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Status:
Possibly Marketed Outside US
Source:
levorphanol by Hoffman-La Roche
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Levorphanol Sulfate (brand name Levo-Dromoran) is an opioid medication used to treat moderate to severe pain. It is one of two enantiomers of the compound racemorphan and was first described in Germany in 1948 and approved for use in the United States in 1953 as an orally active, morphine-like analgesic. Levorphanol is approved for use in moderate to severe pain where an opioid analgesic is appropriate. Levorphanol has a wide range of activities including mu-opioid agonism, delta agonism, kappa1 and kappa3 receptor agonism, N-methyl-D-aspartate receptor antagonism and reuptake inhibition of both norepinephrine and serotonin. This multimodal profile might prove effective for pain syndromes that are refractory to other opioid analgesics, such as central and neuropathic pain and opioid-induced hyperalgesia. Levorphanol is well suited as a first-line opioid and can also be used during opioid rotation. It has no known effect on the cardiac QT interval or drug-drug interactions involving hepatic cytochrome P450s enzymes. In these regards, levorphanol may offer a superior safety profile over methadone and other long-acting opioids. Despite its prospective value of multiple mechanisms of action and the potential for treating various types of pain, levorphanol use has been largely supplanted by other recently approved opioids. Its waning use over the years has caused it to be referred to as the “Forgotten Opioid” and resulted in what some consider its underutilization. In fact, levorphanol is relatively unfamiliar to most prescribers.
Status:
Possibly Marketed Outside US
Source:
Alodorm by Good, M.L.|Bryan, S.E.
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Nitrazepam (trade names: Alodorm, Apodorm, Arem, Mogadon, Nitrados, Nitrazadon, Nitrosun, Ormodon, Paxadorm, Remnos, and Somnite) is a hypnotic drug of the benzodiazepine class, indicated for the short-term relief of severe, disabling anxiety and insomnia. Nitrazepam has sedative and motor-impairing properties, as well as amnestic, anticonvulsant, and skeletal muscle relaxant effects. Nitrazepam is used to treat short-term sleeping problems (insomnia), namely difficulty falling asleep, frequent awakening, early awakening, or a combination of each. Nitrazepam is sometimes tried to treat epilepsy when other medications fail. It has been found to be more effective than clonazepam in the treatment of West syndrome, which is age-dependent epilepsy, affecting the very young. In uncontrolled studies, nitrazepam has shown effectiveness in infantile spasms and is sometimes considered when other anti-seizure drugs have failed. However, drowsiness, hypotonia, and most significantly tolerance to anti-seizure effects typically develop with long-term treatment, generally limiting Nitrazepam to acute seizure management. More common side effects may include: Central nervous system depression, including somnolence, dizziness, depressed mood, rage, violence, fatigue, ataxia, headache, vertigo, impairment of memory, impairment of motor functions, hangover feeling in the morning, slurred speech, decreased physical performance, numbed emotions, reduced alertness, muscle weakness, double vision, and inattention have been reported. Unpleasant dreams and rebound insomnia have also been reported. Nitrazepam is a long-acting benzodiazepine with an elimination half-life of 15–38 hours (mean elimination half-life 26 hours).
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Iometopane (RTI-55, beta-CIT) is a cocaine congener, binding to the neuronal dopamine and serotonin reuptake transporters affinity of Kd = 0.3 nM. Radiopharmaceutical forms of RTI-55 are used in single-photon emission computer tomography. Radioisotops 123I and 125I are favored, but 124I also used as a positron emitter to diagnose Parkinson's Disease.
Status:
Possibly Marketed Outside US
Source:
Brintellix by Lundbeck
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Vortioxetine DL-lactate is a lactate salt of vortioxetine and its chemical name is 1-[2-(2,4-dimethylphenylsulfanyl)-phenyl]-piperazine
(RS)-2-hydroxypropanoate. Vortioxetine DL-lactate is manufactured from the milled Vortioxetine hydrobromide via the nonisolated
free base. One site is involved in the manufacture of the lactate salt of Vortioxetine. Vortioxetine is an antidepressant for the treatment of major depressive disorder. Unlike the film-coated tablets where a hydrobromide salt of the active substance is used, the oral
drops formulation contains vortioxetine DL-lactate as the active substance which shows higher solubility in polar solvents. Vortioxetine is a novel multimodal antidepressant that acts as a serotonin (5-HT)3, 5-HT7, and 5-HT1D receptor antagonist; 5-HT1B receptor partial agonist; 5-HT1A receptor agonist; and 5-HT transporter inhibitor in vitro.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
There is no available information about this compound
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ABSOLUTE)
Glycitin (4'-Hydroxy-6-Methoxyisoflavone-7-D-Glucoside) is a soy isoflavone. Isoflavone mixtures from soybean containing glycitin exert anti-obese and antidiabetic, antineoplastic, antioxidant effects. Isoflavone supplementation in healthy males may enhance cognitive processes which appear dependent on oestrogen activation. Glycitin underwent hydrolysis of the beta-glycoside moiety and little further biotransformation, leading to high plasma glycitein concentrations.
Status:
Possibly Marketed Outside US
Source:
Calblock by Daiichi Sankyo|Ube Industries
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Azelnidipine is a dihydropyridine calcium channel antagonist being jointly developed by Daiichi Sankyo Inc (formerly Sankyo) and Ube Industries. Azelnidipine is a L-type calcium channel antagonist. Azelnidipine was approved by Pharmaceuticals and Medicals Devices Agency of Japan (PMDA) on Jan 31, 2003. Azelnidipine is indicated for the treatment of hypertension. Its trend name is Calblock. Azelnidipine has two enantiomers (R-(−)- and S-( )-enantiomers) due to an asymmetric carbon at the 4-position, and the (R)-(−) enantiomer of dihydropyridine calcium antagonists is considered to possess intrinsic pharmacological activity. The
pharmacological action of azelnidipine resides in the (R)-enantiomer. This is in marked contrast to other calcium channel blocker (CCB) in which the (S)-enantiomer is responsible for the biological activity. There were no
significant differences in the inhibitory effects on TGF-b1-induced expression of COL1A1 mRNA among vitamin E - pretreated LX-2 cells
treated with azelnidipine (racemate), (R)-(-)-azelnidipine
or (S)-( )-azelnidipine, although the L-type
voltage-operated calcium channel blocking activity of (R)-(-)-
enantiomer was more potent than that of the (S)-( )-
enantiomer.
Status:
Possibly Marketed Outside US
Source:
Calblock by Daiichi Sankyo|Ube Industries
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Azelnidipine is a dihydropyridine calcium channel antagonist being jointly developed by Daiichi Sankyo Inc (formerly Sankyo) and Ube Industries. Azelnidipine is a L-type calcium channel antagonist. Azelnidipine was approved by Pharmaceuticals and Medicals Devices Agency of Japan (PMDA) on Jan 31, 2003. Azelnidipine is indicated for the treatment of hypertension. Its trend name is Calblock. Azelnidipine has two enantiomers (R-(−)- and S-( )-enantiomers) due to an asymmetric carbon at the 4-position, and the (R)-(−) enantiomer of dihydropyridine calcium antagonists is considered to possess intrinsic pharmacological activity. The
pharmacological action of azelnidipine resides in the (R)-enantiomer. This is in marked contrast to other calcium channel blocker (CCB) in which the (S)-enantiomer is responsible for the biological activity. There were no
significant differences in the inhibitory effects on TGF-b1-induced expression of COL1A1 mRNA among vitamin E - pretreated LX-2 cells
treated with azelnidipine (racemate), (R)-(-)-azelnidipine
or (S)-( )-azelnidipine, although the L-type
voltage-operated calcium channel blocking activity of (R)-(-)-
enantiomer was more potent than that of the (S)-( )-
enantiomer.
Status:
Possibly Marketed Outside US
Source:
Valerian by Bos, R. et al.
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Valerian is on the FDA’s list of substances that are generally recognised to be safe (GRAS). The root oil and extracts may be used as spice or seasoning. Valerian is most commonly used for sleep disorders. The essential oil of valerian contains a variety of compounds including valerenic acid and its derivatives, hydroxyvalerenic acid, acetoxyvalerenic acid and valerenal.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (RACEMIC)
HA-242, a benzodioxan derivative, is a muscle relaxant. It can be used for the treatment of central nervous muscular spasticity. Was marketed under the name Quiloflex. Quiloflex (HA-242) is a reflex inhibitor used in human medicine for the symptomatic treatment of spasticity due to pyramidal tract lesions. Quiloflex was also used for casting cattle and horses, and although well tolerated at a dosage of 1-8 mg/kg body wt. in cattle, it was unsuitable for use in this species as the onset of relaxation was slow and the sedation prolonged. A dosage of 6 mg/kg i/m in horses gave relaxation suitable for surgery in 30 min.