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

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Showing 161 - 170 of 657 results

Status:
Investigational
Source:
INN:cefsumide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefsumide is an antibiotic of the cephalosporin group patented by Fujisawa Pharmaceutical Co. Cefsumide 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.
Status:
Investigational
Source:
INN:bedoradrine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Bedoradrine (also known as KUR-1246 or MN-221), an ultra selective beta 2-adrenoceptor agonist, that participated in phase II clinical trials as an adjunct to standard therapy in the management of patients with acute exacerbation of asthma who did not respond to standard therapy. In addition, the drug was involved in trials for the treatment of preterm labor in obstetrical practice. Bedoradrine is also was studied in phase I of clinical trials for its use for treating chronic obstructive pulmonary disease, however, the efficacy for this disease was uncertain.
Status:
Investigational
Source:
INN:ridazolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Ridazolol is a cardioselective and vasodilating beta-adrenergic receptor antagonist. It also has moderate alpha-adrenolytic activity (the presence of a heterogeneous population of postjunctional alpha adrenoceptors has been suggested). Ridazolol was investigated for use in arrhythmias and ischaemic heart disorders. In patients with confirmed coronary artery disease and reproducible ST-segment depression, blood pressure and heart rate under exercise were significantly reduced for 5 hours, and improvement of ST-segment depression lasted 1 hour. Ridazolol is well tolerated. This drug is not currently used.
Status:
Investigational
Source:
INN:nafetolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Nafetolol (K5407) is a beta-blocking agent.
Status:
Investigational
Source:
INN:indopanolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Indopanolol is indole derivative patented by German pharmaceutical company Sandoz-Patent-G.m.b.H. as α- and β-adrenergic receptor blocking agent.
Status:
Investigational
Source:
JAN:RITOBEGRON ETHYL HYDROCHLORIDE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ritobegron (KUC 7483) is a selective β3-adrenoceptor agonist that was developed for oral treatment of overactive bladder. It is the prodrug of the active compound KUC-7322. Phase I studies have investigated the pharmacodynamic and pharmacokinetic effects of ritobegron in healthy individuals and patients with spinal cord injury. Ritobegron exhibits a high selectivity for the bladder versus other organs, and decreased intravesical pressure with minimal effects on the cardiovascular system in rats. When administered in combination with organic anion transporter (OAT) inhibitors such as probenecid (primarily used in treating gout and hyperuricemia), the plasma concentration of the active compound KUC-7322 may increase.
Status:
Investigational
Source:
INN:imoxiterol
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Imoxiterol (also known as RP 58802B) is benzimidazole derivatives patented by pharmaceutical company Laboratoire Roger Bellon S. A as a long-acting β-adrenergic agonist. In preclinical models, nebulized Imoxiterol produced a rapid onset and long-lasting inhibition of histamine-induced bronchospasm in the anaesthetized guinea-pig. Given orally, Imoxiterol produced a greater than three-fold shift to the right of the dose-response curve and depressed the maximum response to histamine. Imoxiterol prevented the development of bronchial hyperreactivity. Although PAF-induced bronchial hyperreactivity was not accompanied by an increase in the number of pulmonary eosinophils, Imoxiterol reduced the numbers of eosinophils recovered by lavage. Imoxiterol significantly inhibited PAF-induced microvascular leakage into guinea-pigs lung.
Status:
Investigational
Source:
INN:cefuracetime
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefuracetime is an impurity of Cefuroxime, which is an antibacterial agent.
Status:
Investigational
Source:
INN:soquinolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Soquinolol [WE 704] is a β-blocker that was under clinical development for the treatment of heart failure, but this research was discontinued. Soquinolol is a highly potent non-subtype-selective beta-adrenergic receptor blocker, which is devoid of any intrinsic sympathomimetic activity. Its local anaesthetic activity (membrane stabilizing effect) is very weak. It also shows good enteral efficacy and long duration of action. In binding studies with heart (Ki beta 1 = 3.25 nmol/l) and lung membranes (Ki beta 2 = 0.85 nmol/l) its binding profile was found to be similar to that of propranolol.
Status:
Investigational
Source:
INN:phenyracillin [INN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Phenyracillin is the 2,5-diphenylpiperazine salt of benzylpenicillin. It is antibiotic from Pencillium spp. and also other fungal spp. Shows activity against gram-positive bacteria. Phenyracillin was well tolerated.

Showing 161 - 170 of 657 results