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

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Showing 181 - 190 of 366 results

Status:
Possibly Marketed Outside US
Source:
Pirroksan by All-Union Scientific-Research Chemical-Pharmaceutical Institute
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Proroxan is a non-selective а-adrenoblocker. Proroxan was found to prevent the development of hypertensive crises and improve cerebral bioelectrical parameters in most of hypertensive patients. Proroxan has been used as an antihypertensive and in the treatment of Ménière’s disease, motion sickness, and allergic dermatitis.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Guanazodine is a new antihypertensive drug. Guanazodine caused a sustained decrease in the systemic blood pressure of spontaneously hypertensive rats, renal hypertensive dogs and normal cats. No tachyphylaxis developed when the drug was administered orally. The heart rate decreased. Guanazodine relaxed the cat nictitating membrane, attenuated the positive chronotropic response to sympathetic nerve stimulation in anesthetized dogs and in isolated rabbit aorta to transmural electrical stimulation. Guanazodine potentiated the pressor response to noradrenaline but attenuated the response to tyramine in anesthetized cats. It may be concluded that the hypotensive effect of guanazodine is related to adrenergic neuron blocking action, the noradrenaline-depleting action in peripheral tissues is similar to the effect of guanethidine and bethanidine. However, this drug is less potent than guanethidine. Toxicity and side effects appear to be less with guanazodine than with guanethidine and bethanidine.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Alinidine, a specific bradycardiac agent, which reduces myocardial oxygen consumption and improves exercise tolerance in patients with angina pectoris. In randomized controlled trial alinidine did not enhance myocardial salvage or preservation of left ventricular function of major arrhythmias in the early phase of infarction. The development of this drug was stopped because it was not sufficiently specific for its target.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Aganodine, an imidazoline/ alpha-2 receptor agonist, can lower intraocular pressure in the sympathetic neurons of the eye and possibly in the central nervous system.
Status:
Possibly Marketed Outside US
Source:
NCT01363648: Phase 4 Interventional Completed Cognitive Impairment
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Choline alfoscerate (alpha-Glycerylphosphorylcholine or Alpha-GPC) is a nootropic choline-containing phospholipid. Choline alphoscerate increases the release of acetylcholine in rat hippocampus, facilitates learning and memory in experimental animals, improves brain transduction mechanisms and decreases age-dependent structural changes occurring in rat brain areas involved in learning and memory. The compound exerts neuroprotective effects in models of altered cholinergic neurotransmission and of brain vascular injury. In clinical studies choline alphoscerate improved memory and attention impairment, as well as affective and somatic symptoms in dementia disorders. In Europe alpha-GPC is a prescription medication for the treatment of Alzheimer's disease. It is available in two forms; one is taken by mouth, and the other is given as a shot. In the United States alpha-GPC is only available as a dietary supplement, mostly in products promoted to improve memory. Other uses for alpha-GPC include treatment of various kinds of dementia, stroke, and "mini-stroke" (transient ischemic attack, TIA). Alpha-GPC is also used for improving memory, thinking skills, and learning.
Status:
Possibly Marketed Outside US
Source:
NCT01418118: Phase 4 Interventional Completed Oral Cancer
(2008)
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
Source:
Lofexidine by Nattermann & Cie
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Levlofexidine is R-enantiomer of a α2A adrenergic receptor agonist Lofexidine. Levlofexidine (as a component of Lofexidine) can be used as a short-acting anti-hypertensive but is mostly used to help relieve symptoms of heroin or opiate withdrawal in opiate dependency. Lofexidine is approved in the United Kingdom but is still undergoing clinical trials in the United States. Levlofexidine showed an approximately 9-fold higher affinity than Dexlofexidine for the alpha 2-adrenoceptor-like binding sites in rat brain membranes identified by [3H]-clonidine and was 4 times more potent at displacing [3H]-prazosin from alpha 1-adrenoceptors. The possibility of using lofexidine to treat alcohol addiction withdrawal symptoms has been investigated and has not yet been shown to be an effective treatment.
Status:
Possibly Marketed Outside US
Source:
Farial by Nordmark-Werke [W. Germany]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Indanazoline, an imidazoline derivative, (E-VA-16, as monohydrochloride active substance of Farial) is a nasal decongestant. As a nasal spray it can be used for the treatment of acute, chronic and allergic rhinitis. It is characterized by a pronounced vasoconstrictive action after local or intravenous application. This is due to a direct action of the compound on alpha-adrenergic receptors. When applied systemically Indanazoline being a peripherally acting alpha-sympathomimetic induces a rise in blood pressure and a reduction of heart rate and exerts antiphlogistic, spasmolytic, hyperglycemic and diuretic actions. When given by the intranasal route the substance influences blood pressure and heart rate only at concentrations considerably higher than those intended for use in therapy. After enteral administration the effective doses also markedly exceed the single therapeutic doses. There was no evidence of side-effects restricting the use of the drug as compared to other imidazoline derivatives.
Levopropylhexedrine acts similar to amphetamine, at therapeutic doses has anorexigenic effect.
Status:
Possibly Marketed Outside US
Source:
Pressionorm by Helopharm [W. Germany]
Source URL:

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.

Showing 181 - 190 of 366 results