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(Phenylpiperazinyl-butyl)oxindoles as selective 5-HT7 receptor antagonists.
A series of potent 5-hydroxytryptamine 7 (5-HT 7) ligands has been synthesized that contain a 1,3-dihydro-2 H-indol-2-one (oxindole) skeleton. The binding of these compounds to the 5-HT 7 and 5-HT 1AExpand
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Medicinal chemistry of 5-HT5A receptor ligands: a receptor subtype with unique therapeutical potential.
Although the 5-HT(5) receptor subfamily was discovered more than 15 years ago, it is unambiguously the least known 5-HT receptor subtype. The G(i)/G(0)-mediated signal transduction and its intensiveExpand
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A novel GABA(A) alpha 5 receptor inhibitor with therapeutic potential.
Novel 2,3-benzodiazepine and related isoquinoline derivatives, substituted at position 1 with a 2-benzothiophenyl moiety, were synthesized to produce compounds that potently inhibited the action ofExpand
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Interactions of non-charged tadalafil stereoisomers with cyclodextrins: capillary electrophoresis and nuclear magnetic resonance studies.
The single isomer drug R,R-tadalafil (Cialis) contains two chiral centers thus four stereoisomers (R,R-, S,S-, S,R- and R,S-tadalafil) exist, however, only the most potent inhibitor, theExpand
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Continuous flow production in the final step of vortioxetine synthesis. Piperazine ring formation on a flow platform with a focus on productivity and scalability
In this study, the piperazine formation step of vortioxetine synthesis was investigated under continuous flow conditions. The batch variant of this step could be carried out at laboratory scale atExpand
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Optimization of (arylpiperazinylbutyl)oxindoles exhibiting selective 5-HT₇ receptor antagonist activity.
A series of (arylpiperazinylbutyl)oxindoles as highly potent 5-HT(7) receptor antagonists has been studied for their selectivity toward the 5-HT(1A) receptor and α(1)-adrenoceptor. SeveralExpand
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Synthesis and in vitro evaluation of oxindole derivatives as potential radioligands for 5-HT(7) receptor imaging with PET.
The most recently discovered serotonin (5-HT) receptor subtype, 5-HT(7), is considered to be associated with several CNS disorders. Noninvasive in vivo positron emission tomography (PET) studies ofExpand
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5-HT6/7 Receptor Antagonists Facilitate Dopamine Release in the Cochlea via a GABAergic Disinhibitory Mechanism
In humans, serotonin (5-HT) has been implicated in numerous physiological and pathological processes in the peripheral auditory system. Dopamine (DA), another transmitter of the lateral olivocochlearExpand
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New One-Pot Synthesis of 3-Alkyl- and 3-(ψ-Hydroxyalkyl)oxindoles from Isatins
A new and efficient one-pot procedure has been developed for the synthesis of 3-alkyl- and 3-(ψ-hydroxyalkyl)oxindoles from isatins by treatment with alcohols and diols in the presence of RaneyExpand
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Manufacture of High-Purity Meloxicam via Its Novel Potassium Salt Monohydrate
An improved procedure for the manufacture of 4-hydroxy-2-methyl-N-(5-methyl-1,3-thiazol-2-yl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide (meloxicam) is described. The key intermediate of thisExpand
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