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Volumn 17, Issue 7, 2007, Pages 2022-2025

N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors

Author keywords

hERG; Metabolic stability; Noradrenaline reuptake; Serotonin reuptake; SNRI

Indexed keywords

AMINE; CYTOCHROME P450 2D6; DULOXETINE; SEROTONIN NORADRENALIN REUPTAKE INHIBITOR; VENLAFAXINE;

EID: 33847732615     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.01.020     Document Type: Article
Times cited : (16)

References (20)
  • 11
    • 33847706643 scopus 로고    scopus 로고
    • After we completed this series, researchers at Eli Lilly independently published their own work in this area, Beadle, C. D.; Cases-Thomas, M. J.; Clark, B. P.; Gallagher, P. T.; Masters, J. J.; Timms, G. H.; Walter, M. W.; Whatton, M. A.; Wood, V. A.; Gilmore, J. WO2005000811.
  • 12
    • 0025890297 scopus 로고
    • 50 values, that is, concentration required to inhibit the specific uptake of radiolabelled substrate into the cells by 50% relative to maximum (vehicle only) over a 10-point dose-response range.
    • 50 values, that is, concentration required to inhibit the specific uptake of radiolabelled substrate into the cells by 50% relative to maximum (vehicle only) over a 10-point dose-response range. A minimum of three experiments were made
    • (1991) Anal. Biochem. , vol.194 , pp. 302
    • Blakely, R.D.1    Clark, J.A.2    Rudnick, G.3    Amara, S.G.4
  • 15
    • 33847743994 scopus 로고    scopus 로고
    • note
    • This is in contrast to the piperazine series described in Ref. 6, in which a 2-substituent delivers potent dual 5-HT and NA reuptake inhibition.
  • 16
    • 33847692509 scopus 로고    scopus 로고
    • note
    • The human hepatocyte assay was able to accurately determine half-lives of up to 240 min, whereas the maximum measurable half-life in human liver microsomes was 120 min.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.