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Restrict the search for
icosapent ethyl
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Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Pirenperone, a quinazoline derivative, is a selective antagonist at serotonin receptor 2A binding sites. The liposoluble compound pirenperone has been studied in a variety of behavioral tests including the sensitive d-lysergic acid diethylamide (LSD) cue discrimination assay, in which it served as a potent LSD-antagonist. Pirenperone also proved to be an effective antagonist of serotonin-mediated behavioral responses including the head twitch response thought to be mediated by serotonin receptors.
Status:
Investigational
Source:
INN:goxalapladib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Goxalapladib (SB-677116) is a selective inhibitor of Lipoprotein associated phospholipase A2 (Lp-PLA2).
Class (Stereo):
CHEMICAL (RACEMIC)
Pentisomide is an agent structurally related to disopyramide. Pentisomide is a class-I antiarrhythmic agent with a marked effect on depolarization (action of class Ia and Ic) and on repolarization. Pentisomide dose-dependently inhibited ischaemia-reperfusion arrhythmia. Pentisomide had been in phase II clinical trial for the treatment of arrhythmias. The electrophysiologic effects of pentisomide were investigated after intravenous and oral application in patients with drug refractory atrioventricular nodal tachycardia and patients with orthodromic atrioventricular re-entrant tachycardia. If intravenous pentisomide did not prevent induction of the tachycardia, oral pentisomide was not effective either. Long-term treatment with pentisomide had to be discontinued because of possible side effects.
Class (Stereo):
CHEMICAL (ACHIRAL)
Iosumetic Acid is a triiodoaminoisophthalic acid derivative patented by Schering A.-G. as contrast medium for direct and indirect lymphography.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Rupintrivir is a peptide aldehyde that targets the human rhinovirus (HRV) 3C proteinase enzyme and has the potential for the treatment of the common cold. Rupintrivir is derived from AG-6084 - in order to develop human rhinovirus 3C protease inhibitors with improved pharmacological properties, Agouron replaced the backbone amide moiety of the series which yielded AG-6084, with a ketomethylene isostere. A phase II efficacy study has been completed in healthy patients infected with the rhinovirus. Ruprintrivir was well tolerated; blood-tinged mucus and nasal passage irritation were the most common adverse effects reported. Pharmacokinetic analysis of plasma and nasal ruprintrivir concentrations revealed intranasal drug residence with minimal systemic absorption. The fact that rupintrivir is active against noroviruses belonging to genogroup I (Norwalk virus), genogroup V (murine norovirus), and the recombinant 3C-like protease of a GII norovirus suggests that the drug exerts cross-genotypic anti-norovirus activity and will thus most likely be effective against the clinically relevant human norovirus strains. Rupintrivir is also a high affinity inhibitor of Enterovirus-71 3C protease.
Status:
Investigational
Source:
NCT01757860: Phase 1 Interventional Completed Drug Safety
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
1α-HYDROXYVITAMIN D5 (CARD-024) is non-hypercalcemic, selective vitamin D receptor agonist under development for the treatment of cardiovascular disease, secondary hyperparathyroidism in chronic kidney disease and intestinal bowel disease fibrosis. CARD-024 attenuated the pro-fibrotic response of colonic myofibroblasts to high matrix stiffness, suggesting that it may ameliorate intestinal fibrosis.
Status:
Investigational
Source:
INN:pimefylline [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Pimefylline is an N-methylated xanthine derivative. It is a coronary vasodilator and muscle relaxant.
Class (Stereo):
CHEMICAL (ACHIRAL)
Nitromiphene (NIT; CI 628) is a triarylethylene antiestrogen shown to be effective in treatment of experimental breast cancer. Nitromiphene is one of the earliest nonsteroidal selective estrogen receptor modulators (SERMs). It is an anti-estrogen capable to translocate the estrogen receptor to the nucleus and to induce the replenishment of the cytosol receptor. Nitromiphene inhibited the uptake of [3H]-estradiol in rat whole homogenates and isolated cell nuclei tissues and the pituitary, and inhibited estradiol-induced female sexual behavior. Nitromiphene has thus been shown to suppress the growth of chemically induced and ransplantedmammary tumors in rodents. Also, Nitromiphene was shown to have potent, prolonged antiuterotropic effects in immature rats. Nitromiphene has been shown to undergo conversion to demethyl Nitromiphene (CI628M), a phenolic metabolite which had greater affinity for estrogen receptors and greater biological potency in vitro than did Nitromiphene. However, the in vivo antiestrogenic effects of Nitromiphene and demethyl Nitromiphene were similar, possibly due to facile O-demethylation of the former compound after administration.
Class (Stereo):
CHEMICAL (ACHIRAL)
Nitraquazone (TVX 2706) is an phosphodiesterase inhibitor with antiinflammatory action. It strongly enhances the increase in intracellular levels of cyclic AMP caused by appropriate effectors in all systems tested so far. EC50 values are in the submicromolar range. The effect is apparently neither due to an increased responsiveness of the hybrid cells for an effector like prostaglandin E1 nor to an increased activity of adenylate cyclase, but to an inhibition of both low and high affinity cyclic AMP phosphodiesterases. Half-maximal inhibition of enzyme activity is obtained at 10 uM TVX 2706. TVX 2706 does not interfere with the calmodulin activation of phosphodiesterase. Nitraquazone affected cytokine production by PHA-stimulated human blood cells. Nitraquazone was active in reducing the production of IL-5 (IC50 = 0.8 uM), while its potency against IL-2, GM-CSF and IFN-gamma was 3-6 times lower.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Dicarfen hydrochloride is a spasmolytic agent, local anesthetic and antiparkinsonian agent.
