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Restrict the search for
methyl salicylate
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Class (Stereo):
CHEMICAL (ABSOLUTE)
Romergoline (FCE 23884) is an ergoline derivative and a dopamine receptor agonist and antagonist. Its action depends on the functional state of the biological substrate, mostly related to the presence or absence of dopamine. In healthy animals, it behaves as a full dopamine antagonist, but in denervated models it behaves as an agonist. Therefore, romergoline was suggested to be potentially useful in both psychotic states and extrapyramidal diseases. In Parkinson patients, the degree of dopamine receptor stimulation was found to be insufficient to improve symptoms. Information about further development of romergoline is not available.
Status:
Investigational
Source:
NCT00385099: Phase 2 Interventional Completed Irritable Colon
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Emicerfont (GW876008) is a nonpeptide vcorticotropin-releasing factor type 1 (CRF1) receptor antagonist. It was in clinical trials for the treatment of anxiety disorders, irritable bowel syndrome and major depressive disorder however development of emicerfont has been discontinued.
Status:
Investigational
Source:
NCT01064037: Phase 2 Interventional Terminated Heart Failure
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Cinaciguat acts specifically on oxidized/haem-free soluble guanylyl cyclase by binding to the enzyme's haem pocket and mimicking the nitric-oxide-bound haem group. It is in clinical development for the treatment of acute decompensated heart failure. Cinaciguat had been in phase II clinical trials. However, trials were terminated early because of an excess of hypotension in the cinaciguat arms and subsequent slow enrolment.
Class (Stereo):
CHEMICAL (ACHIRAL)
Lifarizine is a use- and voltage-dependent antagonist of human voltage sensitive sodium currents. Lifarizine inhibited both the plateau and the spike phases of the Ca2+ increases suggesting that, in addition to its known sodium channel blocking properties, it may also inhibit more than one class of calcium channel in the synaptosomes. Lifarizine reduced both infarct area and volume in the mouse with middle cerebral artery occlusion. Lifarizine was in phase II for the treatment of stroke but this investigation was discontinued.
Status:
Investigational
Source:
NCT02367820: Phase 3 Interventional Completed Low Back Pain
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT00143520: Phase 2/Phase 3 Interventional Completed Type 2 Diabetes
(2004)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Rivoglitazone hydrochloride (CS-011) is a thiazolidinedione-derivative peroxisome proliferator–activated receptor (PPAR)-γ agonist. It has been developed as potential treatment in type 2 diabetes mellitus and was shown to decrease plasma glucose and triglyceride levels in a dose-dependent manner in animals. Phase II and III clinical studies have assessed the efficacy and safety of rivoglitazone hydrochloride in patients with type 2 diabetes mellitus.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cefsumide is an antibiotic of the cephalosporin group patented by Fujisawa Pharmaceutical Co. Cefsumide binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Setoperone is and antagonist of the brain serotonin 5-HT2 receptor and particular the 5-HT2A isoform. Setoperone is radiolabeled with the radioisotope fluorine-18 and is used in positron emission tomography (PET) in neuroimaging for the study neuropsychiatric disorders, such as schizophrenia and depression.
Class (Stereo):
CHEMICAL (ACHIRAL)
Ropizone (SC-13504) is an anticonvulsant. This compound both enhances and inhibits [3H]dextromethorphan (DM) high-affinity binding to different areas of the guinea pig brain, suggesting distinct binding site types in the brain. Ropizone was shown to have limited anti-convulsant activity against chemically induced seizures. The drug may have anti-grand mal activity but lacked any anti-petit mal effect in Beagle dogs. No information on the current use of this compound is available.
Status:
Investigational
Source:
NCT03739125: Phase 3 Interventional Completed Type2 Diabetes
(2017)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Lobeglitazone (trade name Duvie; Chong Kun Dang Pharmaceutical Corporation) was developed as effective and safe antidiabetic TZD drug. Lobeglitazone is a peroxisome proliferator-activated receptor-γ agonist. Lobeglitazone was conceptually designed by modification of the rosiglitazone structure with a substituted pyrimidine. Lobeglitazone has a p-methoxyphenoxy group at the 4-position of the pyrimidine moiety. Lobeglitazone showed more potent activity than the reference compounds (pioglitazone and rosiglitazone) with an EC50 value of 0.018 uM in a type 2 diabetes animal model, which is 16 times lower than pioglitazone (EC50 0.30 uM). Lobeglitazone exhibited similar efficacy profiles in glycemic control and lipid modulation to pioglitazone, but with a 30 times smaller dose in clinical studies. Lobeglitazone displays 12 times higher affinity to PPARγ than rosiglitazone and pioglitazone. Lobeglitazone acts as an insulin sensitizer by binding and activating Peroxisome Proliferator-Activated Receptors (PPAR) gamma within fat cells. By promoting the binding of insulin at fat cells, lobeglitazone has been shown to reduce blood sugar levels, lower hemoglobain A1C (HbA1C) levels, and improve lipid and liver profiles. Lobeglitazone was approved by the Ministry of Food and Drug Safety (Korea) in 2013. Lobeglitazone is not approved for use by either the Food and Drug Administration (USA), Health Canada, or by the European Medicines Agency for use in the management of diabetes.