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

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Showing 161 - 170 of 567 results

Squalene is a naturally occurring polyprenyl compound primarily known for its key role as an intermediate in cholesterol synthesis. It received its name because of its occurrence in shark liver oil (Squalus spp.), which contains large quantities and is considered the richest source of squalene. However, it is widely distributed in nature, with reasonable amounts found in olive oil, palm oil, wheat-germ oil, amaranth oil, and rice bran oil. The primary therapeutic use of squalene currently is as an adjunctive therapy in a variety of cancers. Although epidemiological, experimental and animal evidence suggests anti-cancer properties, to date no human trials have been conducted to verify the role this nutrient might have in cancer therapy regimens.
Status:
Possibly Marketed Outside US
Source:
Japan:Diisopropylamine Dichloroacetate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Diisopropylamine (DIPA) is a secondary amine, which is used as a chemical intermediate, and catalyst for the synthesis of pesticides and pharmaceuticals. DIPA is primarily used as a precursor for the herbicides dilate and triallate, as well as certain sulfenamides used in the vulcanization of rubber. It is used for adjusting pH in cosmetic formulations, in colognes, and toilet cleaners. It is associated with tobacco either as a natural component of tobacco, pyrolysis product (in tobacco smoke), or additive for one or more types of tobacco products. When given intravenously to hypertensive patients, DIPA is known as an antihypertensive agent. DIPA exerts its action by lowering arterial blood pressure, reduction of stroke volume and cardiac output. DIPA reduced blood glucose concentrations in fasted mice and in fasted, glucose-loaded, or streptozotocin-diabetic rats. DADA (diisopropylamine dichloroacetate) was identified as an active domain of pangamic acid. DADA is a vasodilator of peripheral and cerebral arterioles. DADA also considered to aid in the detoxification of chemical and metallic metabolites, possibly by the formation of chelate-like compounds whose excretion by the kidneys is facilitated and increased. DADA increases oxygen utilization and cortical glucose uptake.
Alprenolol is a beta adrenoreceptor blocking agent and 5HT1A antagonist, developed by AstraZeneca and now available as generic drug. It is used for treatment of hypertension, angina pectoris due to coronary atherosclerosis and acute myocardial infarction.
Status:
Possibly Marketed Outside US
Source:
Japan:Alilusem Potassium
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Alilusem (M17055) is under development as a novel loop diuretic for oral administration. M17055 has a potent diuretic effect and can be categorized as a loop diuretic that inhibits both the cotransport of Na+, K+, and 2Cl- at the thick ascending Henle’s loop and the reabsorption of Na+ at the distal tubule cells in the kidney. Structure of M17055 is different from those of other loop diuretics; M17055, which has a sulfate group in its structure is soluble and well absorbed, and its bioavailability in humans is 42-60% (unpublished observation). Considering that the pKa of M17055 is 2.39, almost of M17055 would be in ionized form at physiological pH in the small intestine. In humans, the major elimination route of M17055 is renal excretion, 59-72% of the dose being recovered in unchanged form in urine; the remainder is thought to be metabolized by both CYP3A4 and CYP2C9.
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:
Japan:Clofenamide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Clofenamide is a benzenedisulfonamide-based agent and carbonic anhydrase (CA) inhibitor with diuretic activity. Clofenamide inhibits CA, thereby preventing sodium, bicarbonate and thus water reabsorption in the proximal convoluted tubule resulting in diuresis.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Clopamide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Clopamide is a thiazide diuretic which helps in removing fluid from the body. Clopamide is used in treatment of hypertension and edema.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Zidapamide (1-methyl-2-(3'-sulphenyl-4'-chlorobenzamido)-isoindoline) is an isoindoline derivative exerting diuretic, salutaric and hypotensive activity.
Status:
Possibly Marketed Outside US
Source:
Japan:Cadralazine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Cadralazine is an antihypertensive of the hydrazinophthalazine chemical class. In hypertensive patients the optimal effect, based on the antihypertensive efficacy to tolerability ratio, is seen after a 15 mg dose when the drug is administered as monotherapy. When administered in combination with other antihypertensive agents, a 10 mg daily dosage seems appropriate. Noncomparative trials have shown that, in patients who had failed to respond adequately to a beta-blocker and/or diuretic, the addition of cadralazine 10 to 30 mg once daily reduced systolic/diastolic blood pressure by 11 to 19%/13 to 22%. This antihypertensive effect becomes evident over a 2- to 6-week period of therapy and persists during longer term administration. Comparative studies have shown that cadralazine is superior to placebo, and has a similar blood pressure lowering effect to hydralazine, dihydralazine and prazosin in patients not controlled by beta-blocker and/or diuretic but who continued to receive these treatments. Similarly, cadralazine and chlorthalidone were equally effective in reducing blood pressure in resting hypertensive patients but cadralazine shows an advantage in reducing the pressor response in exercising patients. Cadralazine is well tolerated when administered with a beta-blocker or diuretic. Most adverse effects become less frequent and severe with continued use, occur more frequently at dosages of 20 mg/day or more, and do not generally require withdrawal of therapy. Manifestations of the drug's vasodilating properties such as headache, asthenia, dizziness, palpitations and flushing are the most commonly reported symptoms during cadralazine monotherapy, but these may be reduced during combination therapy. The drug does not appear to induce a systemic lupus-like erythematosus syndrome, as may occur with hydralazine, but additional clinical experience is required to completely exclude this possibility. The therapeutic potential of cadralazine cannot be clearly established until the present limited clinical base is expanded to include comparisons with other classes of vasodilating drugs (ACE inhibitors and calcium antagonists), and its utility in the management of other indications such as severe hypertension during pregnancy has been adequately explored.
Status:
Possibly Marketed Outside US
Source:
Japan:Piretanide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Piretanide (INN, trade names Arelix, Eurelix, Tauliz) has been synthesized in 1973 at Hoechst AG (Germany) as a loop diuretic[2] compound by using a then-new method for introducing cyclic amine residues in an aromatic nucleus in the presence of other aromatically bonded functional groups. Studies of piretanide in rats and dogs in comparison with other high-ceiling diuretics such as furosemide and bumetanide found a more suitable dose/response rate (regression line) and a more favourable sodium/potassium excretion ratio. These findings led eventually to clinical studies in man and finally to the introduction as a saluretic and antihypertensive medication in Germany, France, Italy and other countries.

Showing 161 - 170 of 567 results