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

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Showing 12601 - 12610 of 12951 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Diisopromine, a spasmolytic and a choleretic, in combination with sorbitol was marketed under the brand name Agofell. Agofell is prescribed for the biliary stasis and biliary insufficiency, hypotonia of the gall bladder, spasm of the biliary duct and of the sphincter of Oddi, cholecystitis, cholelithiasis, post cholecystotomy syndrome.
Dilevalol, the RR-stereoisomer of labetalol, is a non-cardioselective β-adrenoceptor antagonist with substantial partial β2-agonist and negligible α1-blocking activity. Reduction in blood pressure during dilevalol administration is associated with peripheral vasodilatation, and heart rate remains essentially unchanged. Following oral administration, dilevalol is completely absorbed. Once-daily administration is possible, due to a long elimination half-life. In vitro and in vivo animal studies and results obtained in humans reveal that dilevalol is a nonselective blocker of β1- and β2-adrenoceptors, with a similar potency to propranolol, but has negligible antagonistic activity at α1-receptors. Dilevalol, the R,R′ stereoisomer, makes up 25% of racemic labetalol, the drug, approved by FDA for the treatment of hypertension. The relaxing potency of dilevalol was approximately 4.7 times more potent than that of labetalol. Dilevalol markedly reduced the diastolic blood pressure with only a slight increase of heart rate In pithed rats, while isoproterenol and pindolol caused moderate to marked positive chronotropic effects in proportion to their hypotensive effects. These results suggest that dilevalol has more potent ISA than labetalol. In contrast to labetalol, dilevalol possesses little, if any, alpha-adrenergic blocking activity. The compound is 3 to 10 times less potent than labetalol at α1-adrenergic receptors under a variety of experimental conditions. Moreover, it is 300- to 1000-fold less potent at alpha1-adrenergic receptors compared with β1-adrenergic receptors. The pA2 values for dilevalol as an α antagonist range from 5.9 to 6.4. Because maximal plasma concentrations of the drug after administration of a 400-mg dose are approximately 0.5 pmol, it is doubtful that alpha blockade is involved in the antihypertensive response to dilevalol in humans.
Status:
Possibly Marketed Outside US
Source:
NCT00531947: Phase 4 Interventional Completed Major Depressive Disorder
(2007)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Butalamine hydrochloride under the brand name Adrevil forte is an effective drug for the treatment of patients suffering from blood flow disorders of the lower extremities.
Gentamicin is an antibiotic of the aminoglycoside group, is derived from the growth of Micromonospora purpurea, an actinomycete. Gentamicin is a complex of three different closely related aminoglycoside sulfates, Gentamicins C1, C2, and C1a that have different patterns of methylation at the 69 position of the ring. Gentamicin C1a is a broad-spectrum antibiotic against Gram-positive and Gram-negative bacteria but may cause ear and kidney damage. Gentamicin C1a binds to the A-site RNA of the 30S bacterial ribosomal subunit. Adverse reactions include adverse renal effects, neurotoxicity (dizziness, vertigo, tinnitus, roaring in the ears, hearing loss, peripheral neuropathy or encephalopathy), respiratory depression, lethargy, confusion, depression, visual disturbances, etc.
Status:
Possibly Marketed Outside US
Source:
Japan:Dimefline Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


DIMEFLINE is a pneumokinetic and respiratory stimulant. It has been used for the treatment of respiratory insufficiency. The mechanism of action is unknown.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Biphenamine is a local anesthetic with antibacterial and antifungal properties. It has been used in the treatment of seborrheic scalp disorders.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)


Zorubicin is a benzoylhydrazone derivative of the anthracycline antineoplastic antibiotic daunorubicin, but it introduces lower cardiomyopathy and bone marrow toxicity. Zorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair as well as RNA and protein synthesis. The cytotoxic effect results from intercalation between DNA pairs. To minimize toxicity, individualized dose regimens are given preferentially over prolonged periods of time by carefully inspecting i.v. administration to prevent extravasation.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Medibazine (Vialibran) is a piperazine derivative. Medibazine is a coronary vasodilating agent. Although several non-controlled trials report favorable results with angina patients this medication certainly does not provide any outstanding results.
Aceclidine is a parasympathomimetic agent used in the treatment of open-angle glaucoma as topical eye drop solution. It is as a muscarinic acetylcholine receptor agonist with weak anticholinesterase activity. Acting directly on the motor end-plate (cholinergic nerve endings) it decreases intraocular pressure and mediates the contraction of iris muscle. Aceclidine increased outflow facility in human eyes in vitro by a direct stimulation of the outflow tissues in the absence of an intact ciliary muscle. This effect was biphasic, occurring at concentrations of 10 uM and lower with no effect at higher concentrations. Passed numerous clinical trials in Russia, France, Italy and other countries and was widely used in Europe but never been in clinical use in USA.

Showing 12601 - 12610 of 12951 results