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

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Showing 31631 - 31640 of 31824 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Azidocillin is a narrow-spectrum, semisynthetic penicillin derivative with antibacterial activity towards Grain-positive and Gram-negative microorganisms, including Haemophilus influenze, against which it is as effective as ampicillin. Azidocillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis. Azidocillin can be applied in the treatment of inflammation of upper airways, middle ear, sinuses, throat, larynx and palatine tonsils. The substance is excreted with urine in 50-70% in the unchan¬ged form. It binds to the blood plasma proteins in 84%, and its half-life period is 30 min. The side effects are similar as those of benzylpenicillin but occur less frequently.
Status:
Possibly Marketed Outside US
Source:
Japan:Fentiazac
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Fentiazac is a non-steroidal anti-inflammatory agent developed for the treatment of pain disorders. The drug was marketed under the name Norvedan, however, its current marketing status is unknown and supposed to be "discontinued".
Status:
Possibly Marketed Outside US
Source:
Japan:Aclatonium Napadisilate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Aclatonium (also known as aclatonium napadisilate) is a cholinergic agonist that has been developed and used in Asia as an activator of gastrointestinal motility.
Status:
Possibly Marketed Outside US
Source:
Japan:Bopindolol Malonate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Bopindolol (4-[benzoyloxy-3-tertbutylaminopropoxy]-2-methylindole hydrogen malonate) is an indole beta-adrenoceptor antagonist bearing a benzoyl ester residue on the beta-carbon atom of the propanolamine side chain. Bopindolol is metabolized by esterase to benzoic acid and an active metabolite, 18-502 [4-(3-t-butylamino-2-hydroxypropoxy)-2-methyl indole], which is further metabolized to 20-785 [4-(3-t-butylaminopropoxy)-2-carboxyl indole]. Bopindolol produces sustained blockade of beta 1- and beta 2-adrenoceptors, has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is used in the treatment of hypertension. In limited trials bopindolol has also successfully reduced symptoms in patients with angina pectoris, anxiety and essential tremor.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)


Conditions:

Fenbutrazate is a prodrug of phenmetrazine, a psychostimulant for the treatment of obesity. Fenbutrazate acts as an agonist of monoamine transportes upon conversion to the active metabolite. The drug is no longer marketed due to its addictive profile.
Status:
Possibly Marketed Outside US
Source:
NCT01744236: Phase 4 Interventional Completed Type 2 Diabetes
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tilarginine is L-N-monomethyl arginine (L -NMMA), a non-selective inhibitor of nitric oxide synthase (NOS), which has been studied in the treatment of septic shock and cardiogenic shock complicating myocardial infarction. Despite strong evidence that excessive nitric oxide (NO) production plays a pivotal role in the pathogenesis of septic shock and may contribute to the pathogenesis of cardiogenic shock complicating myocardial infarction, outcome studies in these two disorders have proved disappointing. Tilarginine therapy was associated with an excess mortality, particularly at doses > 5 mg/(kg h), in septic shock, whereas the effects of a lower dose (1 mg/(kg h)) in cardiogenic shock complicating myocardial infarction were neutral. The excess mortality in patients with septic shock was almost certainly the result of unfavorable hemodynamic changes induced by Tilarginine (decreased cardiac output, increased pulmonary vascular resistance and reduced tissue oxygen delivery) whereas the lack of benefit in patients with cardiogenic shock complicating myocardial infarction may have been because the dose of Tilarginine was too low.
Status:
Possibly Marketed Outside US
Source:
Canada:PLATINUM MURIATICUM
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Conditions:

Diamminedichlorodihydroxyplatinum IV is the platinum-based antineoplasticis agent. Oxaliplatin is cis, cis, trans- isomer of Diamminedichlorodihydroxyplatinum IV. Oxaliplatin show high stability and therefore can be utilized orally for outpatient care. Although oxoplatin is capable of binding directly to DNA after prolonged incubation, platinum(IV) agents are considered to be largely inert prodrugs that are converted to highly cytotoxic platinum(II) compounds by reducing substances, enzymes, or microenvironmental conditions. Reaction of oxoplatin with 0.1 M hydrogen chloride mimicking gastric acid yields cis-diammine-tetrachlorido-platinum(IV) (DATCP[IV]), which exhibits two-fold increased activity. The oxoplatin metabolite DATCP(IV) constitutes a potent cytotoxic derivative that may be produced by gastric acid or acidic areas prevailing in larger solid tumors, depending on the respective pharmaceutical formulation of oxoplatin.
Status:
Possibly Marketed Outside US
Source:
Canada:SODIUM TETRACHLOROAURATE(III)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Amineptine is a selective inhibitor of dopamine reuptake. The drug was developed in France and was marketed for the treatment of depressive disorders under the name Survector among the others. Amineptine was withdrawn from the French market in 1999 because of abuse and drug dependence and because of its hepatic (cholestatic injuries) and cutaneous (acne) adverse effects.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Flupirtine is a triaminopyridine derivative having a chemical structure - 2-amino-3-ethoxy-carbonylamino-6-4-fluoro-benzylamino-pyridine. The basic molecule used for synthesis of flupirtine was 2, 6-dichoro 3-nitropyridine. It was first synthesized in 1980s in Germany and was marketed by Degussa Pharma. Flupirtine is a centrally acting, non-opioid analgesic that is available in a number of European countries for the treatment of a variety of pain states. The therapeutic benefits seen with flupirtine relate to its unique pharmacological properties. Flupirtine displays indirect NDMA receptor antagonism via activation of potassium channels and is the first representative of a pharmacological class denoted the 'selective neuronal potassium channel openers'. The generation of the M-current is facilitated by flupirtine via the opening of neuronal Kv7 potassium channels. The opening of these channels inhibits exaggerated neuronal action potential generation and controls neuronal excitability. Neuronal hyperexcitability is a physiological component of many pain states such as chronic pain, migraine and neurogenic pain.

Showing 31631 - 31640 of 31824 results