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

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Showing 331 - 340 of 657 results

Status:
Possibly Marketed Outside US
Source:
Japan:Bupranolol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Bupranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Ophthalmic Bupranolol is used for the management of glaucoma and oral Bupranolol is used for the management of cardiovascular disorders. S-Bupranolol has also being shown to have superior preclinical safety profile and great antinociceptive efficacy and should be considered as a unique b-AR compound to advance future clinical pain studies.
Status:
Possibly Marketed Outside US
Source:
Canada:FENOTEROL HYDROBROMIDE
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Fenoterol is a beta2-adrenoreceptor agonist, used as a bronchodilator for the treatment and prevention of bronchospasms, associated with asthma and chronic obstructive airway disease, including bronchitis and pulmonary emphysema. Fenoterol is also used for tocolysis during premature labor. Marketing of fenoterol for treatment of asthma was suspended in Australia and New Zealand because of an increased risk of deaths, most likely due to excessive self-administration of the drug.
Status:
Possibly Marketed Outside US
Source:
Japan:Tilisolol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Tilisolol (, 4-[3-(tert-butylamino)- 2-hydroxyproxy]-N-methylisoeabostyril hydrochloride/N-696 ) is a non-selective beta-adrenergic blocking agent, and has a long-lasting and stable action in the clinical treatment of hypertension and angina pectoris. This antihypertensive effect of tilisolol might be largely attributable to its potent beta-adrenergic antagonistic effects. The measurement of the I-V relationship with or without tilisolol excluded the activation of ATP-sensitive K+ current (at least in cardiac muscle) under physiological conditions. However, several investigators suggested that tilisolol has a direct action on smooth muscle cells through ATP-sensitive K+ channels. The possibility that tilisolol has additional effects on the membrane ionic channels of cardiac myocytes under ischemic conditions remains to be tested. It was synthesized by Nisshin Hour Milling Co., Ltd. (Tokyo, Japan)
Status:
Possibly Marketed Outside US
Source:
Japan:Lenapenem Hydrochloride Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Lenapenem is an anti-bacterial agent that was tested in late 90's in phase II clinical trials against bacterial infections. Lenapenem was shown to be active against both Gram-positive and Gram-negative bacteria and exerted its therapeutic effect by inhibiting penicillin binding proteins. The development of the drug was terminated due to the safety reason.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefluprenam
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)



Cefluprenam is an anti-bacterial agent of broad spectrum. It was active in vitro against different bacteria strains with MIC values from 0.78 ug/ml to 3.13 ug/ml. The drug exerts its bactericidal activity through inhibition of penicillin-binding proteins, showing high affinity to all four subtypes. Cefluprenam was tested for the treatment of respiratory tract infections in phase III study, however the drug development was stopped.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefcapene Pivoxil Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefcapene is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcapene binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
Etafenone is an antiarrhythmic and coronary vasodilator drug. Etafenone exerts negative inotropic action on myocardium. It is able to block calcium channels. As a coronary vasodilator which produces a decrease in the heart rate and myocardial oxygen consumption, etafenone has been used in the therapy of ischemic heart disease.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Ancarolol is a beta-adrenoceptor antagonist which can be used therapeutically as an antihypertensive.
Status:
Possibly Marketed Outside US
Source:
Japan:Ceftezole Sodium
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ceftezole sodium is a cephalosporin antibiotic. Ceftezole was found to be a broad-spectrum antibiotic, active in vitro against many species of gram-positive and gram-negative bacteria except Pseudomonas aeruginosa, Serratia marcescens and Proteus vulgaris. Ceftezole sodium is used as an injectable or through an intravenous mode of delivery. The bactericidal activity of ceftezole results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). The PBPs are transpeptidases which are vital in peptidoglycan biosynthesis. Therefore, their inhibition prevents this vital cell wall component from being properly synthesized. Ceftezole has been shown to exhibit potent alpha-glucosidase inhibitory activity. In in vitro alpha-glucosidase assays, ceftezole was shown to be a reversible, non-competitive inhibitor of yeast alpha-glucosidase with a Ki value of 5.78 x 10(-7) M when the enzyme mixture was pretreated with ceftezole. Ceftezole is used for the treatment of susceptible bacterial infections including septicemia, respiratory, biliary or GU tract, skin and skin structure, endocarditis. Surgical prophylaxis.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Carazolol is a beta1/beta2 adrenoreceptor blocking agent. Activity and safety of the drug were evaluated in clinical trials that were conducted in healthy subjects and in patients suffering from either chronic bronchitis or asthma. The drug, however, was not developed for human use. Instead, carazolol is used in to reduce stress in animals during transportation. In veterinary medicine, carazolol is given by intramuscular injection to pigs is indicated in stress-inducing situations. In cattle, carazolol is intended to be used for the prevention of shipment stress caused by transportation and formation of new herds.

Showing 331 - 340 of 657 results