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

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Showing 6201 - 6210 of 12702 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Norcholestenol iodomethyl I-131 (I-131 adosterol) is a cholesterol analogue, used for local diagnosis of areas with adrenal gland disorder. Upon entering the cell, adosterol is converted to a metabolically inert ester, and becomes trapped in the cell.
Status:
Possibly Marketed Outside US
Source:
Japan:Bucladesine Sodium
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Bucladesine is a cyclic nucleotide derivative which mimics the action of endogenous cAMP and is a phosphodiesterase inhibitor. The compound is used in a wide variety of research applications because it mimics cAMP and can induce normal physiological responses when added to cells in experimental conditions. cAMP is only able to elicit minimal responses in these situations. The neurite outgrowth instigated by bucladesine in cell cultures has been shown to be enhanced by nardosinone. Recently, the effect of bucladesine as a cAMP analog has been studied on the pentylenetetrazol-induced seizure in the wild-type mice. The data showed that bucladesine (300nM/mouse) reduced the seizure latency and threshold. In addition they found that combination of bucladesine and pentoxyfillin has additive effect on seizure latency and threshold. Bucladesine is more lipophilic than cAMP and in contrast to cAMP capable of penetrating cell membranes. Bucladesine interferes with different protein kinases which are normally activated by cAMP. Bucladesine has undergone in the past clinical developments as systemic treatment for cardioprotection and as topical treatment to improve wound healing. In Japan, a bucladesine ointment (Actosin® ointment; Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan) was marketed to treat skin ulcers. Clinical studies have shown favourable effects on diabetic foot ulcers or decubitus, but the compound was later withdrawn despite good tolerability. One possible reason for the withdrawal may be the odour of the cream formulation which can be related to the hydrolytic cleavage in aqueous solutions resulting in release of butyric acid.
Status:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Haloxon is an organophosphorus anthelmintic once used against nematodes of the abomasum and small intestine in ruminants. Haloxon is an organophosphorus cholinesterase antagonist. Laboratory and field trials with 7-day-old, 14-day-old and adult infections of the common gastrointestinal nematodes in 600 sheep showed that Haloxon at a dose rate of 30 to 55 mg. per kg. body-weight was a very highly efficient anthelrnintic. The drug was particularly effective against all stages of Haemonchus contenus, Trichostrongylus spp. and Coopería curticei; it was more active against adult than against larval Ostertagia spp" and Nematodirus spp. High activity was also reported against Strongyloides papillosus, Bunostomum trigono-cephalum and Oesophagostomum venulosumum but not against Trichuris avis nor Chabertia ovina.
Status:
Possibly Marketed Outside US
Source:
Fohnetten N by Macht, D.I.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Benzyl mandelate is of comparatively low toxicity on the one hand and is pharmacologically effective on the other hand. The most important pharmacological action of the drug is on smooth muscle. Benzyl mandelate has been used for its antispasmodic actions. It has also been included in preparations with analgesics in an attempt to increase the analgesic effect. Drugs with benzyl maleate were indicated for the angina prevention and for pain condition treatment.
Status:
Possibly Marketed Outside US
Source:
Japan:Lynestrenol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Lynestrenol is a progestogen structurally related to norethisterone; it is used singularly, or as the progestogenic component of oral contraceptives. It is also used in treatments for menstrual disorders. Lynestrenol is typically used as an oral contraceptive, but also for the treatment of menstrual disorders like: Oligo-menorrhea and hypo-menorrhea; Polymenorrhoea; Fibrocystic mastopathy; Endometriosis; Endometrial carcinoma and/or metastases etc. As a synthetic oral progestogen, Lynestrenol has similar effects as that of the natural progesterone hormone. It has a strong progestational effect on the uterine endometrium by transforming the proliferative endometrium into a secretory one. It also inhibits the secretion of gonadotropin, suppresses maturation of follicles in the ovaries and ovulation, and reduces menstrual bleeding. Lynestrenol has minimal estrogenic, androgenic and anabolic effects.
Fluspirilene, a neuroleptic drug, which is used clinically to treat schizophrenic patients, by blocking of dopamine receptors, especially the dopamine D2 receptors. Fluspirilene also displays calcium channel-blocking activity; it inhibits glutamate release primarily by reducing presynaptic Ca2+ influx via N-type Ca2+ channels that also may contribute to the antischizophrenic action of the drug. Recently in the frame of a project of drugs repositioning, fluspirilene was studied as an anti-cancer drug. It was found, that fluspirilene demonstrates a significant inhibitory effect on the proliferation and invasion of glioma cells. Thus, it can be a promising drug for the treatment of glioblastoma. In addition, fluspirilene, as a potential cyclin-dependent kinase 2 inhibitor, was investigated in animal models for the treatment of human hepatocellular carcinoma. Taken into account that fluspirilene has a long history of safe human use, the drug can be applicable in clinical therapy for cancer’s disease immediately.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Nicoboxil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Nicoboxil is a nicotinate used in topical preparations as a rubefacient which has vasodilating properties mediated by prostaglandin. Nicoboxil is a component of finalgon® (nonivamid and nicoboxil), a topical cream for joint and muscle pains. The hyperaemic effect of Nicoboxil has an earlier onset and it is more intense than the nonivamide hyperaemic effect.
Status:
Possibly Marketed Outside US
Source:
Canada:P-TERT-PENTYLPHENOL
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



4-tert-Pentylphenol (4-tert-Amylphenol) is used to make phenolic resins (novolaks and resoles), which are used in paints and varnishes and as printing ink resins. The ethoxylated novolaks are used as oil field demulsifiers. Because of the high cost of 4-tert-pentylphenol, which is related to the high cost of the starting material, many of the resin applications have been reformulated using 4-tertbutylphenol. The substance is also used as a germicide in cleaning solutions, although it is being replaced by quaternary ammonium salts. Kegley et al. (2007) confirm that both the substance and its potassium and sodium salts are antimicrobial or fungicidal active ingredients of several disinfectant products that are currently registered with the US authorities. It appears that some of these products are used in animal husbandry, including the control of highly infectious diseases such as avian influenza (US EPA, 2007d). 4-tert-Amylphenol was used as an esterogen receptor (ER) ligand.
Opipramol (Insidon, Pramolan, Ensidon, Oprimol) is an antidepressant and anxiolytic used in Germany and other European countries. Although it is a member of the tricyclic antidepressants, opipramol's primary mechanism of action is much different in comparison, it doesn’t represent a tricyclic antidepressant drug as it does not inhibit the neuronal uptake of norepinephrine and/or serotonin. Opipramol also acts as a low to moderate affinity antagonist for the D2, 5-HT2, H1, H2, and muscarinic acetylcholine receptors. H1 and H2 receptor antagonism account for its antihistamine effects, and muscarinic acetylcholine receptor antagonism is responsible for its anticholinergic properties. Opipramol was developed by Schindler and Blattner in 1961. Opipramol is typically used in the treatment of generalized anxiety disorder (GAD) and somatoform disorders. Its anxiolysis becomes prominent after only one to two weeks of chronic administration. Upon first commencing treatment, opipramol is rather sedating in nature due to its antihistamine properties, but this effect becomes less prominent with time. The therapy with Opipramol indicates an additional therapy with neuroleptics, hypnotics and tranquilizers (e.g. Barbiturates, Benzodiazepines). Therefore, it should be noted that some specific reactions, particularly CNS depressant effects could be intensified and an intensification of common side effects may occur. If necessary the dosage may be reduced. Co-administration with alcohol can cause stupor. MAO Inhibitors should be discontinued at least 14 days before the treatment with Opipramol. Concomitant use of Opipramol with β-blockers, antiarrhythmics (of class 1c), as well as drugs from tricyclic antidepressant group and preparations which influence the microsomal enzyme system, can lead to change in plasma concentration of these drugs. Co-administration of neuroleptics (example- haloperidol, risperidone) can increase the plasma concentration.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Methisazone is N-methyl-isatin beta-thiosemicarbazone. This is one of a series of isatin beta-thiosemicarbazones which have been shown in the laboratory to have antiviral activity against vaccinia and variola viruses. It has been reported to be effective for smallpox prophylaxis.

Showing 6201 - 6210 of 12702 results