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

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Showing 51 - 60 of 124 results

Status:
Possibly Marketed Outside US
Source:
Japan:Dilazep Dihydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dilazep is a coronary and cerebral vasodilator as an adenosine reuptake inhibitor. Dilazep is an inhibitor of platelet aggregation and of membrane transport of nucleosides. Dilazep is also known to have a vasodilating effect on renal vessels and is often used in patients with ischaemic heart disease, cerebral ischemia or renal dysfunction to improve tissue circulation.
Status:
Possibly Marketed Outside US
Source:
Theodrenaline by ZYF Pharm Chemical
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

THEODRENALINE, a theophylline derivative, is a cardiac stimulant. A 20:1 mixture of cafedrine and THEODRENALINE (AKRINOR®) is widely used in Germany for the treatment of hypotensive states during anesthesia and in emergency medicine.
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

Class (Stereo):
CHEMICAL (ACHIRAL)

Tiazotic acid is an antioxidant. As tiazotic acid morpholinium salt it is marketed under the brand names Thiotriazoline, Tiokor among others in Russia, Ukraine, Uzbekistan as the treatment of ischemic heart diseases. It is proposed to be a hepatoprotective, wound-healing and antiviral agent. A comparative international multicenter randomized trial, assessed anti-anginal anti ischemic efficacy and safety of Trimetazidine (60 mg/d) and Thiotriazoline (600 mg/d) in symptomatic patients with chronic ischemic heart disease receiving the first line therapy. The study assessed the efficacy of the two drugs on total exercise duration, time to 1-mm ST segment depression, the number of angina attacks and nitroglycerin tablets consumed amount. Both drugs have demonstrated clinical efficacy equal for all primary and secondary endpoints. Thiotriazoline was also used for the he correction of hepatotoxicity during combined chemoradiotherapy for cancer patients.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Beta-acetyldigoxin (under the brand name Novodigal), a beta-acetyl derivative of digoxin, acts as a prodrug. It is deacetylated in the cells of the intestinal mucosa and is present inside the body solely in the form of digoxin. β-acetyldigoxin has a higher bioavailability than digoxin. Beta-acetyldigoxin is a substrate of P-glycoprotein.
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.