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

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Showing 11221 - 11230 of 11247 results

cis-Dosulepin is a stereoisomer of Dothiepin (trade name Prothiaden, Dothep, Thaden, and Dopress; Dosulepin (INN, BAN) a tricyclic antidepressant that is used in several European and South Asian countries, as well as Australia, South Africa, and New Zealand. Dosulepin is used for the treatment of the major depressive disorder and neuropathic pain. Dosulepin is only Therapeutic Goods Administration and Medicines and Healthcare products Regulatory Agency approved for the treatment of the major depressive disorder. Dothiepin is not used in the United States. The central action of cis-dosulepin was compared with that of its antidepressant stereoisomer trans-dosulepin, cis-dosulepin exerted weaker anti-reserpine, anti-tetrabenazine, and 3H-5-HT (serotonin) uptake inhibiting actions than trans-dosulepin, but cis-dosulepin's inhibition of 3H-dopamine and 3H-norepinephrine uptake was slightly more potent than that of trans-dosulepin. On the other hand, cis-dosulepin exhibited extremely potent anticholinergic action in oxotremorine induced tremor, isolated ileum and the 3H-quinuclidinyl benzilate binding test. It also showed potent apomorphine enhancing the action and shortened the period of immobility in the forced swimming test in animals.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Iprindole under the brand name Prondol was used as an antidepressant but now is no longer marketed. It possesses the beta-adrenergic properties and has an indirect beta 2-mimetic effect.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Bamifylline (or bamiphylline), a selective antagonist of the A1 adenosine receptor, was studied in the therapy of asthmatic syndromes.
Status:
Possibly Marketed Outside US
Source:
Majeptil by Wilson, W.L.|Shane, L.L.|Moyer, J.H.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Thioproperazine is a potent neuroleptic with antipsychotic properties. Thioproperazine has a marked cataleptic and antiapomorphine activity associated with relatively slight sedative, hypothermic and spasmolytic effects. It is virtually without antiserotonin and hypotensive action and has no antihistaminic property. It is used for the treatment of all types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes. Overdosage may result in severe extrapyramidal symptoms with dysphagia, marked sialorrhea, persistent and rapidly increasing hyperthermia, pulmonary syndrome, state of shock with pallor and profuse sweating, which may be followed by collapse and coma.
Status:
Possibly Marketed Outside US
Source:
Mydocalm by Richter, G.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Tolperisone is a centrally acting muscle relaxant first synthesized in 1956 and used in clinical practice since the 1960’s. Tolperisone is an aryl alkyl β-aminoketone with an asymmetric carbon atom α to the carbonyl group. The dextrorotatory enantiomer was reported less effective, however, no detailed analyses of the enantiomers are available. The precise mechanism of action of tolperisone is not fully known. The most prominent effect of tolperisone is its inhibitory action on pathways of spinal reflexes. It suppresses the mono and polysynaptic reflex transmission by both pre-synaptic and post-synaptic mechanisms.
Status:
Withdrawn

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Pangamic acid (6-O-(dimethylaminoacetyl)-D-gluconic acid) has been detected 1938 and described as a natural, universally occurring substance with multiple biological and medical functions. In this respect pangamic acid has been worldwide on the market since decades as a drug stimulating cellular respiration. In addition to the natural pangamic acid, diisopropylammonium dichloroacetate (DIPA), a synthetic product not found in biological material, is on the market requesting similar biological functions. Pangamic acid is the name given to a product originally claimed to contain D-gluconodimethyl aminoacetic acid, which was obtained from apricot kernels and later from rice bran. It is also referred to as vitamin B15, but pangamic acid is not generally recognized as a vitamin. Despite serious safety concerns, pangamic acid is used for improving exercise endurance; treating asthma and related diseases, skin conditions including eczema, lung problems, painful nerve and joint conditions, cancer, and arthritis; improving the oxygenation of the heart, brain, and other vital organs; and “detoxifying” the body. It is also used for treating alcoholism, hangovers, and fatigue; protecting against urban air pollutants; extending cell life; strengthening the immune system; lowering bloodcholesterol levels; and assisting in hormone regulation. Since there is no standard identity for the chemicals in pangamic acid, how it might work is unknown. Although pangamic acid is also called vitamin B15, there is no research that shows it is required by the body, as the term “vitamin” would suggest. The United States Food and Drug Administration has recommended seizing any chemicals advertised as pangamic acid and restraining the importation and interstate shipment of pangamic acid on the grounds that pangamic acid and pangamic acid products are unsafe for use and have no known nutritional properties
Status:
Withdrawn

Class (Stereo):
CHEMICAL (RACEMIC)

Aminorex is an anorectic stimulant drug. Aminorex inhibits norepinephrine and dopamine transporters with IC50 of 0.33 and 0.85 uM. It was briefly available as an appetite suppressant in the 1960s in Switzerland, Germany, and Austria, but was found to cause pronounced vasoconstriction in the pulmonary vasculature, and was withdrawn from the market in 1972 due to several cases of fatal and life-threatening pulmonary hypertension. In the USA aminorex is an illegal schedule I drug.
Status:

Class (Stereo):
CHEMICAL (RACEMIC)

CLOMACRAN, a non-phenothiazine tricyclic compound, is an antipsychotic drug.
Doxepin is a dibenzoxepin tricyclic antidepressant marketed worldwide. It is a white crystalline solid readily soluble in water, lower alcohols and chloroform. The mechanism of action of doxepin is not definitely known. It is not a central nervous system stimulant nor a monoamine oxidase inhibitor. The current hypothesis is that the clinical effects are due, at least in part, to influences on the adrenergic activity at the synapses so that deactivation of norepinephrine by reuptake into the nerve terminals is prevented. Antidepressants may increase risk of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults (18–24 years of age) with major depressive disorder and other psychiatric disorders. Drowsiness is the most commonly noticed side effect. This tends to disappear as therapy is continued. Other infrequently reported CNS side effects are confusion, disorientation, hallucinations, numbness, paresthesias, ataxia, extrapyramidal symptoms, seizures, tardive dyskinesia, and tremor. : Cardiovascular effects including hypotension, hypertension, and tachycardia have been reported occasionally. Skin rash, edema, photosensitization, and pruritus have occasionally occurred. Eosinophilia has been reported in a few patients. There have been occasional reports of bone marrow depression manifesting as agranulocytosis, leukopenia, thrombocytopenia, and purpura. Doxepin is used to treat depression, anxiety disorders, itchiness, trouble sleeping, and as a second-line treatment of chronic idiopathic urticaria (hives). Its oral formulations are FDA-approved for the treatment of depression, anxiety, and insomnia and its topical formulations are FDA-approved the short-term management (up to 8 days) of atopic dermatitis and lichen simplex chronicus. Whereas in Australia and the UK, the only licensed indication(s) is/are in the treatment of major depression and pruritus in eczema, respectively.

Showing 11221 - 11230 of 11247 results