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Restrict the search for
icosapent ethyl
to a specific field?
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Scientists at Parke-Davis first synthesized Pramiracetam (brand name Pramistar) in the late 1970’s. It was first tested with Alzheimer’s patients. Seeing mixed results, the company tried it with major depressive disorder and licensed it as an orphan drug to Menarini. Pramiracetam is a central nervous system stimulant and nootropic agent belonging to the racetam family of drugs. Pramistar is used for the treatment of concentration and memory disturbances caused by the degeneration of brain cells or to diseases of the blood vessels supplying the brain, conditions that arise both in elderly patients (aged over 65 years). By stimulating choline uptake, pramiracetam indirectly modulates the release of acetylcholine and stimulates increased activity in the hippocampus. Because this part of the brain is absolutely crucial to the memory function, the general stimulation that pramiracetam creates can improve both the formation of new memories and the retention of reference or long-term memories. The increased activity in the hippocampus also increases cerebral blood flow, which enhances alertness and improves cognitive abilities in general. Pramiracetam may have other mechanisms of action as well. Researchers have hypothesized that in addition to its action in the brain, pramiracetam acts outside the brain in peripheral sites that rely on the adrenal glands. Animal studies suggest that pramiracetam may also increase or restore brain membrane fluidity, which facilitates cell signaling. Unlike many other racetam class nootropics, pramiracetam does not appear to strongly alter either wakefulness or emotional states. This can be explained by pramiracetam’s very limited influence on the production and release of serotonin, GABA and dopamine, the neurotransmitters that have the greatest effect on mood and anxiety levels.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Minaprine, a psychotropic drug, which was effective in the treatment of various depressive states. This drug was withdrawn because of the serious side effect. It was found, that minaprine inhibited the following enzymes, acetylcholinesterase and monoamine oxidase (MOA) A. It also binds to dopamine D1 and D2 receptors. Experiments on rodents also have revealed that minaprine suppressed the inhibitory effect of hydroxytryptamine (5-HT) on dopamine (DA) release via the inhibition of 5-HT binding at the 5-HT2 receptor on the nerve terminal.
Status:
Possibly Marketed Outside US
Source:
Bururalol hydrochloride
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Bufuralol is a non-cardioselective beta-adrenergic blocker with high intrinsic sympathomimetic activity. It has affinity for both β1 and β2-adrenergic receptors. It acts as a potent β-adrenoceptor antagonist with partial agonist activity. Bufuralol is primarily metabolized by cytochrome P450 (CYP) isoform CYP2D6, with CYP1A2 and CYP2C19. Activity of bufuralol has been shown to yield antianginal and antihypertensive effects. It appears to have a higher incidence of adverse eflects than with other beta blockers. Bufuralol has been in phase III clinical trials for the treatment of hypertension. However, this research has been discontinued.
Status:
Possibly Marketed Outside US
Source:
Zoniclezole hydrochloride
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Zoniclezole was proven to have anticonvulsant profile. It is representative of a novel class of water-soluble agents being developed for the treatment of epilepsy. Zoniclezole has been shown to be a potential antagonist of electroshock-induced seizures in animals, and to some degree, pentylenetetrazol-induced seizures. In preclinical studies the compound had prolonged efficacy at relatively low doses. Zoniclezole is glutamate receptor antagonist.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Atosiban (brand name Tractocile) is a competitive antagonist of human oxytocin at receptor level. In rats and guinea pigs, atosiban was shown to bind to oxytocin receptors, to decrease the frequency of contractions and
the tone of the uterine musculature, resulting in a suppression of uterine contractions. Atosiban was also shown to bind to the vasopressin receptor, thus inhibiting the effect of vasopressin. Tractocile is indicated to delay imminent pre-term birth in pregnant adult women with:
− regular uterine contractions of at least 30 seconds duration at a rate of ≥ 4 per 30 minutes
− a cervical dilation of 1 to 3 cm (0-3 for nulliparas) and effacement of ≥ 50%
− a gestational age from 24 until 33 completed weeks
− a normal foetal heart rate.
Atosiban does not have U.S. Food and Drug
Administration (FDA) approval for use in the United States.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Guanoclor is an anti-hypertensive agent developed by
Pfizer Ltd. (U.K.). It seems to be effective in various types of hypertension
(unknown aetiology, renal, and malignant). It affects both
systolic blood-pressure and diastolic blood-pressure. It is an
adrenergic neurone-blocking agent, which also interferes with
noradrenaline synthesis by inhibition of the enzyme dopamine
beta-hydroxylase. Clinical use of the compound was first
reported by Lawrie et al. (1964), who achieved satisfactory
blood-pressure control in 60% of their cases with guanoclor
alone, and in a further 18% with the addition of a thiazide
diuretic. They also noted a significant reduction in urinary
noradrenaline levels during guanoclor administration. Guanochlor has an affinity for the Na+/H+ exchanger ranging between 0.5 uM and 6 uM in different systems and is more potent than amiloride in all systems studied. It is suggested that guanochlor recognizes a binding site on the Na+/H+ exchanger that is distinct from the amiloride binding site.
Status:
Possibly Marketed Outside US
Source:
ZATEBRADINE HYDROCHLORIDE
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Zatebradine is a bradycardic compound that blocks hyperpolarization-activated inward current (If) through cyclic nucleotide-gated cation (HCN) channels in sinoatrial node cells. Additionally, it can block voltage-gated outward K+ (IK) currents and related neuronal hyperpolarization-activated inward current (Ih) channels but exhibits little or no activity for L-type Ca2+ (ICa) currents. When assessed through telemetric ECG recording in mice, zatebradine reduced heart rate from 600 to 200 beats per minute with an ED50 value of 1.8 mg/kg and induced increasing arrhythmia at concentrations >10 mg/kg.
Status:
Possibly Marketed Outside US
Source:
LESHCUTAN
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Methylbenzethonium chloride is a quaternary ammonium with antimicrobial activity, which is used in combination with aminoglycoside antibiotic, paromomycin (brand name LESHCUTAN) for the topical treatment of cutaneous leishmaniasis.
Status:
Possibly Marketed Outside US
Source:
LESHCUTAN
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Methylbenzethonium chloride is a quaternary ammonium with antimicrobial activity, which is used in combination with aminoglycoside antibiotic, paromomycin (brand name LESHCUTAN) for the topical treatment of cutaneous leishmaniasis.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Dihexyverine (Metaspas, Spasmodex) is an anticholinergic and direct smooth muscle relaxant (spasmolytic). Dihexyverine is sold in France under the brand name Spasmodex. It is indicated for the treatment of the gastrointestinal tract disorders. Dihexyverine is a muscarinic acetylcholine receptor antagonist.
