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

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Showing 49671 - 49680 of 55039 results

Status:
Investigational
Source:
INN:avitriptan
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Avitriptan (BMS-180048), a new 5-HT 1B/1D receptor agonist, has been studied in phase II clinical trials in patients with migraine headaches. Later experiments have confirmed antimigraine activity together with coronary side-effect potential that is why further studies were discontinued.
Status:
Investigational
Source:
INN:sibrafiban
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sibrafiban (G-7453) is the orally administered, nonpeptide, double-prodrug of Ro 44-3888 which is a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban is a double prodrug that undergoes bioconversion to the inactive prodrug Ro 48-3656 and to the active IIb/IIIa antagonist, Ro 44-3888, after oral administration. Sibrafiban was undergoing clinical trials for secondary prevention of cardiac events in patients stabilised after acute coronary syndromes. Sibrafiban has been shown to have comparable efficacy to aspirin in preventing recurrent ischemic events in patients suffering from acute coronary syndromes. Sibrafiban was under development by Genentech and Hoffmann-La Roche, and in phase III trials as an antithrombotic. The development of sibrafiban was discontinued in 1999 following unfavorable Phase III efficacy data.
Status:
Investigational
Source:
INN:oxadimedine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Oxadimedine, an antihistamine that was developed as a local anesthetic. Information about the current use of this compound is not available.
Status:
Investigational
Source:
INN:trebenzomine [INN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Trebenzomine (CI-686) is a centrally acting psychotropic drug structurally distinct from currently available drugs. Preclinical studies indicate that trebenzomine, unlike most psychotropic drugs, has both neuroleptic and stimulant profiles. Stimulant properties of trebenzomine include potentiation of methamphetamine-induced self-stimulation. Neuroleptic properties of trebenzomine include reduction of septal hyperirritability, suppression of conditioned avoidance behavior, blockade of apomorphine-induced emesis in dogs, and elevation of brain homovanillic acid (HVA). Trebenzomine's effect on dopamine (DA) metabolism appears to be related more to the presynaptic release of DA rather than by blockade of postsynaptic DA receptors. Unique preclinical profile suggests a mechanism of action other than dopamine antagonism which could have implications regarding current thinking on the pathophysiology of schizophrenia.
Status:
Investigational
Source:
INN:triclofenol piperazine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

2,4,5-Trichlorophenol is a grey flake or needle-shaped solid. It is used as an intermediate in the manufacture of the herbicide 2,4,5-Trichlorophenoxyacetic Acid (2,4,5-T) and as a fungicide and bactericide. 2,4,5-trichlorophenol (triclofenol piperazine, Ranestol) is an antifungal agent, which was also used against light hookworm infections. Thirty persons who were positive for hookworm eggs in their stools were treated with 50 mg/kg of triclofenol piperazine dissolved in 5 per cent polyethylene glycol Ranestol® in soft gelatin capsules. Nineteen of these showed 77 to 100 % reduction in egg count average when compared with the pre-treatment counts. Side reactions were limited to mild and transient nausea in 23, vomiting in 7, transient abdominal cramps and headache in 2 each. 2,4,5-trichlorophenol complexed with dicyclohexylamine was used for treatment of experimental mycosis. From the mycological and clinical evaluation the conclusion can be drawn that the effect of phenol in lipophilic ointment is comparable to that of clotrimazole.
Status:
Investigational
Source:
INN:cesium (¹³¹Cs) chloride [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Cesium Cation CS-131 is an unstable radioisotope of cesium (Cs) with radiocytotoxic application. Cs-131 is a gamma photon-emitting radionuclide with high energy and a relatively short half-life of 9.7 days. Intraoperative cesium-131 (Cs-131) brachytherapy performed at the time of neurosurgical resection may represent an excellent salvage treatment option.
Status:
Investigational
Source:
INN:pirogliride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pirogliride is the antidiabetic agent. It has been found to produce a hypoglycemic effect in nondiabetic rats, dogs, mice, and monkeys. To being three to four times more potent than tolbutamide, pirogliride also differs from the sulfonylureas in lowering blood glucose concentrations of streptozotocin-diabetic rats and db/db mice, and, moreover, oral administration to normal fasted dogs did not produce the characteristic rise in insulin concentrations observed with tolbutamide. Pirogliride potentiates glucose-induced insulin secretion from isolated islets. This effect is accompanied by a facilitated glucose metabolism. Pirogliride partially prevents the known inhibitory effects of mannoheptulose on glucose-induced secretion and utilization. Pirogliride was found to produce a concentration-dependent inhibition of gluconeogenesis in rat kidney cortex slices. hepatocytes and perfused liver. Pirogliride was metabolized in man to a small extent by oxidation of the 4-position of the phenyl ring.
Status:
Investigational
Source:
INN:buthalital sodium
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Buthalital is a barbiturate derivative which was under development as a short-acting anesthetic. However, development was discontinued, perhaps due to its extremely rapid elimination rate] and buthalital sodium was never marketed.
Status:
Investigational
Source:
INN:tipentosin
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Tipentosin is prazosin derivative. It is an angiotensin-converting enzyme inhibitor. Tipentosin was developed as an antihypertensive agent.
Status:
Investigational
Source:
INN:demelverine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Demelverine is an antispasmodic agent and bronchodilator.

Showing 49671 - 49680 of 55039 results