a potent and selective inhibitor of dopamine-β-hydroxylase. This compound in Phase 2 of clinical trial for the treatment cocaine addiction and posttraumatic stress disorder.
Status:
Investigational
Source:
INN:mezilamine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Mezilamine is a dopamine antagonist, it blocks presynaptic but stimulates postsynaptic alpha-adrenoceptors. Potential antipsychotic drug.
Methylenedioxymethamphetamine (or 3,4-methylenedioxymethamphetamine (MDMA)), a synthetic, psychoactive drug also known as ecstasy that was used as a recreational drug. This drug acts as both a stimulant and psychedelic and exerts its effects in the brain on neurons that use the chemicals serotonin, dopamine and norepinephrine to communicate with other neurons. In spite of the presence of this compound in the List of control and forbidden compounds, it was studied in psychotherapy for patients with chronic, treatment-resistant posttraumatic stress disorder. Initial results showed efficacy for the treatment approach, although further studies are needed.
Status:
Investigational
Source:
INN:naronapride [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Naronapride (ATI-7505), an orally administered, cisapride analogue and serotonin4 (5HT4) receptor agonist, is being developed by Renexxion for the treatment of multiple gastrointestinal disorders. Sinovant is initially developing naronapride for the treatment of irritable bowel syndrome – constipation (IBS-C), a disease that affects millions of Chinese patients and for which few effective treatment options are available. Naronapride has been evaluated in over 900 subjects in multiple randomized controlled clinical studies and has demonstrated promising results in patients with gastroesophageal reflux disease (GERD), erosive esophagitis (EE), and chronic idiopathic constipation (CIC). Naronapride’s low systemic absorption and high specificity for 5HT4 and D2 receptors is thought to improve its safety and tolerability profile relative to other members of the class.
Status:
Investigational
Source:
INN:levofacetoperane [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Levophacetoperane is a piperidine derivative. Levofacetoperane is a sympathomimetic central nervous system stimulant and is commonly used to treat depression. Levophacetoperane is also a known analeptic and is strongly linked to apnea reversal in dogs after a single intravenous injection.
Status:
Investigational
Source:
INN:delergotrile
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Delergotrile is a derivative of ergot alkaloids with dopaminergic and anti-parkinsonian action. Delergotine shows neuropharmacological action typical of postsynaptic dopamine D1 receptor stimulants, in particular in the extrapyramidal system. In addition, delergotine stimulates adenylate cyclase coupled serotonin receptors and antagonize central alpha-adrenergic receptors. The compound was studied in the clinical trials, in new, non-levodopa-treated parkinsonian patients. Delergotine elicited a significant but mostly only mild or moderate antiparkinsonian efficacy which seems to be less than that of levodopa.
Status:
Investigational
Source:
INN:cianergoline
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Cianergoline is an ergoline derivative with marked dopaminergic agonist and a predominant cardiovascular action patented by Farmitalia Carlo Erba S.p.A for hypertension treatment. The preclinical evaluation shows dose-related hypotensive effects after single oral, intraduodenal and intravenous administration of Cianergoline in cats, dogs, and rats. Cianergoline showed a prompt onset of action and a prolonged effect on blood pressure at low doses without substantially modifying animals heart rate. One month daily oral administration of Cianergoline in rats produced an antihypertensive effect persisting through the entire experiment with no signs of tachyphylaxis. Unfortunately, in clinical trials Cianergoline caused a slight, statistically non-significant blood pressure lowering effect in patients with essential hypertension and does not modify the release of prolactin, lipid metabolism or the basal activity or postural responsiveness of the renin-angiotensin-aldosterone axis and of the sympathetic nervous system.