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Volumn 19, Issue 16, 2009, Pages 4630-4633

Novel, achiral aminoheterocycles as selective monoamine reuptake inhibitors

Author keywords

Indole; Major depressive disorder; Monoamine reuptake inhibitor; Neurotransmitter; TRI; Triple reuptake inhibitor

Indexed keywords

3 AMINOPIPERIDINE; 3 AMINOPYRROLIDINE; 4 AMINOPIPERIDINE; ANTIDEPRESSANT AGENT; CARBENE; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; HETEROCYCLIC AMINE; MONOAMINE; MONOAMINE UPTAKE INHIBITOR; PHENYL GROUP; PIPERIDINE DERIVATIVE; POTASSIUM CHANNEL HERG; PYRROLIDINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 67651097819     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.06.076     Document Type: Article
Times cited : (6)

References (20)
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    • note
    • Neither the postulated electrophilic diiminoquinone-like intermediate or its derivatives were identified in metabolite ID studies.
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    • note
    • TDI was measured as the percentage of CYP3A4 inactivation after pre-incubation of the test compound for 25 min with human liver microsomes. The potential risk was ranked low if the measured value was less than that observed for ethynylestradiol (no clinical effects observed due to TDI), high if it was greater than that observed for verapamil (drug-drug interactions observed in the clinic), and moderate if it lay between ethynylestradiol and verapamil.
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    • note
    • + currents in CHO cells expressing the human ERG channel. Recordings were made at 30 °C with test compounds at two concentrations (0.3 μM, 1 μM, or 1 μM, 10 μM).
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    • note
    • int measured in HT format: total incubation volume 250 μL, 0.5 mg/mL microsomal protein, reaction started by adding NADPH and performed at 37 °C with no shaking. 40 μL aliquots at four time-points (0.1, 10, 20 and 30 min) were taken then the samples transferred to 384 well plates for LC/MS analysis.
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    • note
    • CYP2D6 and CYP3A4 inhibition was measured in a fluorescence based assay where CYP marker substrates become fluorescent upon CYP metabolism.
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    • note
    • app A to B and B to A) values. Substrate concentration 10 μM.
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* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.