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

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Showing 2091 - 2100 of 3134 results

Guanoclor is an anti-hypertensive agent developed by Pfizer Ltd. (U.K.). It seems to be effective in various types of hypertension (unknown aetiology, renal, and malignant). It affects both systolic blood-pressure and diastolic blood-pressure. It is an adrenergic neurone-blocking agent, which also interferes with noradrenaline synthesis by inhibition of the enzyme dopamine beta-hydroxylase. Clinical use of the compound was first reported by Lawrie et al. (1964), who achieved satisfactory blood-pressure control in 60% of their cases with guanoclor alone, and in a further 18% with the addition of a thiazide diuretic. They also noted a significant reduction in urinary noradrenaline levels during guanoclor administration. Guanochlor has an affinity for the Na+/H+ exchanger ranging between 0.5 uM and 6 uM in different systems and is more potent than amiloride in all systems studied. It is suggested that guanochlor recognizes a binding site on the Na+/H+ exchanger that is distinct from the amiloride binding site.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Guanoxabenz is an antihypertensive drug that was in clinical use in the 1980s. It acts as a selective agonist of alpha2A1 and alpha2B1 adrenergic receptors. Guanoxabenz is the main metabolite of the FDA-approved drug guanabenz.
Dirlotapide is indicated for the management of obesity in dogs. Dirlotapide is a microsomal triglyceride transfer protein (MTP) inhibitor. It mainly acts locally in the gut to reduce appetite, increase fecal fat and produce weight loss in dogs. The adverse reactions associated with treatment with Dirlotapide include vomiting, loose stools/diarrhea, lethargy, and anorexia.
Status:
Possibly Marketed Outside US
Source:
Vorozole by Janssen Pharmaceutica
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

Vorozole is a specific, non-steroidal inhibitor of aromatase enzyme that catalyzes the last step in estrogen biosynthesis. Vorozole interferes with the aromatase heme. The drug can be useful for postmenopausal patients with advanced breast cancer.
Status:
Possibly Marketed Outside US
Source:
Trocoxil by Searle
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Mavacoxib (trade name Trocoxil) is a veterinary drug used to treat pain and inflammation in dogs with the degenerative joint disease. Mavacoxib is a non-steroidal anti-inflammatory drug (NSAID) of the coxib class. Mavacoxib acts by preferential inhibition of COX-2-mediated prostaglandin synthesis. It, therefore, possesses analgesic and anti-inflammatory properties. The products of COX-2 metabolism are also involved in ovulation, implantation, and closure of the ductus arteriosus. Mavacoxib is well absorbed after oral administration; bioavailability was 87% in fed dogs and 46 % in fasted conditions and the recommended dose is based on administration with food. Therapeutic concentrations in fed dogs are reached rapidly and peak concentrations are obtained in less than 24 hours after administering a dose. Mavacoxib is approximately 98% bound to plasma proteins. It is extensively distributed throughout the body and almost all the mavacoxib-related residues in plasma comprise parent drug. The rate of body clearance of mavacoxib is slow and the major route of elimination is by biliary excretion of the parent drug. Adverse reactions of the digestive tract such as vomiting and diarrhea were commonly reported, loss of appetite, hemorrhagic diarrhea, and melaena have been reported in uncommon cases. Gastrointestinal ulceration was reported in rare cases. Apathy, degradation of renal biochemistry parameters and impaired renal function have been reported in uncommon cases. In rare cases, these adverse reactions may be fatal.
Status:
Possibly Marketed Outside US
Source:
Eftapan by Mauvernay, R.Y.
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



Eprazinone has been variously described as having mucolytic or expectorant properties as well as a direct relaxant action on bronchial smooth muscle and it suppress the excitation of cough center to stop coughing. It is usually used to treat symptoms of cough and phlegm caused by respiratory diseases such as cold, upper respiratory infection, bronchitis, and pneumonia The most commonly reported adverse reactions include loss of appetite, nausea/vomiting, stomach discomfort, diarrhea (including loose stool) and symptom of irritation.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)


Eprozinol inhibits bronchoconstriction by an action on histamine H1 receptors and has been used in the treatment of asthma and bronchitis. No significant changes in cAMP and cGMP levels are observed in guinea pig trachea, with eprozinol or isoprenaline, at doses capable of inducing relaxation. Eprozinol is only a very weak phosphodiesterase inhibitor, at large concentrations. The anti-bronchoconstrictor activities of eprozinol and isoprenaline with regard to histamine are directly additive and show absolutely no interference with one another. Propranolol is without effect on in vivo anti-bronchoconstrictor activity of eprozinol on tracheal musculature. It is concluded, that the mechanisms brought into play by eprozinol to exert anti-bronchoconstrictor and bronchorelaxant activity, are completely independent of the adrenergic system. In a retrospective study of 199 cases of accidental or intentional acute poisoning with eprozinol, eprazinone and zipeprol, collected at the Poison Control Center were seven cases of seizures, all after ingestion of eight times the therapeutic dose. They resolved rapidly and without recurrence with symptomatic treatment.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Morniflumate is a non-steroidal anti-inflammatory drug and represent as a beta-morpholinoethyl ester of niflumic acid, which is rapidly hydrolyzed in the plasma, releasing the free acidic form, the molecule responsible for the pharmacological effects. It was shown, that morniflumate was effective in the treatment of chronic recurring bronchitis and inhibited cyclooxygenase-1, 2 (COX-1, 2). Morniflumate has a 30-year history of clinical use, particularly for the treatment of pain associated with pediatric ear-nose-throat (ENT) infection. In addition, it appears to be a valid and well-tolerated alternative to other NSAIDs, or to antibiotics, for the treatment of pain and other symptoms of soft tissue inflammation.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

NELTENEXINE, an amide derivative of ambroxol and thiophenecarboxylic acid, is a mucolytic agent. It is an elastase inhibitor used in the treatment of human lung diseases.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Variotin (Pecilocin), an antifungal antibiotic, is produced by Paecilomyces varioti Bainer var. antibioticus and was isolated by Takeuchi et al. (1959). It is used topically for the treatment of human dermatomycosis.

Showing 2091 - 2100 of 3134 results