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

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Showing 2111 - 2120 of 2273 results

Status:
Investigational
Source:
INN:tiapamil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tiapamil (also known as Ro 11-1781) is a dithiane derivative patented by Hoffmann-La Roche, F., und Co., A.-G. as calcium-channel antagonist useful for myocardial infarction treatment. Tiapamil, like verapamil, inhibited in a concentration-dependent manner Ca2+-induced contractions in isolated, K+-depolarized preparations of rat renal artery, dog coronary artery and rabbit main pulmonary artery. The inhibitory effects of Tiapamil can be overcome by raising the Ca2+ concentration of the bath fluid. In the rabbit main pulmonary artery, Tiapamil reduces 45Ca influx into the K+-depolarized vascular smooth muscle cells. Tiapamil inhibits the slow potentials in partially depolarized guinea-pig papillary muscles. Tiapamil decreases contractile force in isolated guinea-pig atria and papillary muscles, as well as in isolated cat hearts. Tiapamil also reduces heart rate and increases coronary flow in these preparations. Tiapamil doubled coronary artery blood flow in the coronary sinus blood without producing major changes in blood pressure and heart rate in anesthetized dogs. Tiapamil did not affect contractions of isolated guinea-pig ileum, rat stomach strips or rat vas deferens in response to various stimulants. Tiapamil have no major effects on renal water and electrolyte excretion, on autonomic nerves and receptors, on pain perception and on the central nervous system. Acute, subacute, and chronic toxicity studies demonstrate low toxicity for Tiapamil with no tendency for accumulation. In clinical trials, Tiapamil effectively lowers systolic and diastolic blood pressure, but have no effects on heart rate
Status:
Investigational
Source:
INN:fluprostenol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
INN:etoxazene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ethoxazene (2,4-diamino-4-ethoxyazobenzene) is an analgesic compound. It may be used as an indicator of acidity in an examination of gastric function.
Status:
Investigational
Source:
INN:cloperidone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Cloperidone is a quinazolinedione derivative with sedative and antihypertensive properties. Cloperidone was discovered in 1965 by Miles Laboratories. The activity of the compound was demonstrated by behavioral observations in dogs and cats, by rotarod and activity cage experiments in mice and in other models.
Status:
Investigational
Source:
INN:diacetolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Diacetolol is the major metabolite of the β-adrenoceptor blocking agent, acebutolol. In vitro, the β-adrenoceptor blocking potency of diacetolol was less than that of acebutolol but its cardioselectivity (atrial relative to tracheal tissue) was greater. Diacetolol had weak intrinsic sympathomimetic activity, and no significant membrane-stabilizing activity. It did not restore sinus rhythm to anaesthetized dogs with ouabain-induced arrhythmias but was similar to acebutolol in preventing arrhythmia induced by adrenaline/methylchloroform in anaesthetized cats. Study of diacetolol pharmacokinetics and bioavailability suggests either a first-pass effect or incomplete absorption of diacetolol after oral administration. Diacetolol plasma half-life after oral administration is about 12 h and is not dose-dependent. Diacetolol possesses significant antihypertensive action against moderate essential hypertension in man. Its antihypertensive effect is associated with a reduction in the heart rate and a decrease in plasma renin activity.
Status:
Investigational
Source:
INN:phenarsone sulfoxylate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Phenarsone sulfoxylate (Aldarsone), a pentavalent arsenical, is a condensation product of 3-amino-4 hydroxylphenylarsonic acid with sodium formaldehyde sulfoxylate. It is an antiamoebic agent. Aldarsone has a spirochetal power superior to that of tryparsamide. Aldarsone may be used in conjunction with artificial fever therapy and penicillin therapy to improve the results in symptomatic syphilis of the central nervous system (neurosyphilis).

Showing 2111 - 2120 of 2273 results