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

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Showing 451 - 460 of 462 results

Perhexiline, 2-(2,2-dicyclohexylethyl)piperidine, is an anti-anginal drug. Perhexiline reduces fatty acid metabolism through the inhibition of carnitine palmitoyltransferase, the enzyme responsible for mitochondrial uptake of long-chain fatty acids. Perhexiline is used for reducing the frequency of moderate to severe attacks of angina pectoris due to coronary artery disease in patients who have not responded to other conventional therapy or in whom such therapy may be contraindicated. Heart Metabolics Limited is developing perhexiline for the treatment of hypertrophic cardiomyopathy
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Carbuterol is a beta-adrenergic bronchodilator with selectivity for bronchial smooth muscle relative to cardiac and vascular tissues of several species including man. In vitro studies demonstrated that carbuterol was a direct acting beta-adrenergic agonist, not dependent on endogenous catecholamine release, and was devoid of alpha-adrenergic agonist activity. The activity of the racemate was shown to reside primarily in the l-enantiomer. Carbuterol inhibited immunologically induced release of histamine and slow reacting substance of anaphylaxis from passively sensitized fragmented rhesus monkey lung and also inhibited passive cutaneous anaphylaxis in rats. Acute toxicity studies in mice, rats and guinea pigs indicated a wide safety margin for carbuterol. Carbuterol is a safer and more effective bronchodilator than ephedrine.
Perhexiline, 2-(2,2-dicyclohexylethyl)piperidine, is an anti-anginal drug. Perhexiline reduces fatty acid metabolism through the inhibition of carnitine palmitoyltransferase, the enzyme responsible for mitochondrial uptake of long-chain fatty acids. Perhexiline is used for reducing the frequency of moderate to severe attacks of angina pectoris due to coronary artery disease in patients who have not responded to other conventional therapy or in whom such therapy may be contraindicated. Heart Metabolics Limited is developing perhexiline for the treatment of hypertrophic cardiomyopathy
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Reproterol is a short-acting β2 adrenoreceptor agonist used in the treatment of asthma. Reproterol increases the generation of cAMP in isolated peripheral blood monocytes in vitro more effectively than does orciprenaline. In the presence of the highly potent but nonselective ß-antagonist, propranolol, the cAMP-generating action of reproterol was inhibited only partially. Reproterol has gained wide use when it was licensed as a fixed combination therapy with cromoglycate. Until today, the bronchodilator effects of reproterol and the bronchoprotective and anti-inflammatory actions of cromoglycate combined in one inhaler remain the successful fixed combination of a disease-modifying and symptomatic drug for the treatment of asthma.
Status:
Possibly Marketed Outside US
Source:
Japan:Carumonam Sodium
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



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)

Apalcillin is a naphthydridine derivative of ampicillin. Apalcillin has a broad spectrum of antibacterial activity that is very similar to that of piperacillin, except that apalcillin is significantly more active against Pseudomonas aeruginosa and Acinetobacter spp. Against Acinetobacter spp., apalcillin is uniquely active, compared to the other penicillins and comparison drugs. Strains producing high amounts of β-lactamases do become resistant to apalcillin. PAH (p-aminohippurate) clearance was significantly decreased during apalcillin infusion. Apalcillin appeared to compete with PAH for proximal tubular secretion but induced no further renal dysfunction.
Status:
Possibly Marketed Outside US
Source:
Japan:Cetraxate Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Cetraxate is an oral gastrointestinal medication, mucosal protectant. Cetraxate might indirectly stimulate capsaicin-sensitive afferent nerves and increase mucosal blood flow, and that this may be a key mechanism underlying its gastroprotective action. Cetraxate prevents gastric mucosal blood flow decrease in H. pylori-infected patients. It is usually used to improve gastric mucosal lesion in acute gastritis or acute exacerbation of chronic gastritis and to treat gastric ulcer. The most commonly reported adverse reactions include constipation, rash, nausea, vomiting, dry mouth and diarrhea.
Status:
Possibly Marketed Outside US
Source:
Japan:Temocapril Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Temocapril is a prodrug-type angiotensin-I converting enzyme (ACE) inhibitor not approved for use in the United States but is approved in Japan and South Korea. Temocapril can also be used in hemodialysis patients without risk of serious accumulation.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Acefylline is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. Acephylline piperazine is a theophylline derivative with a direct bronchodilator action. It has the advantages over theophylline in being far less toxic and producing minimal gastric irritation. It is indicated for the treatment of asthma, emphysema, acute and chronic bronchitis associated with bronchospasm.Acefylline relaxes smooth muscles, relieves bronchospasm & has a stimulant effect on respiration. It stimulates the myocardium & central nervous system, decreases peripheral resistance & venous pressure & causes diuresis. The mechanism of action is still not clear, inhibition of phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism & effects on intracellular calcium. Sodium phenobarbital is a non-selective central nervous system depressant that is primarily used as sedative-hypnotic.
Status:
Withdrawn

Class (Stereo):
CHEMICAL (RACEMIC)



Pronetalol (Pronethalol) is a nonselective beta-adrenoceptor antagonist that is structurally related to propranolol. Pronethalol displays a ∼125–150-fold lower affinity (140–830 nM) for beta-adrenoceptors than propranolol (1.1–5.7 nM). Pronethalol was the first beta-adrenoceptor antagonist used for the treatment of coronary heart disease and cardiac arrhythmias. Pronethalol is a cationic-amphiphilic agent that exhibits membrane-stabilizing effects that are unrelated to beta-adrenoceptor blockade. Pronetalol itself never came into widespread clinical use; it was found to produce thymic tumors in mice, and was discarded in favor of a similar, safer compound, ICI 45,520.

Showing 451 - 460 of 462 results