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Volumn 16, Issue 7, 2006, Pages 2022-2025

Discovery of novel and selective tertiary alcohol containing inhibitors of the norepinephrine transporter

Author keywords

MMT; ADHD; Atomoxetine; Attention deficit hyperactivity disorder; Depression; Dopamine; Inhibitor; Metariminol; Morpholine; Norepinephrine; Reuptake; Selective norepinephrine reuptake inhibitor; Serotonin; Tertiary alcohol

Indexed keywords

ALCOHOL DERIVATIVE; BENZENE DERIVATIVE; DOPAMINE; MORPHOLINE DERIVATIVE; NORADRENALIN; NORADRENALIN TRANSPORTER; NORADRENALIN UPTAKE INHIBITOR; PROTEIN INHIBITOR; REAGENT; SEROTONIN TRANSPORTER;

EID: 33144462082     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.12.061     Document Type: Article
Times cited : (15)

References (22)
  • 11
    • 33144481454 scopus 로고    scopus 로고
    • note
    • 2 with 0.2% DEMA (diethylmethylamine); temperature: 35°C; outlet pressure: 100 bar; injection: 1 ml (500 mg); detection: UV at 260 nm.
  • 12
    • 33144472260 scopus 로고    scopus 로고
    • note
    • 20 +29.7° (MeOH, 11.78 g/l). Other data identical to enantiomer 1.
  • 13
    • 33144486065 scopus 로고    scopus 로고
    • note
    • See Ref. 8 for detailed experimental procedures for Grignard addition and deprotection. Enantiomer separation was achieved using the following methods: isomers 1 and 2 chiral HPLC on a Chiralpak AD 10 μm column (supplied from Chiral technologies, Illkirch, France) with 85% heptane: 15% ethanol (0.2% DMEA) as eluent using a flow rate of 12 ml/min and UV detection at 260 nm. Isomers 3 and 4 chiral HPLC on a Chiralpak AD 10 μm column (supplied from Chiral technologies, Illkirch, France) with 85% heptane: 15% ethanol (0.2% DMEA) as eluent using a flow rate of 12 ml/min and UV detection at 260 nm.
  • 14
    • 33144479105 scopus 로고    scopus 로고
    • or by emailing data_request@ccdc.cam.ac.uk, or by contacting The Cambridge Crystallographic Data Centre, 12, Union Road, Cambridge CB2 1EZ, UK; fax: +44 1223 336033.
    • CCDC 291659 contains the supplementary crystallographic data for this paper. These data can be obtained free of charge via www.ccdc.ac.uk/ data_request/cif, or by emailing data_request@ccdc.cam.ac.uk, or by contacting The Cambridge Crystallographic Data Centre, 12, Union Road, Cambridge CB2 1EZ, UK; fax: +44 1223 336033.
  • 18
    • 33144484820 scopus 로고    scopus 로고
    • note
    • Remaining parent compound 16 after 15 min incubation in liver microsomes (1 μmol/l, 0.5 mg/ml protein) of different species: Human 98%, Dog 60% and Rat 0%.
  • 19
    • 33144485202 scopus 로고    scopus 로고
    • note
    • Compound 15 was shown to be configurationally stable in solution for at least 3 days at 40°C, in water, 0.1 N HCl and in buffer solutions over a pH range of 2-8.
  • 22
    • 33144463874 scopus 로고    scopus 로고
    • note
    • Male Sprague-Dawley rats gavaged 1 h prior to 6.25 mg/kg subcutaneous α-MMT. Rats sacrificed 4 h after α-MMT administration (N = 5).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.