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Class (Stereo):
CHEMICAL (RACEMIC)
Lorapride is a centrally acting sulfonamide. It has pharmacodynamic properties that are mainly related to ulcer treatment. On the basis of its psychopharmacologic profile, it has no neuroleptic potential, but it does exhibit some psychostimulating components. After oral administration, absorption of lorapride was rapid. The rate of absorption was first order for solution and zero order for capsule.
Class (Stereo):
CHEMICAL (RACEMIC)
Sumetizide is a sulfonamide derivative belonging to the class of the thiazide diuretics with anti-hypertensive activity. Sumetizide was patented by Richard Hurmer and Jean Vernin but never marketed.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Adaprolol is a beta-adrenergic antagonist that is being developed as a topical agent to treat glaucoma. Adaprolol demonstrated a safer cardiovascular profile, especially in the population over 70 years old. It was in Phase II clinical trials for the treatment of glaucoma. This research has been discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Diamfenetide (aka diamphenethide) is a fasiolicide used in sheep. It is effective against immature flukes but with diminishing activity as the fluke ages. It has proven an effective compound for use in prophylactic programs against Fasciola hepatica. Diamphenethide is deacetylated in the host liver to an active monoamine and diamine. The amine of diamfenetide has an action
which produces an elevation of malate concentration
in Fasciola. Malate is an intermediary product of glucose in this parasite. It is known that dopamine, a putative
neurotransmitter in Fasciola has a protective effect
against diamfenetide but the mode of action of a
diamfenetide has yet to be defined in greater detail.
Status:
Investigational
Source:
NCT01355497: Phase 3 Interventional Completed Muscle Wasting
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
MK-2866 (Gtx-024) is a selective androgen receptor modulator (SARM) for treatment of conditions such as muscle wasting and osteoporosis. It is a non-steroidal agent with anabolic activity designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.
Class (Stereo):
CHEMICAL (ACHIRAL)
Dichlorotetrafluoroethane is used for cryoanalgesia. Dichlorotetrafluoroethane has been used as an anesthetic in dermabrasion. Cryoanalgesia with dichlorotetrafluoroethane is effective and easily utilized by a dermatologist and a nurse assistant or even by a physician on his own, with occasional help from his patient. Dichlorotetrafluoroethane is a common fluorocarbon aerosol propellant. Dichlorotetrafluoroethane exhibits a vasodepressor activity on skeletal muscle vascular bed, which is readily overcome by the hypotension-induced activation of the sympathetic system but which becomes evident when reflex activity is prevented by vagotomy. The inhalation of fluorocarbons caused a depression of myocardial contractility, aortic hypotension a decrease in cardiac output and an increase in pulmonary vascular resistance. In rats, severe electrocardiographic changes including marked bardycardia, atrioventricular heart block of the second degree and complete heart block were registered.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Daltroban (also known as BM 13505, SKF 96148), a specific thromboxane A2 receptor antagonist, was studied as an antithrombotic agent. The drug was licensed to Smith Kline Beecham, underwent phase III clinical trials in the UK and Germany as an antithrombotic agent but did not enter clinical trials in the USA. Besides, вaltroban was investigated in patients with an ischemic heart disorder. However, the development of daltroban has been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Bederocin (REP8839) is a novel methionyl-tRNA synthetase (MetS) inhibitor being developed by Replidyne (GlaxoSmithKline licensed REP8839 to Replidyne it). The biochemical activity of REP8839 was shown by specific inhibition of purified S. aureus MetS (50% inhibitory concentration, <1.9 nM). Target specificity was confirmed by overexpression of the metS gene in S. aureus, resulting in an eightfold increase in the MIC for REP8839. Macromolecular synthesis assays in the presence of REP8839 demonstrated a dose-dependent inhibition of protein synthesis and RNA synthesis in S. pneumoniae R6, but only protein synthesis was affected in an isogenic rel mutant deficient in the stringent response. REP8839 is a novel diary diamine-containing MetS inhibitor that has not been previously disclosed but is related to the previously described compounds and is currently being evaluated as a topical antibiotic for the treatment of skin infections and eradication of S. aureus from the anterior nares.
Status:
Investigational
Source:
INN:befloxatone [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Befloxatone (MD-370,503) is a reversible inhibitor of monoamine oxidase A that was developed by Synthelabo for the treatment of depression, social phobias, and panic disorders. This drug participated in phase III clinical trials in France for depression. In addition participated in phase II for smoking cessation, anxiety disorders. Befloxatone has a good safety profile, lacking sedative, convulsant, anticholinergic and cardiovascular effects. However, all studies were discontinued.
Class (Stereo):
CHEMICAL (RACEMIC)
Ronipamil was developed as a verapamil analogue with a longer duration of action. However, it has much less calcium antagonist action than verapamil. Ronipamil has been tested for its ability to reduce ischaemia-induced arrhythmias in conscious rats. Compared to similar compounds, ronipamil was less effective and produced no statistically significant antiarrhythmic effects in rats. It had limited haemodynamic effects and no marked actions on blood pressure and heart rate. In another study, ronipamil prolonged survival time after traumatic shock and was shown to possess anti-shock potential. No information on current development of this drug is available.