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

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Showing 2711 - 2720 of 3069 results

Status:
Investigational
Source:
INN:fasidotril
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Fasidotril is a diester prodrug of the active metabolite fasidotrilat. Fasidotrilat inhibited both angiotensin I converting enzyme (ACE, EC 3.4.25.1) and neprilysin (NEP, EC 3.4.24.11, also named neutral endopeptidase, enkephalinase, or atriopeptidase) at nanomolar concentrations (Ki = 9.8 nM against ACE and 5.1 nM against NEP) Fasidotril was being developed for the treatment of myocardial infarction, congestive heart failure and myocardial infarction.
Status:
Investigational
Source:
INN:metiprenaline
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Metiprenaline was developed as a bronchodilator. Information about the current use of this compound is not available.
Status:
Investigational
Source:
INN:myrophine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Myrophine is an opiate analog and long-acting prodrug for morphine with a slow onset of effects. It is weaker than morphine as an analgesic but longer-lasting in effects and was thought to have a more local anesthetic effect than morphine, though with a somewhat greater tendency to cause histamine reactions like itching and rash. In addiction studies conducted in human subjects in the 1950s, myrophine did not substitute for morphine in withdrawal, did not produce notable morphine-like effects, and did not produce addiction or dependence regardless of dose or how it was administered.
Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research. In humans, ritanserin increases deep slow-wave sleep, improved liveliness in a variety of psychiatric disorders and facilitated participation in behaviour therapy. During clinical trials, unexpected observations indicated that ritanserin may be of value in treating obsessive-compulsive disorder, acute mania, negative symptoms of schizophrenia, drug addicts, etc. Clinical observations confirmed the efficacy of ritanserin in the chronic withdrawal phase after detoxification from ethanol. Ritanserin had been in phase III clinical trials by Janssen L.P. for the treatment of anxiety disorder and major depressive disorder. However, the clinical development of ritanserin was discontinued.
Status:
Investigational
Source:
USAN:Amicibone
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Amicibone is an antitussive agent.
Status:
Investigational
Source:
INN:domoxin
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Domoxin is a hydrazine derivative. It is monoamineoxidase inhibitor. Domoxin was developed as antithrombotic agent.
Status:
Investigational
Source:
INN:nebracetam
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Nebracetam (WEB1881FU) is a pyrrolidinone nootropic. Like other racetams, it is an aminomethyl pyrrolidinone derivative of piracetam. It was first synthesized in Germany in the late 1980s, where it was manufactured by Boehringer Ingelheim. Nebracetam is a M1-muscarinic agonist. In Jurkat cells Nebracetam induced a rise of [Ca2+]i in the medium with 1 mM Ca2+ and without Ca2+ (plus 1 mM EGTA). The nebracetam-induced [Ca2+]i rise was blocked by atropine greater than pirenzepine greater than AF-DX 116. Nebracetam facilitates the ganglionic muscarinic transmission through acting on presynaptic sites. Nebracetam has been investigated as a cognition-enhancing drug, but most of the studies have taken place in animal models. It has been shown to protect neurons in animals exposed to low levels of oxygen and low blood sugar. Nebracetam is also protective against glutamate toxicity, presumably via its modulation of calcium entry. In animal models of Alzheimer’s disease, nebracetam improved memory in a dose-dependent manner. It also protected against ischemia- (lack of oxygen) induced neuronal death in a rat model of stroke. The compound has also been tested as a possible antidepressant, presumably because its mechanism of action (reducing dopaminergic and serotonergic uptake) is similar to other commonly used antidepressants. Some studies have taken place in humans. A single dose was shown to alter brain waves in healthy volunteers, who showed increased alpha activity and an associated decrease of slow activity and of fast activity in the frontal cortex. These results imply that nebracetam might improve linguistic learning and memory processing. A trial in dementia patients reported that significant clinical improvement occurred after 8 weeks. However, other studies did not replicate this finding.
Status:
Investigational
Source:
NCT00604123: Phase 2 Interventional Completed Allergic Rhinitis
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT04586790: Phase 2 Interventional Unknown status Spinal Shock
(2020)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Norepinephrine hydrochloride, (±)- (DL-Norepinephrine Hydrochloride) is a vasoconstrictor, cardiac stimulant, α- and β-sympathomimetic agent. DL-Norepinephrine hydrochloride is an adrenergic drug. Norepinephrine is an endogenous catecholamine that is the neurotransmitter at sympathetic postganglionic fibers. It has potent beta1- and alpha-stimulating effects. In contrast to epinephrine, norepinephrine has only minor effects on beta2 receptors. The clinical effects of norepinephrine administration are mainly increased cardiac index and increased vascular (systemic and pulmonary) resistance. Several adult studies have suggested that norepinephrine is useful in increasing SVR in patients with hyperdynamic or vasodilatory septic shock that is not responsive to dopamine or epinephrine. Additionally, it can augment coronary blood flow by increasing systemic diastolic pressure, at the expense of increasing afterload.
Status:
Investigational
Source:
JAN:L-ISOPRENALINE HYDROCHLORIDE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Levisoprenaline (l-isoproterenol) is beta1- and beta2-adrenoreceptor agonist. In Japan, continuous inhalation of levisoprenaline is a recommended treatment for pediatric patients with acute severe exacerbation. Compared with salbutamol, l-isoproterenol reduced modified pulmonary index score more rapidly. But in most countries do not recommend continuous inhalation of l-isoproterenol to treat pediatric patients with acute severe exacerbation of asthma due to worsening asthma control. Levisoprenaline was used to cause experimental chronic heart failure in rats.

Showing 2711 - 2720 of 3069 results