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

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Showing 91 - 100 of 657 results

Status:
Investigational
Source:
INN:cetamolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Cetamolol is a beta adrenergic antagonist with intrinsic sympathomimetic activity, patented by Imperial Chemical Industries Ltd for cardiovascular disease treatment. The average plasma half-life of cetamolol is 6.4 hours in humans and peak serum levels are reached 1 to 2 hours after drug intake; oral doses as low as 10 mg produced significant reductions in exercise-induced tachycardia 24 hours after drug administration. Cetamolol is approximately three times as potent as atenolol in blocking exercise-induced tachycardia.
Status:
Investigational
Source:
INN:exaprolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Exaprolol is a non-selective antagonist at beta-adrenoceptors exerting antiarrhythmic and local anesthetic activity. It inhibits the inotropic and chronotropic responses. Exaprolol liberates histamine from isolated mast cells and decreases the uptake of extracellular histamine. It acts on mast cells due to the direct and indirect ion exchange mechanism resulted in disproportion between histamine and granule liberation.
Status:
Investigational
Source:
INN:brobactam
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Brobactam is a synthetic inhibitor of beta-lactamases produced by both gram-positive and gram-negative bacteria. Brobactam potentiates the antibacterial activity of ampicillin against a wide range of clinically important bacterial strains which produce beta-lactamase. No resistant sub-population was observed amongst the strain s of staphylococci studied, and the development of resistance in vitro was not recorded in individual strains of Staphylococcus aureus and Escherichia coli exposed to subinhibitory concentrations of ampicillin/brobactam. Reduced sensitivity was observed in the case of one strain of M. morganii, which was known to produce an inducible chromosomal cephalosporinase.
Status:
Investigational
Source:
INN:piroxicillin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Piroxicillin is a broad-spectrum antibiotic. In vitro it is more active than piperacillin, apalcillin and mezlocillin especially against the following strains; E. coli, Ps. aeruginosa, Ps. stutzeri, K. pneumoniae, Eb. cloacae, Ser. marcescens, Proteus, Sh. flexneri, Y. enterocolitica, Cb. freundii, Acb. calcoaceticus, Bacteroides and Sc. faecalis. It shows very low MIC values against clinically important Gram-negative bacteria, primarily Pseudomonas aeruginosa. The action of piroxicillin is bactericidal.
Status:
Investigational
Source:
INN:meluadrine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Meluadrine (Hoku 81) is a beta-adrenergic receptor agonist with tocolytic activity. Meluadrine binds to and activates beta-2 adrenergic receptors of myometrial smooth muscle in the uterus, thereby activates adenyl cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP levels leads to a reduction in intracellular calcium concentration, thereby causes smooth muscle relaxation and decreases the intensity of uterine contractions. Meluadrine is a bronchodilator, and one of the metabolites of tulobuterol. Meluadrine was approximately 8 times more potent than tulobuterol, approximately twice as potent as salbutamol, and approximately as potent as isoprenaline in relaxing effect on the isolated tracheal smooth muscle preparation of guinea pigs.
Status:
Investigational
Source:
INN:adicillin
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Adicillin (Penicillin N) is a penicillin derivative produced by Cephalosporium acremonium. Adicillin is dextrorotatory. Inactivated by penicillinase as is penicillin G, but differs from the common penicillin by its antibacterial activity and hydrophilic character. Active against Sarcina lutea, Proteus vulgaris, Salmonella typhimurium, Diplococcus pneumoniae. Shows practically no activity against B. subtilis and Staph. aureus. The toxicity is somewhat less than that of penicillin G, although penicillin N is excreted more slowly.
Status:
Investigational
Source:
INN:nicainoprol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Nicainoprol, also known as RU-42924, is calcium channel antagonist and a putative class I antiarrhythmic agent. Nicainoprol was shown to be useful in the prevention and treatment of arrhythmias associated with acute myocardial infarction. Nicainoprol had been in phase II clinical trials for the treatment of arrhythmia. However, this research has been discontinued.
Status:
Investigational
Source:
INN:cefedrolor
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefedrolor is a broad-spectrum cephalexin antibiotic patented by pharmaceutical company Bristol-Myers Co.
Status:
Investigational
Source:
INN:ibuterol [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Ibuterol, a prodrug that is rapidly hydrolyzed to form a drug, terbutaline. Terbutaline, a beta-2 adrenergic agent used to treat asthma.
Status:
Investigational
Source:
INN:dioxifedrine
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Dioxifedrine is the putative metabolite of 3,4-methylenedioxymethamphetamine. It is the sympathomimetic agent and beta-2 -adrenergic agonist with bronchodilator activity. Dioxifedrine selectively binds to and activates beta-2 adrenergic receptors in bronchiolar smooth muscle, thereby causing stimulation of adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased intracellular cAMP levels cause relaxation of bronchial smooth muscle. In stimulatory studies dioxifedrine increased locomotor activity from 15 to 30 min following the drug administration. Following intracerebroventricular injection dioxifedrine rapidly reduced blood pressure and heart rate.