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Restrict the search for
telotristat ethyl
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Pirodavir (R77975) (ethyl 4-[2-(1-[6-methyl-3-pyridazinyl]-4-piperidinyl)ethoxy]benzoate) and its predecessor (R61837) belong to a series of pyridazine analogues developed by the Janssen Research Foundation. Compared to R61837, pirodavir was 500-fold more potent as an antiviral in vitro, inhibiting 80% of 100 rhinovirus serotypes tested at concentration of 0.064 mg/mL or less. Pirodavir acts at an early stage of the viral replication cycle (up to 40 min after infection) and reduces the yield of selected rhinoviruses 1,000- to 100,000-fold in a single round of replication. The mode of action appears to be serotype specific, since pirodavir was able to inhibit the adsorption of human rhinovirus 9 but not that of human rhinovirus 1A. Pirodavir is a novel capsid-binding antipicornavirus agent with potent in vitro activity against both group A and group B rhinovirus serotypes.
Class (Stereo):
CHEMICAL (ACHIRAL)
Sulnidazole is a nitroimidazole derivative patented by Belgian pharmaceutical company Janssen Pharmaceutica N. V. as an antiprotozoal agent that effective against Trichomonas vaginalis.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Tiotidine is a controversial histamine H2 receptor ligand with negligible activity against H1- and H3- receptors. It was found that tiotidine behaves as an inverse agonist in U-937 cells, diminishing basal cAMP levels. Tiotidine showed two binding sites, one with high affinity and low capacity and the other with low affinity and high capacity. Tiotidine is currently in use as a radioligand in histamine H2-receptor binding studies. Compared to cimetidine, tiotidine appears to be approximately eight times more potent on a molar basis than cimetidine as an inhibitor of acid secretion, and the tiotidine effect is more prolonged. It was developed for the treatment of peptic ulcer.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Sonepiprazole exhibits highly specific binding
to the D4 dopamine receptor with more than 100-fold
selectivity for the D4 receptor over other receptors, including
dopamine, serotonin, and adrenergic receptors. It is a neutral antagonist at the D4 dopamine
receptor and is devoid of dopamine agonist activity. Sonepiprazole selectively induces c-fos expression in
the prefrontal cortex and blocks behavioral, biochemical, and
genomic effects of repeated amphetamine administration in rats. Sonepiprazole was investigated as an antipsychotic for the treatment of schizophrenia in a placebo-controlled clinical trial, but in contrast to its comparator olanzapine no benefits were found and it was not researched further for this indication.
Class (Stereo):
CHEMICAL (ACHIRAL)
Ocaperidone [R 79598] is an equipotent antagonist of central dopamine D2 and serotonin2 receptors being investigated as a potential antipsychotic agent. Ocaperidone is a benzisoxazol piperidine antipsychotic primarily binds and with high affinity to 5-HT2 (serotonin) receptors, alpha1 and alpha 2 adrenergic receptors, dopamine D2 receptors and histamine H1 receptors. Ocaperidone is an antagonist primarily at the 5HT and D2 receptors. A proposed mechanism of action is the central D2 receptor blockade which is common to all neuroleptics that are used to treat positive symptoms of schizophrenia.
Class (Stereo):
CHEMICAL (RACEMIC)
Tienoxolol is a benzoic acid derivative patented by Centre d'Activite et de Recherche Pharmaceutique Industrielle Biologique et Medicale as β-sympatholytic and diuretic. Tienoxolol acts as a beta-adrenergic receptor antagonist shows potent diuretic and natriuretic activity and, besides that anti-hypertension activity in preclinical models. In clinical trials, Tienoxolol significantly and dose-dependently reduced exercise-induced tachycardia. This effect started 1 h after drug administration, peaked between 4 h and 6 h and lasted at least 12 h.
Status:
Investigational
Source:
Rev Med Interna Neurol Psihiatr Neurochir Dermatovenerol Med Interna. 1978;30(4):299-304.: Not Applicable Human clinical trial Completed Gastrointestinal Diseases
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Metiamide is an antagonist of histamine H2-receptors synthesized at Smith Kline & French Laboratories. It potently inhibited gastric acid secretion. Metiamide demonstrated promising clinical effects in patients with duodenal ulcers but questionable safety.
Class (Stereo):
CHEMICAL (ACHIRAL)
FLOSATIDIL is an antihypertensive drug discontinued in Phase II for angina pectoris.
Status:
Investigational
Source:
INN:fluzoperine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Fluzoperine was studied as an antiarrhythmic agent. However, information about the current use of this drug is not available.
Status:
Investigational
Source:
INN:fopirtoline [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
