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

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Showing 34831 - 34840 of 34988 results

Status:
Possibly Marketed Outside US
Source:
Fenoctimine sulfate by ZYF Pharm Chemical
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Fenoctimine is a nonanticholinergic inhibitor of gastric acid secretion in dogs and rats. Fenoctimine was more potent than cimetidine in the reduction of basal acid secretion in the gastric fistula rat and inhibited the production of gastric acid stimulated by histamine, gastrin tetrapeptide or bethanechol in the chronic gastric fistula dog. This compound is not an H2-antagonist but does inhibit the H+/K+-ATPase of hog gastric mucosa. The in vitro metabolism of fenoctimine by rat liver homogenates resulted in the oxidation of the aliphatic chain at the seven carbon, initially to an alcohol and then to a ketone. The unexpectedly weak effect of fenoctimine as a gastric antisecretory agent in humans, as well as anticholinergic effects, may be due to its extensive metabolism, which is different from that seen in dog and rat. The development of fenoctimine has been discontinued for unspecified reason.
Status:
Possibly Marketed Outside US
Source:
NCT02741947: Phase 4 Interventional Completed Parkinson Disease
(2014)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Benserazide is a peripherally-acting aromatic L-amino acid decarboxylase (AADC) or DOPA decarboxylase inhibitor. Benserazide is only used in conjunction with L-dopa for the treatment of Parkinson's disease under the brand name Madopar in the UK. Madopar HBS (125 mg) is a controlled-release dosage form with 100 mg L-dopa and 25 mg benserazide.
Status:
Possibly Marketed Outside US
Source:
GASTROZEPIN by Boehringer Ingelheim
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pirenzepine is a M1 muscarinic receptor antagonist, which is prescribed for the treatment of gastric and duodenal ulcer in Europe. The drug preferentially acts on the gastric mucosa to inhibit secretion of both gastric acid and pepsin. Experiment with healthy volunteers demonstrated that pirenzepine passes the blood-brain barrier, but only to a small extent.
Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 / dopamine D2 blocking activity. It is not available in the US but marketed in other countries for prophylaxis of a migraine, occlusive peripheral vascular disease, the vertigo of central and peripheral origin, motion sickness and as an adjuvant in the therapy of epilepsy. The drug is also investigated for the treatment of schizophrenia.
Status:
Possibly Marketed Outside US
Source:
ZOPRANOL by Squibb Institute for Medical Research
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Zofenopril is an inhibitor of Angiotensin Converting Enzyme (ACE), which is approved in Europe for the treatment of hypertension and acute myocardial infarction.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Adinazolam, a benzodiazepine agonist, is an effective anxiolytic agent with antidepressant properties. It was shown, that adinazolam by itself had relatively weak benzodiazepine agonist activity, and much of the pharmacological activity belonged to its active metabolite N-desmethyladinazolam (NDMAD). Adinazolam has never been FDA approved, but it is sold as a research chemical.
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.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Fluperolone (P-1742 or Methral) is a topical fluorinated prednisolone derivative exerting an anti-inflammatory activity. It demonstrated effectivity in the treatment of various dermatoses.
Pizotifen (INN) or pizotyline (USAN), trade name Sandomigran, is a benzocycloheptene-based drug used as a medicine, primarily as a preventative to reduce the frequency of recurrent migraine headaches. Pizotifen is a serotonin antagonist acting mainly at the 5-HT2A and 5HT2C receptors. It also has some activity as an antihistamine as well as some anticholinergic activity. The main medical use for pizotifen is for the prevention of vascular headache including migraine and cluster headache. Pizotifen is one of a range of medications used for this purpose, other options include propranolol, topiramate, valproic acid and amitriptyline. While pizotifen is reasonably effective, its use is limited by side effects, principally drowsiness and weight gain, and it is usually not the first choice medicine for preventing migraines, instead being used as an alternative when other drugs have failed to be effective. It is not effective in relieving migraine attacks once in progress. Pizotifen has also been reported as highly effective in a severe case of erythromelalgia, a rare neurovascular disease that is sometimes refractory to the other drugs named above. Side effects include sedation, dry mouth, drowsiness, increased appetite and weight gain. Occasionally it may cause nausea, headaches, or dizziness. In rare cases, anxiety, aggression and depression may also occur. Pizotifen is well absorbed from the gastro-intestinal tract, peak plasma concentrations occurring approximately 5 hours after oral administration. The absorption of pizotifen is fast (absorption half life 0.5 to 0.8 hours) and nearly complete (80%). Over 90% is bound to plasma proteins. Pizotifen undergoes extensive metabolism. Over half of a dose is excreted in the urine, chiefly as metabolites; a significant proportion is excreted in the faeces. The primary metabolite of pizotifen (N-glucuronide conjugate) has a long elimination half-life of about 23 hours.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefpimizole Sodium
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Cefpimizole is an antibiotic of broad spectrum developed in Japan for the treatment of such conditions as uncomplicated gonorrhea and gynecologic infections. The drug was tested in clinical trials, however, its development was terminated.

Showing 34831 - 34840 of 34988 results