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

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Showing 71 - 80 of 116 results

Meldonium (3-(2,2,2-trimethylhydrazinium)propionate; MET-88; quaterine, trade-named as Mildronate) is an antiischemic drug developed at the Latvian Institute of Organic Synthesis. It is a clinically used in the treatment of heart failure, myocardial infarction, arrhythmia, atherosclerosis, and diabetes. Mechanism of action is based on the regulation of energy metabolism pathways through l-carnitine lowering effect. L-Carnitine biosynthesis enzyme γ-butyrobetaine hydroxylase and carnitine/organic cation transporter type 2 (OCTN2) are the main known drug targets of meldonium, and through inhibition of these activities, meldonium induces adaptive changes in the cellular energy homeostasis. Since L-carnitine is involved in the metabolism of fatty acids, the decline in its levels stimulates glucose metabolism and decreases concentrations of l-carnitine related metabolites, such as long-chain acylcarnitines and trimethylamine-N-oxide. Meldonium is used in neurological clinics for the treatment of brain circulation disorders. It appears to improve patients' mood; they become more active, their motor dysfunction decreases, and asthenia, dizziness, and nausea become less pronounced. CNS effects of Meldonium could be mediated by stimulation of the nitric oxide production in the vascular endothelium by modification of the gamma-butyrobetaine and its esters pools. It is hypothesized that mildronate may increase the formation of the gamma-butyrobetaine esters. Meldonium was on the World Anti-Doping Agency’s (WADA) list of drugs being monitored until September 2015, when it was added to the list of banned substances, effective January 1, 2016.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Cloridarol is a vasodilator that was studied for the treatment of coronary insufficiency in Italy in the 1970s. In normolipidemic rats, cloridarol decreased plasma triglycerides without affecting cholesterolemia and fast- or norepinephrine-induced lipolysis. The drug proved effective in reducing fructose-induced hypertriglyceridemia and dietary hypercholesterolemia in rats.
Status:
Possibly Marketed Outside US
Source:
Japan:Carbocromen Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Chromonar is a coronary vasodilator agent, it dilates coronary vessels and increases coronary blood flow volume rate, contributes to the development of collateral circulation (with prolonged use), improves metabolic processes in myocardium. The mechanism of action of a role played by its inhibitory effect on phosphodiesterase, accompanied by accumulation in the cells of cyclic 3 ', 5'-adenosine monophosphate. Due to the relatively low therapeutic efficacy Chromonar use is limited, mainly in the early stages of coronary heart disease with angina pectoris in the absence of long-standing and long strokes, when there is no expressed stenotic process.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Dopexamine hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dopexamine hydrochloride is a synthetic catecholamine, structurally related to dopamine, with marked intrinsic agonist activity at beta 2-adrenoceptors, lesser agonist activity at dopamine DA1- and DA2-receptors and beta 1-adrenoceptors, and an inhibitory action on the neuronal catecholamine uptake mechanism. The drug is administered by intravenous infusion, and is characterized by a rapid onset and short duration of action. Dopexamine is being tested as a treatment for heart failure and sepsis.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Cinepazet is an ethyl ester of cinepazic acid. It acts by inhibiting the influx of extracellular calcium into cells through the slow calcium channel in the cell membrane. In the 1970s cinepazet was marketed in France and Italy under tradename Vascoril for the treatment of angina.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

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.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Propatylnitrate (or propatyl nitrate), a coronary vasodilator that has been studied for the relief of acute attacks of angina pectoris. However, was revealed that this drug didn’t abolish or diminish the frequency of attacks of angina pectoris.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)


Gepefrine (Pressionorm and Wintonin) is an antihypotensive agent. It was used for therapy of orthostatic dysregulation. One hour after oral administration of 30 mg or 45 mg gepefrine the blood pressure increased significantly at rest and more markedly on standing and during the step test. Gepefrine led to a reduction in pathological orthostatic regulation during the early phase as well as to the prevention of subjective and objective signs of orthostatic adjustment disorder during the late phase. Patients with insufficient rise in blood pressure during the step test (80 watts) showed after gepefrine a distinct tendency towards normalisation and the regression of subjective states of exhaustion. Gepefrine caused on average no substantive alternations in heart rate during all phases of the investigation. Complications or side-effects due to the method or the medicament were not observed.
Status:
Possibly Marketed Outside US
Source:
Japan:Norfenefrine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Norfenefrine or meta-octopamine, also known as 3,β-dihydroxyphenethylamine, is an adrenergic agent used as a sympathomimetic drug which is marketed in Europe, Japan, and Mexico. Along with its structural isomer p-octopamine and the tyramines, norfenefrine is a naturally occurring, endogenous trace amine and plays a role as a minor neurotransmitter in the brain. Norfenefrine controls blood pressure in acute hypotensive states eg pheochromocytomectomy, sympathectomy, poliomyelitis, spinal anesth, MI, septicemia, blood transfusion and drug reactions. Adjunct in treatment of cardiac arrest and hypotension.