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

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Showing 341 - 350 of 525 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Quinupramine is a tricyclic antidepressant used in the treatment of reactive and endogenous depression. Quinupramine was found to possess a higher affinity for muscarinic cholinergic receptor binding sites in brain and heart, compared with imipramine. Quinupramine also displayed a substantial affinity for 5-HT2 receptors in the cerebral cortex. Quinupramine may show many adverse side effects such as dry mouth, urinary retention, and daytime drowsiness.
Dibenzepin is a tricyclic antidepressant of the dibenzo-epine group. It is a selective noradrenaline uptake inhibitor, which exhibits in vitro and in vivo imipramine-like effects. It binds strongly to histamine H1 receptors in the brain and, to a lesser extent, to cholinergic receptors. The pharmacological profile of dibenzepin corresponds widely to its biochemical properties: histamine antagonism, tetrabenazine antagonism, potentiation of various noradrenergic effects and anticholinergic effects. Dibenzepin is only available in European countries for the treatment of depression.
Status:
Possibly Marketed Outside US
Source:
Lenigesial by Inpharzam [W. Germany]
Source URL:

Class (Stereo):
CHEMICAL (MIXED)


Viminol is an opioid analgesic developed by the company Zambon. It is marketed under tradename Dividol for the treatment of pain due to various causes, including the treatment of pain due to osteoarthritis, neuritic pain, vascular pain, visceral pain, neoplastic pain, and pain due to other sources. In vivo studies demonstrated that the analgesic effects of viminol depend on the stereo configuration: the R,R-enantiomer exhibit agonistic activity, while the S,S-enantiomer produce the opposite effect.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Tropatepine is an anticholinergic drug. Intramuscular injections of tropatepine are used to counteract the extrapyramidal effects of neuroleptic drugs and for the treatment of Parkinson's disease. The drug is marketed in Europe under tradename Lepticur.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxetorone is an antimigraine drug used for the disease-modifying treatment of migraines and marketed in several European countries. It works by non-selective inhibition of serotonin receptors and antihistamine agent. The therapeutic effects of oxetorone are primarily linked to antiserotonergic and also antihistamine and anti-adrenergic properties. Antidopaminergic properties are also suspected because hyperprolactinemia and extrapyramidal reactions have been observed. Adverse effects are: hypertonia, drowsiness at the start of treatment, diarrhoea and lymphocytic colitis. Acute intoxications by oxetorone, although uncommon, are potentially severe poisonings.
Status:
Possibly Marketed Outside US
Source:
NCT01890538: Phase 4 Interventional Completed Peripheral Vertigo
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Piracetam (sold under many brand names) is a nootropic drug in the racetams group, with chemical name 2-oxo-1-pyrrolidine acetamide. It shares the same 2-oxo-pyrrolidone base structure with pyroglutamic acid. Piracetam is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), originally marketed in 1971 by UCB Pharma. Presently piracetam is used in many European countries, Asia and South America. In the United States, it is not approved by the US Food and Drug Administration for any medical use and it is not permitted to be sold as a dietary supplement. In the UK, piracetam is prescribed mainly for myoclonus but is used off-label for other conditions. Evidence to support its use for many conditions is unclear. Piracetam's mechanism of action, as with racetams in general, is not fully understood. The drug influences neuronal and vascular functions and influences cognitive function without acting as a sedative or stimulant. It is hypothesized to act on ion channels or ion carriers, thus leading to increased neuron excitability. GABA brain metabolism and GABA receptors are not affected by piracetam. It has been found to increase blood flow and oxygen consumption in parts of the brain, but this may be a side effect of increased brain activity rather than a primary effector mechanism of action for the drug.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Camazepam is a benzodiazepine psychoactive drug, marketed under the brand names Albego, Limpidon and Paxor. It is the dimethyl carbamate ester of temazepam, a metabolite of diazepam. While it possesses anxiolytic, anticonvulsant, skeletal muscle relaxant and hypnotic properties it differs from other benzodiazepines in that its anxiolytic properties are particularly prominent but has comparatively limited anticonvulsant, hypnotic and skeletal muscle relaxant properties. Changes in sleep with camazepam were minimal. However, non-anxious subjects reported being more relaxed the next day. Camazepam may cause skin disorders.
Fonzine (also known as dimetotiazine) is an analgesics and anti-inflammatory agent marketed in Japan and Europe under the name Migristene and indicated for the treatment of migraine and headaches secondary to other disease. Fonzine exerts its activity by inhibiting serotonin and histamine H1 receptors.
Distigmine is an acetylcholinesterase (AChE) inhibitor. Distigmine shows direct binding to muscarinic receptors in the rat bladder, and repeated oral administration of distigmine causes downregulation of muscarinic receptors in the rat bladder. The observed direct interaction of distigmine with the bladder muscarinic receptors may partly contribute to the therapeutic and/or side effects seen in the treatment of detrusor underactivity. It is usually used to treat myasthenia gravis, dysuria due to hypotonic bladder such as neurogenic bladder or after surgery. Common side effects are: nausea/vomiting, abdominal pain, diarrhea, increased salivation, hypersecretion in respiratory tract, sweating, bradycardia, miosis, difficulty in breathing. Distigmine has a greater risk of causing cholinergic crisis because of accumulation of the drug being more likely than with neostigmine or pyridostigmine and so distigmine is rarely used as a treatment for myasthenia gravis, unlike pyridostigmine and neostigmine.
Status:
Possibly Marketed Outside US
Source:
Unknown by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Subarachnoid haemorrhage (SAH) following cerebral aneurysm rupture or trauma can result in the induction of secondary ischaemic brain damage via a decrease in microvascular perfusion, a disruption of the blood-brain barrier and consequent vasogenic oedema, and the delayed spasm of the major cerebral arteries (i.e. vasospasm). It is increasingly apparent that oxygen radical-induced, iron-catalyzed lipid peroxidation (LP) within the subarachnoid blood and vascular wall plays a key role in the occurrence of these secondary events. Tirilazad mesylate, is a nonglucocorticoid, 21-aminosteroid, is a potent cytoprotective inhibitor of LP that works by a combination of radical scavenging and membrane stabilizing properties. It has been demonstrated to attenuate the acute and delayed vascular consequences of SAH and to protect the brain against ischaemic insults. Tirilazad mesylate has been proposed to treat acute ischaemic stroke. When tested on animal models, tirilazad protects brain tissue, and reduces brain damage. However, the drug fails to treat, and even worsens a stroke when studied on a human being.

Showing 341 - 350 of 525 results