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A synthetic analog of PGF2α; an FP receptor agonist and a potent luteolytic agent in rats and hamsters; the optically active, 15(R) enantiomer of cloprostenol responsible for the majority of its biological activity
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A stereoisomer of the antitumor anthracycline doxorubicin that undergoes β-glucuronidation, which partially detoxifies the dose-limiting side effects that are present with doxorubicin; equally cytotoxic to HeLa cells compared to doxorubicin (ID50s = 9 μM)
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A nonselective inhibitor of the mitochondrial F1FO ATP synthase that can reduce the rate of ATP depletion in myocardial ischemia and decrease calcium-induced calcium release oscillation frequency of rat sensory neurons
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A selective serotonin reuptake inhibitor; inhibits monoamine uptake by SERT (IC50 = 70 nM); selective for SERT over the norepinephrine and dopamine transporters (IC50s = 520 and 720 nM, respectively); reduces immobility in the forced swim test in mice at 3.2-56 mg/kg, s.c.; prevents acid sphingomyelinase activation and subsequent ceramide release induced by pp-VSV-SARS-CoV-2 infection in Vero cells at 5 µM
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A derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding; a relatively selective, irreversible antagonist of D2 receptors both in vitro (IC50 = 100 nM) and in vivo; irreversibly inhibits calmodulin at higher doses (IC50 = 10 µM)
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9-keto Fluprostenol is an analog of PGE2 with structural modifications intended to give it a prolonged half-life and greater potency. Fluprostenol is a well-studied, potent analog of PGF2α and acts primarily through the FP receptor.{1182} Oxidation at C-9 of fluprostenol yields 9-keto fluprostenol. It is anticipated that this analog will have strong affinity for EP receptors and act as a PGE2 agonist.
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5-trans PGF2α tromethamine salt is a derivative of 5-trans PGF2α with increased water solubility. Its solubility in PBS is 25 mg/ml compared to 10 mg/ml for 5-trans PGF2α.
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A blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC50 = 0.75 and 0.71 µM, respectively) as well as KCNQ2+3 heteromultimers (IC50 = 0.6 µM); shows good in vivo potency and duration of action
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