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

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Showing 33751 - 33760 of 34007 results

Status:
Possibly Marketed Outside US
Source:
NCT04601324: Phase 4 Interventional Withdrawn Allergic Rhinitis
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Rupatadine is characterised as a non-sedating H1 anti-histamine and platelet-activating factor (PAF) receptor antagonist. Rupatadine is indicated for the treatment of allergic rhinitis and urticaria. Rupatadine is a safe and well tolerated drug in patients over 2 years old, with no central nervous system or cardiovascular effects and it can be taken with or without foods.
Status:
Possibly Marketed Outside US
Source:
Japan:Rilmazafone Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Rilmazafone (previously known as 450191-S) is a water-soluble benzodiazepine prodrug developed in Japan. It has sedative and hypnotic effects. Rilmazafone induces impairment of motor function and has hypnotic properties. Rilmazafone has no effects on benzodiazepine receptors itself, but once inside the body is metabolised by aminopeptidase enzymes in the small intestine to form the active benzodiazepine 8-chloro-6-(2-chlorophenyl)-N,N-dimethyl-4H-1,2,4-triazolo benzodiazepine-2-carboxamide. Preclinical studies have shown its excellent effects inducing and maintaining sleep with little effect on the skeletal muscle. Earlier the clinical dose for this drug as a premedicant was found to be 2-4mg.
Status:
Possibly Marketed Outside US
Source:
Leshcutan by Bensonab, R.A.|Slobodyab, L.B.|Lillickab, L.|Maffiaab, A.|Sullivan, N.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Benzyldimethyl(2-(2-((4-(1,1,3,3-Tetramethylbutyl)-O-Tolyl)Oxy)Ethoxy)Ethyl)Ammonium colloquially known as Methylbenzethonium Chloride has been used in the study stem cell death-inducing small molecules as well as anti-leishmanial activity. It is a component of the pharmaceutical preparation 'Leshctan' antibacterial ointment in Isreal.
Acefylline is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. Acephylline piperazine is a theophylline derivative with a direct bronchodilator action. It has the advantages over theophylline in being far less toxic and producing minimal gastric irritation. It is indicated for the treatment of asthma, emphysema, acute and chronic bronchitis associated with bronchospasm.Acefylline relaxes smooth muscles, relieves bronchospasm & has a stimulant effect on respiration. It stimulates the myocardium & central nervous system, decreases peripheral resistance & venous pressure & causes diuresis. The mechanism of action is still not clear, inhibition of phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism & effects on intracellular calcium. Sodium phenobarbital is a non-selective central nervous system depressant that is primarily used as sedative-hypnotic.
Status:
Possibly Marketed Outside US
Source:
NCT01395329: Phase 4 Interventional Completed Prehypertension
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


BQ-788, a selective endothelin (ET) B-receptor antagonist, was developed by Banyu. This compound is widely used to demonstrate the role of ET-1 and ET(B) receptor subtypes in physiological and/or pathophysiological conditions. BQ-788 was studied against hypertension. However, this study was discontinued. Besides, was shown that BQ788 could protect against brain edema by inhibiting vascular endothelial growth factor-A-mediated decrease in claudin-5. The intralesional applications of BQ788 were well tolerated and showed signs of directly and indirectly reducing the viability of melanoma cells.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Emepronium bromide (Cetiprina) is a quarternary ammonium compound with anticholinergic effects. It is mainly used in the treatment of urinary frequency, urge and urge incontinence and is usually administered orally and occasionally intramuscularly. Emepronium bromide was introduced into Britain, after having been used in Sweden for a number of years. The drug was advocated especially for elderly patients suffering from nocturia and urgency with incontinence, when these were due to causes other than obstruction. It was also advocated for enuresis and hypertonic bladder states following surgery or radiotherapy.
Status:
Possibly Marketed Outside US
Source:
NCT01876628: Phase 4 Interventional Completed Cellulitis
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Flucloxacillin is an isoxazolyl penicillin of the β-lactam group of antibiotics, which exerts a bactericidal effect upon many Gram-positive organisms including β-lactamase-producing staphylococci and streptococci. While no longer used in the United States, Flucloxacillin is supplied under a variety of trade names in other countries, including Floxapen, Flopen, Staphylex. Floxapen is indicated for the treatment of infections due to sensitive Gram-positive organisms, including β-lactamase-producing staphylococci and streptococci. Typical indications including, skin and soft tissue infections; respiratory tract infections; other infections caused by floxapen-sensitive organisms, like example, osteomyelitis, urinary tract infection, septicaemia, endocarditis. Floxapen is also indicated for use as a prophylactic agent during major surgical procedures when appropriate; for example cardiothoracic and orthopaedic surgery. Flucloxacillin, by its action on the synthesis of the bacterial wall, exerts a bactericidal effect on streptococci except those of group D (Enterococcus faecalis) staphylococci. It is not active against methicillin-resistant staphylococci. There is evidence that the risk of flucloxacillin induced liver injury is increased in subjects carrying the HLA-B*5701 allele. Despite this strong association, only 1 in 500-1000 carriers will develop liver injury. Consequently, the positive predictive value of testing the HLA-B*5701 allele for liver injury is very low (0.12%) and routine screening for this allele is not recommended. Flucloxacillin diffuses well into most tissue. Specifically, active concentrations of flucloxacillin have been recovered in bones: 11.6 mg/L (compact bone) and 15.6 mg/L (spongy bone), with a mean serum level of 8.9 mg/L. Flucloxacillin diffuses in only small proportion into the cerebrospinal fluid of subjects whose meninges are not inflamed. It is also excreted in small quantities in mother's milk. In normal subjects approximately 10% of the flucloxacillin administered is metabolised to penicilloic acid. The elimination half-life of flucloxacillin is in the order of 53 minutes.
Status:
Possibly Marketed Outside US
Source:
NCT03278431: Phase 4 Interventional Completed Hookworm Infection
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Oxantel is a narrow-spectrum anthelmintic effective against whipworms in dogs and cats. It is ineffective against other roundworms, flukes, tapeworms or external parasites. Oxantel acts on the nervous system of the worms as inhibitors of acetylcholinesterase. Oxantel, a cholinergic anthelmintic and fumarate reductase inhibitor, significantly inhibited biofilm formation by P. gingivalis and disrupted established biofilms at concentrations below its MIC against planktonic cells. Oxantel was more effective against P. gingivalis in biofilm than metronidazole, a commonly used antibiotic for periodontitis. When oxantel was administrated to human beings for the treatment of trichuriasis, no drug reaction or side effects were reported, and the results of hematologic, biochemical and urinary examinations didn’t reveal any significant drug-related changes.
Status:
Possibly Marketed Outside US
Source:
Апрофен
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Aprofene (widely known as aprophen or Апрофен (in Russia)), a Soviet drug, is an antagonist of muscarinic and nicotinic acetylcholine receptors. It had been used in Russia for the treatment of endarteritis (inflammation of the inner shell of the artery), peptic ulcer of the stomach and duodenum, spastic colitis (inflammation of the colon characterized by sharp contractions), cholecystitis (inflammation of the gallbladder) until was included in the list of psychotropic substances.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Ketobemidone (Cliradon, Ketogan, Ketodur, Cymidon) is a strong opioid analgesic, structurally related to pethidine, which has been in clinical use for more than 50 years. In the Scandinavian countries ketobemidone is only available in combination with a spasmolytic substance N,N-dimethyl-3,3-diphenyl-I-methylallylamine (A29). Ketobemidone has been shown to be a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist. In spite of a relatively low mu-receptor affinity ketobemidone has a higher analgesic potency than morphine by systemic administration. It is probably due to its higher lipophilicity and consequently more easy penetration into the CNS. Ketobemidone is indicated for the treatment of all types of severe pain, such as postoperative, cancer, kidney stones and fractures.

Showing 33751 - 33760 of 34007 results