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

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Showing 131 - 140 of 297 results

Status:
US Previously Marketed
First approved in 1950

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Decamethylene disquaternary salts, with a ten-carbon (C10) chain between the quaternary groups, had the most potent curariform action in the series of polymethylene bisquaternaries. Decamethonium was used clinically as a neuromuscular blocking drug for a short time. Decamethonium was different from d-tubocurarine and that it produced a transient augmentation of contraction. C10 produces neuromuscular block by initiating some active response in the endplate or muscle fibre. Unlike d-tubocurare, decamethonium was not reversed by anticholinesterase agents.
Status:
US Previously Marketed
Source:
Sympatol
(1931)
Source URL:
First marketed in 1931
Source:
Sympatol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Oxedrine (Sympatol, p-synephrine) is a naturally occurring alkaloid molecule first appeared in Europe towards the end of the 1920s being sold as a drug under the brand name Sympatol. Oxedrine was then being prescribed as a remedy for a number of respiratory conditions, which include asthma, whooping cough, colds, and hay fever. More recently, synephrine gained popularity as a weight loss aid and it has become a favored component in the more popular brands of weight loss supplement stacks. This popularity can be attributed in part to the ban imposed on ephedra, to which it shares similar mechanisms of action. Most, if not all of the synephrine being sold as a dietary supplement is extracted and synthesized from the Citrus aurantium plant, more commonly known as bitter orange. Just like ephedrine, synephrine has vasoconstrictive abilities, although at a lesser potency compared to ephedrine. There is no mention of synephrine in editions of Drill's Pharmacology in Medicine later than the 3rd, nor is there any reference to synephrine in the 2012 Physicians' Desk Reference, nor in the current FDA "Orange Book". One current reference source describes synephrine as a vasoconstrictor that has been given to hypotensive patients, orally or by injection, in doses of 20–100 mg.
Naringenin is one of the most abundant flavonoids in natural citrus fruits and has been studied as an antioxidant and anti-inflammatory agent. Besides, it has been investigated for its ability to inhibit the growth of breast, colon, gastric and prostate cancer cells. Experiments on rodents have revealed, that naringenin is a component of Drynaria Rhizome and can enhance memory function and ameliorate Alzheimer's disease pathologies. Using the experimental autoimmune encephalomyelitis, a rodent model of human multiple sclerosis was determined that naringenin may have a potential to ameliorate autoimmune disease by favorably modulating autoimmune response. The precise mechanism of action of naringenin compound is not clear, but it is known, that it is a partial agonist of estrogen receptor that can act as a competitive antagonist in the presence of a potent (or full) agonist. In addition, it binds to collapsin response mediator protein 2 protein (CRMP2) and reduces the Aβ-induced phosphorylation of CRMP2, resulting in axonal growth facilitation.
Tramiprosate is a glycosaminoglycan mimetic designed to interfere with the actions of beta-amyloid peptides (Abeta) early in the cascade of amyloidogenic events. It is a patented variant of the amino acid taurine, which is reported to inhibit the interaction of Abeta with endogenous glycosaminoglycans and thereby prevent beta-sheet formation. Preclinical data have shown that tramiprosate reduces brain and plasma levels of Abeta, prevents fibril formation and exerts cytoprotective effects in the brain. The pharmacological effects have also been demonstrated in clinical trials of patients with mild to moderate Alzheimer's disease. Promising findings for the efficacy of tramiprosate, indicated by improvement or stabilization of cognitive function, have been shown in phase II clinical trials and open-label extensions of these studies. Furthermore, tramiprosate appears to be well tolerated with no reports of safety concerns. Tramiprosate is in phase III clinical trial for the treatment of Alzheimer's disease.
Status:
Possibly Marketed Outside US
Source:
Canada:SKATOLUM
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Skatole or 3-methylindole is a mildly toxic white crystalline organic compound belonging to the indole family. It is formed in the intestine by the bacterial decomposition of l-tryptophan and found in fecal matter, to which it imparts its characteristic odor. Skatole is a partial AhR agonist. Skatole is used in perfume compositions and in artificial Civet bases.
Status:
Possibly Marketed Outside US
Source:
Serenal by Sakai, Y. et al.
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



Oxazolam is a prodrug (precursor) for the benzodiazepine desmethyl-diazepam (nordazepam) and is itself a metabolic product of other benzodiazepines. It has anxiolytic, sedative, and anticonvulsant properties. It is a GABA-A receptor agonist. Oxazolam is marketed in Japan under the brand name Serenal. It is usually used to treat anxiety, tension, depression, and sleeping disorder in neurosis. It is used to treat somatic symptoms in psychosomatic disorders (gastrointestinal diseases, circulatory diseases, endocrine diseases, and autonomic dystonia), anxiety, tension, and depression. It is also used as a preanesthetic medication.
Status:
Possibly Marketed Outside US
Source:
Oxyfedrine by Chemiewerk Homburg
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Oxyfedrine, an amino ketone derivative and partial agonist at beta receptors, has been shown to have potent antianginal properties and to increase coronary blood flow in normal and ischemic myocardial regions.
Status:
Possibly Marketed Outside US
Source:
Meptid by Wyeth
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Meptazinol is a unique opioid analgesic. Binding studies suggest a relative selectivity for mu-1 opioid receptor sites. Meptid is indicated for the treatment of moderate to severe pain, including post-operative pain, obstetric pain and the pain of renal colic. The most commonly reported adverse reactions after treatment with meptazinol are nausea, vomiting, dizziness, diarrhoea and increased sweating, constipation, abdominal pain, rash, vertigo, headache, drowsiness, somnolence and dyspepsia.
Xamoterol (ICI 118,587) is a partial agonist of beta1-adrenoceptors. Xamoterol acts on the cardiac beta 1-adrenergic receptor, modifies the response of the heart to variations in sympathetic activity. At rest, it produces modest improvements in cardiac contractility, relaxation, and filling without increase in myocardial oxygen demand. The improvements are maintained during exercise although the attendant tachycardia is attenuated. The beneficial effects of xamoterol on both systolic and diastolic function suggested that it would be effective in patients with mild-to-moderate heart failure, and this was demonstrated in small placebo-controlled studies where effort tolerance and symptoms were improved. Xamoterol produced improvements in exercise capacity, clinical signs, symptoms and quality of life with a low incidence of adverse experiences. Xamoterol is effective as monotherapy in heart failure.
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.

Showing 131 - 140 of 297 results