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

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Showing 13101 - 13110 of 13362 results

Trifluperidol is an antipsychotic butyrophenone derivative. It is a high-affinity sigma receptor blocker and it was strongly selective for NR1a/2B receptors. It exhibit pharmacological effects and a mechanism of action very similar to that of phenothiazines and thioxanthenes in that it blocks dopaminergic receptors. It is more selective with respect to D2 receptors. Trifluperidol is indicated for the treatment of acute and chronic schizophrenia, mania and hypomania, organic psychoses, childhood behavioral disorders, agitation in psychotic illness and motor tics. Trifluperidol has been suspected as a cause of cataract in Japan. Patients receiving trifluperidol treatment may develop a parkinsonian-like syndrome which responds to withdrawal of the drug or concurrent administration of an anti-parkinsonian drug. Acute dystonias and akathisia are other acute extrapyramidal effects; tardive dyskinesia may supervene after longer periods of treatment.
(-)-Propranolol is a small molecule β-adrenergic receptor antagonist and the active isomer of (±)-Propranolol preparations. (-)-Propranolol blocks the binding of epinephrine, norepinephrine, and other endogenous catecholamines to the β-adrenergic receptor, impeding increases in cardiac flow velocity and general stimulation of the sympathetic nervous system signaled by the association of these molecules to the β-adrenergic receptor. In addition to blockade of agonist binding, antagonism of the β-adrenergic receptor by (-)-Propranolol produces negative chronotropic and inotropic action, effectively dampening the force and rate of cardiac contraction. These negative chronotropic and inotropic effects correlate to a demonstrated suppression of adrenaline-induced cardiac arrhythmia by (-)-Propranolol. Suppression of β-adrenergic receptor activation by (-)-Propranolol has been widely exploited in counteracting situations sensitive to heightened cardiac activity including hypertension, angina pectoris, and cardiac ischemia.
Status:
Possibly Marketed Outside US
Source:
Pepleo by Tanaka, W.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Peplomycin has been developed as novel analog of bleomycin, which has less pulmonary toxicity than bleomycin. Peplomycin has been the subject of extensive studies in Japan and Europe. It is indicated for the treatment of malignant lymphoma, head and neck cancer, lung cancer, prostate cancer and skin cancer. General side effects are: digestive symptoms such as stomatitis, anorexia, nausea/vomiting, general malaise, depilation, fever, chills etc.
Status:
Possibly Marketed Outside US
Source:
ZOPRANOL by Squibb Institute for Medical Research
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Zofenopril is an inhibitor of Angiotensin Converting Enzyme (ACE), which is approved in Europe for the treatment of hypertension and acute myocardial infarction.
Perhexiline, 2-(2,2-dicyclohexylethyl)piperidine, is an anti-anginal drug. Perhexiline reduces fatty acid metabolism through the inhibition of carnitine palmitoyltransferase, the enzyme responsible for mitochondrial uptake of long-chain fatty acids. Perhexiline is used for reducing the frequency of moderate to severe attacks of angina pectoris due to coronary artery disease in patients who have not responded to other conventional therapy or in whom such therapy may be contraindicated. Heart Metabolics Limited is developing perhexiline for the treatment of hypertrophic cardiomyopathy
Cilazapril (Vascace and Dynorm are brand names in a number of European countries) is an angiotensin converting enzyme (ACE; kininase II) inhibitor. It competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Cilazapril is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat. The half-life (30–50 hours) of cilazapril allows for once daily dosing unless the hypertension is severe. Cilazapril is used for the treatment of hypertension, congestive heart failure, post-myocardial infarction, and some other indications. Adverse events were mostly observed within the first 8-16 weeks of treatment, with headache, dizziness, fatigue, nausea, cough and chest pain being the most frequent.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Fosfonet sodium (or phosphonoacetate sodium), an organophosphorus compound, was found to be a specific inhibitor of the virus-induced DNA polymerases and thus could inhibit specifically the replication of herpes-viruses.
Status:
Possibly Marketed Outside US
Source:
NCT01851863: Phase 4 Interventional Completed Dyspepsia
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Melitracen (HCl) is a tricyclic antidepressant with actions and effects similar to amitriptyline.Melitracen (HCl) is given orally in the treatment of depression. It should be withdrawn gradually to reduce the risk of withdrawl symptoms. Melitracen (HCl) is primarily indicated in conditions like Anxiety, Asthenia, Depression, gastro-intestinal disorders associated with anxiety and agitation. Melitracen is marketed in Europe and Japan by Lundbeck and Takeda, respectively, for the treatment of depression and anxiety. In addition to single drug preparations, it is also available as Deanxit, a combination product containing both melitracen and flupentixol. The way this drug works hasn’t been thoroughly researched, but some hypothesize that it may work similarly to the drugs Imipramine and Amitriptyline. In comparison to older TCAs, this drug is thought to work more quickly with more favorable side effects.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Adinazolam, a benzodiazepine agonist, is an effective anxiolytic agent with antidepressant properties. It was shown, that adinazolam by itself had relatively weak benzodiazepine agonist activity, and much of the pharmacological activity belonged to its active metabolite N-desmethyladinazolam (NDMAD). Adinazolam has never been FDA approved, but it is sold as a research chemical.
Status:
Possibly Marketed Outside US
Source:
Schmerz. Apr 2003;17(2):110-6.: Phase 4 Human clinical trial Completed Pain, Postoperative
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

TILIDINE is a low to medium potency opioid analgesic. It is metabolized to its active metabolites, nortilidine and bisnortilidine. Its analgesic activity is largely exerted through nortilidine which is a potent agonist at Mu opioid receptors.

Showing 13101 - 13110 of 13362 results