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

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Showing 51 - 60 of 116 results

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

Class (Stereo):
CHEMICAL (RACEMIC)



Etilefrine is a cardiac stimulant used as an antihypotensive. Intravenous infusion of this compound increases cardiac output, stroke volume, venous return and blood pressure in man and experimental animals, suggesting stimulation of both α and β adrenergic receptors. However, in vitro studies indicate that etilefrine has a much higher affinity for β1 (cardiac) than for β2 adrenoreceptors. Intravenous etilefrine increases the pulse rate, cardiac output, stroke volume, central venous pressure and mean arterial pressure of healthy individuals. Marked falls in pulse rate, cardiac output, stroke volume and peripheral bloodflow, accompanied by rises in mean arterial pressure, occur when etilefrine is infused after administration of intravenous propranolol 2,5 mg. These findings indicate that etilefrine has both β1 and α1 adrenergic effects in man. The French Health Products Agency concluded that etilefrine and heptaminol have an unfavourable harm-benefit balance, and also placed restrictions on the use of midodrine.
Xamoterol (ICI 118,587) is a partial agonist of beta1-adrenoceptors. Xamoterol acts on the cardiac beta 1-adrenergic receptor, modifies the response of the heart to variations in sympathetic activity. At rest, it produces modest improvements in cardiac contractility, relaxation, and filling without increase in myocardial oxygen demand. The improvements are maintained during exercise although the attendant tachycardia is attenuated. The beneficial effects of xamoterol on both systolic and diastolic function suggested that it would be effective in patients with mild-to-moderate heart failure, and this was demonstrated in small placebo-controlled studies where effort tolerance and symptoms were improved. Xamoterol produced improvements in exercise capacity, clinical signs, symptoms and quality of life with a low incidence of adverse experiences. Xamoterol is effective as monotherapy in heart failure.
Peruvoside, main component of neriperside, a tevetoside extracted from Thevitia neriifolia Juss, cardiac glycoside, is used for the treatment of heart failure. It is Na+, K(+)-ATPase inhibitor. Peruvoside also demonstrates anti-cancer activities. Peruvoside inhibited cell growth in androgen-resistant LNCaP-abl prostate at 50 nM, lower than the concentrations required by both Digoxin and Strophanthidin (500 nM), suggesting that it may be a more potent anti-cancer candidate that other CGs. Peruvoside induced apoptotic cell death in human primitive AML KG1a cells and chronic myelogenous leukemia (CML) cell K562.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Acetyldigoxin, a cardiac glycoside that has been studied in patients with congestive heart failure.
Status:
Possibly Marketed Outside US
Source:
Corasore by Loubatieres, A.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Heptaminol is an amino alcohol that has been used as a myocardial stimulant and vasodilator and to relieve bronchospasm. Its most common therapeutic use is in orthostatic hypotension. The mechanism of heptaminol's therapeutic actions is not well understood although it has been suggested to affect catecholamine release or calcium metabolism.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Dimetofrine is a selective agonist of post-synaptic a1-adrenergic receptors. The drug was investigated as a cardiostimulant to treat orthostatic hypotension. Clinical investigation showed that dimetofrine relieves asthenia, paleness, drowsiness, fatigue, headache and other symptoms associated with hypotension. It was observed, that in acidic conditions similar to conditions in the stomach, dimetofrine is able to react with nitrites with the formation of highly mutagenic compound 2,6-dimethoxy-1,4-benzoquinone (DMBQ).
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Cymarin (or cymarine or k-strophanthidin-alpha) is a cardiac glycoside and an anti-arrhythmia and cardiotonic agent. Cymarin works as an inhibitor of Na+ /K+-ATPase . This inhibition has an inotropic effect on the cardiac muscles increasing their force by approximately 100%.
Status:
Possibly Marketed Outside US
Source:
Ethacyzin by Vikhlyaev, Yu.I.|Kaverina, N.V.|Senova, Z.P.|Ul'yanova, O.V.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ethacizine (ethacyzine) is a class Ic antiarrhythmic agent, related to moracizine. It is used in Russia and some other Commonwealth of Independent States countries for the treatment of severe and/or refractory ventricular and supraventricular arrhythmias, especially those accompanied by organic heart disease. It is also indicated as a treatment of refractory tachycardia associated with Wolff–Parkinson–White syndrome.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Gitoformate (or pentaformylgitoxin), a kidney independent glycoside, was used in patients with atrial fibrillation and in the treatment of congestive heart failure. Information, that this drug is used now is not available.