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

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Showing 1951 - 1960 of 3134 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

1,6-Dimethyl-3-carbethoxy-4-oxo-6,7,8,9-tetrahydro-homopyrimidazol (rimazolium, MZ-144) is an analgesic (non-narcotic). It proved to be effective in all the analgesic assays used (independently of the nociceptive stimulus applied) (hot plate, tail flick, writhing tests, Randall-Selitto test, tail clip, surgical pain) differing in this respect from the nonsteroidal antiinflammatory analgetics. Rimazolium lacks the capacity of producing opiate-like physiological dependence. Also rimazolium fails to show any indication of narcotic-like abuse liability by any of clinical assessments. Rimazolium is registered in Hungary under the brand name Probon. In Hungary among analgesics Probon is the first of choice especially in case of chronic pain accompanying chronic respiratory tract diseases.
Esatenolol is the (S) enantiomer of atenolol, a beta1-adrenergic receptor antagonist. Only (S)-atenolol, but not (R)-atenolol, contributes to the beta-blocking effect of currently used racemic atenolol since the same effect can be elicited with the (S)-enantiomer alone. Pure (S)-atenolol has been launched in India for the treatment of hypertension and angina pectoris.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)

Cyfluthrin, a pyrethroid, is one of the components of Temprid, which is used as an insecticide to control most insect pests. Cyfluthrin acts as a stomach poison and through contact and stomach poisoning, it attacks the nervous system; resulting in swift debilitation and has a long residual effect. Target insects include ants, silverfish, cockroaches, grain beetles.
Carumonam is a monobactam antibacterial agent. It was highly active in vitro against members of the family Enterobacteriaceae, Pseudomonas aeruginosa, and Haemophilus influenzae and weakly active against Streptococcus pneumoniae, but it was not active against Staphylococcus aureus. The excellent activity of carumonam against Gram-negative bacteria is related to its high affinity for their penicillin-binding proteins. It is indicated for the treatment of urinary tract infections, chronic respiratory infections, biliary tract infections, peritonitis, sepsis. Another factor that contributes to the excellent activity of carumonam against Gram-negative bacteria is its resistance to beta-lactamases. Adverse effects of the carumonam were limited to phlebitis at the intravenous infusion site; bloody diarrhea.
Nimorazole is an antimicrobial with activity against anaerobic bacteria and protozoa. Its actions and properties are similar to metronidazole. It has also been used in trials studying the treatment of Hypoxia, Radiotherapy, Hypoxic Modification, Gene Profile, Gene Signature, and Head and Neck Squamous Cell Carcinoma, among others. Azanta is developing, nimorazole, as an oral hypoxic radio-sensitiser for the treatment of patients with head and neck cancer who are undergoing radiotherapy. Previously, nimorazole has been approved for use as an anti-protozoal agent and has been launched worldwide. Nimorazole, for the treatment of head and neck cancer patients undergoing radiotherapy received orphan designation by EMA in 2011.
Efaproxiral is a synthetic, small molecule, radiation-sensitising agent being developed by Allos Therapeutics primarily for the treatment of cancer. It works by binding and allosterically stabilising deoxyhaemoglobin in hypoxic regions of tumour tissue. This increases oxygen uptake of the tumour tissue and restores its sensitivity to radiation therapy, making therapy potentially more successful. But no benefit was seen for efaproxiral in phase III clinical trials. The only serious adverse effect detected was hypoxaemia. Efaproxiral is explicitly excluded from the 2012 World Anti-Doping Agency list of Prohibited Substances and is explicitly included in the Prohibited Methods section M1 as a forbidden procedure to alter the oxygen-haemoglobin dissociation curve in order to allosterically modify haemoglobin.
Status:
Possibly Marketed Outside US
Source:
Unknown by Duanmu, C. et al.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Proxazole or 3-alpha-Phenyl-propyl-5-beta-diethylaminoethyl-1,2,3-oxadiazole is a drug used for functional gastrointestinal disorders. It’s an unusual drug because it possesses both anti-inflammatory and antispasmodic properties and because each of these two properties has some uncommon features. The antiinflammatory action takes place mostly against edematous responses and is devoid of ulcerogenic effects which are instead produced by most anti-inflammatory drugs; moreover proxazole prevents indomethacin-induced ulcers without exerting any anti-secretory effect. The antispasmodic activity results in a specific inhibition of smooth muscle spasm, both at the vascular and at the intestinal level, without significant interferences with the physiologic activity of that tissue.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Ethybenzatropine (Ponalid) is an anticholinergic and antihistaminergic drug. It was used as an antiparkinsonian agent. A significant increase in the duration of action of levodopa-induced improvement in parkinsonian symptoms was observed following the administration of ethybenzatropine. Ethybenzatropine also improved, or tended to improve the duration and seventy of onset and end-of-dose levodopa-induced dyskinesias. Thus when levodopa is administered together with etybenzatropine, its length of action on parkinsonian symptoms is prolonged.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Niperotidine is an H2 antagonist structurally related to ranitidine. H2 antagonists inhibit gastric acid secretion by selectively blocking histamine receptor type 2. Niperotidine was proposed for the treatment of peptic ulcer. Bedtime dose of niperotidine inhibits nocturnal gastric acid secretion in healthy subjects. The duration of niperotidine action was 5 to 7 hours. Twenty-five cases of acute hepatitis (including one death from fulminant hepatitis) associated with niperotidine use were reported in Italy between March and August 1995 and drug was withdrawn from the market. The methylenedioxy group of niperotidine is known to undergo metabolism to catechol and quinone metabolites.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Altizide, a thiazide diuretic, and aldosterone antagonist, in combination with spironolactone was marketed under brand name Aldactazine to treat patients with mild to moderate hypertension. In addition, Aldactazine was investigated for the treatment of congestive cardiac insufficiency.

Showing 1951 - 1960 of 3134 results