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

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Showing 2211 - 2220 of 2240 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Toliprolol is beta-adrenergic blocker. It was developed as antianginal and antihypertensive agent. Toliprolol is moderately lipophilic. It appears to have the appropriate characteristics for cerebral beta-adrenoreceptor imaging. However, tissue uptake of toliprolol was dominated by the nonspecific binding, both in the brain and in peripheral target organs, such as heart and lung. Toliprolol seems unsuitable for visualization of cerebral beta-adrenoceptors. After application of ethanol to mice, the content of glycogen of the liver and the brain decreased. By pretreatment with the beta-sympatholytic agent toliprolol, the ethanol-induced break-down of glycogen was partially blocked in the liver and completely abolished in the brain. In contrast, mainly synergistic effects of ethanol and toliprolol on the glycolysis of the liver and the brain were found. Toliprolol reduced the greater variance during the emotionally stressful situation in doses insufficient to diminish the mean increase in forearm blood flow.
Status:
Possibly Marketed Outside US
Source:
Japan:Bupranolol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Bupranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Ophthalmic Bupranolol is used for the management of glaucoma and oral Bupranolol is used for the management of cardiovascular disorders. S-Bupranolol has also being shown to have superior preclinical safety profile and great antinociceptive efficacy and should be considered as a unique b-AR compound to advance future clinical pain studies.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Bambuterol hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Bambuterol is an active precursor of the selective beta2-adrenergic agonist terbutaline. Bambuterol is the bis-N,N-dimethyl-carbamate of terbutaline. Bambuterol is a remarkably selective and potent inhibitor of cholinesterase. BAMBEC (Bambuterol hydrochloride) oral solution or tablets are indicated for the management of asthma, bronchospasm and/or reversible airways obstruction.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Acetarsol
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Acetarsone is a pentavalent arsenical compound with antiprotozoal and antihelmintic properties. It was first discovered in 1921 at Pasteur Institute by Ernest Fourneau, and sold under the brand name Stovarsol (fourneau is the French word for stove). Before stovarsol was used in the treatment of congenital syphilis, it had already been used in other diseases : amoebiasis, acquired syphilis, yaws, trypanosomiasis and malaria, and a formidable list of toxic manifestations can be compiled from the literature. Bender (I927) recorded six cases of poisoning with malaise, fever, cedema, jaundice, diarrhoea, albuminuria, bronchitis, coryza and skin troubles, such as diffuse erythema, dryness and pruritus. Of 232 cases of amoebiasis treated by Brown (I935) without a death, thirteen (5.6%) had toxic erythemata, some of them so severe as to amount to exfoliative dermatitis. Although its mechanism of action is not fully known, acetarsone may bind to protein-containing sulfhydryl groups located in the parasite, thereby forming lethal As-S bonds. This may prevent their functioning and eventually kill the parasite.
Status:
Possibly Marketed Outside US
Source:
Japan:Efonidipine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Efonidipine is a 1,4-dihydropyridine derivative for the treatment of hypertension and angina. Efonidipine exerts its antihypertensive and antianginal effects through blocking L- and T-type calcium channels.
Status:
Possibly Marketed Outside US
Source:
Xylamidine tosylate by Wellcome Research
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Xylamidine is a peripherally-restricted antagonist of 5HT2A and 5HT1A receptor. It is used to study the role of the serotonin receptors in the regulation of food intake, cardiovascular function, and regulation of body temperature.
Etoperidone is an atypical antidepressant introduced in Europe in 1977. The activity of etoperidone is made mainly by its major metabolite 1-(3'-chlorophenyl)piperazine (mCPP). mCPP binds with different affinity to most of the serotonergic receptors and adrenergic receptors. This metabolite is an agonist of 5-HT2c and an antagonist of 5-HT2a. Part of etoperidone structure contributes to the activity in the α-adrenergic receptors. Etoperidone has been studied for the treatment of depression, tremors in Parkinson, extrapyramidal symptoms and male impotence. It is not certain if it was ever approved and marketed but its current status is withdrawn.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Propamidine isetionate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Propamidine, an aromatic diamidine compound, is widely used as an antimicrobial agent. Propamidine isethionate, the salt of propamidine with isethionic acid, is used in the treatment of Acanthamoeba infection. Diseases caused by Acanthamoeba include keratitis and granulomatous amoebic encephalitis.
Status:
Possibly Marketed Outside US
Source:
Japan:Barnidipine Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Bamidipine is an antihypertensive drug belonging to the dihydropyridine (DHP) group of calcium antagonists. The product was originally developed by Yamanouchi Pharmaceutical (Tokyo, Japan) and is currently marketed in Japan under the trade name of Hypoca (Astellas Pharma Inc, Tokyo, Japan). It is available in a modified-release formulation which has a gradual onset of action and is effective in a single daily oral dose of 10 to 20 mg. Bamidipine has selective action against cardiovascular calcium antagonist receptors and its antihypertensive action is related to the reduction of peripheral vascular resistance secondary to its vasodilatory action. The clinical antihypertensive efficacy of barnidipine is similar to that of other DHP calcium antagonists such as nitrendipine and amlodipine, and antihypertensives belonging to other drug classes such as atenolol and enalapril. Barnidipine has been found to be as efficacious and well tolerated as hydrochlorothiazide in the management of hypertension in elderly patients. Barnidipine is generally well tolerated. As with other DHP calcium antagonists, vasodilator adverse events such as headache, flushing and peripheral oedema account for most of the adverse events reported with its use and are usually transient. Oedema is less frequent than with amlodipine and nitrendipine. Its use is not associated with reflex tachycardia.
Status:
Possibly Marketed Outside US
Source:
WHO-ESSENTIAL MEDICINES LIST:6.5.5.1
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Suramin is an antiprotozoal and anthelmintic compound. It is indicated for the treatment of African trypanosomiasis (African sleeping sickness; trypanosome fever) and Onchocerciasis (river blindness). Additionally, suramin exhibits antineoplastic action. It was discovered that suramin produced dramatic, but transient, improvement of core symptoms of autism spectrum disorder.

Showing 2211 - 2220 of 2240 results