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Volumn 21, Issue 24, 2011, Pages 7281-7286

Nicotinic acids: Liver-targeted SCD inhibitors with preclinical anti-diabetic efficacy

Author keywords

Liver targeted; Nicotinic acid; OATP; SCD; Stearoyl coenzyme A

Indexed keywords

ACYL COENZYME A DESATURASE; ACYL COENZYME A DESATURASE INHIBITOR; ANTIDIABETIC AGENT; NICOTINIC ACID DERIVATIVE; ORGANIC ANION TRANSPORTER 1; ORGANIC ANION TRANSPORTER 1B1; ORGANIC ANION TRANSPORTER 1B2; ORGANIC ANION TRANSPORTER 1B3; OXYGENASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 81255199178     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.10.040     Document Type: Article
Times cited : (19)

References (51)
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    • 77952561929 scopus 로고    scopus 로고
    • For reviews of small molecule SCD inhibitors, see
    • For reviews of small molecule SCD inhibitors, see: P. Dobrzyn, and A. Dobrzyn Expert Opin. Ther. Patents 20 2010 849
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  • 36
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    • Recently, nicotinic acid (niacin) has been shown to be actively transported into human liver cells, see:, and references within
    • Recently, nicotinic acid (niacin) has been shown to be actively transported into human liver cells, see: H.M. Said, S.M. Nabokina, K. Balamurugan, Z.M. Mohammed, C. Urbina, and M.L. Kashyap Am. J. Physiol. Cell Physiol. 293 2007 C1773 and references within
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    • Said, H.M.1    Nabokina, S.M.2    Balamurugan, K.3    Mohammed, Z.M.4    Urbina, C.5    Kashyap, M.L.6
  • 38
    • 77956262443 scopus 로고    scopus 로고
    • Conditions which describe the fresh rat hepatocyte assay can be found in Ref. 9 A similar rat hepatocyte assay as the one utilized in this manuscript has recently been described, see
    • Conditions which describe the fresh rat hepatocyte assay can be found in Ref. 9 A similar rat hepatocyte assay as the one utilized in this manuscript has recently been described, see: C. Su, H. Gullberg1, H. Simko, M. Luthman, P.-O. Edlund, and T. Lundbäck J. Chromatogr. B 878 2010 2427
    • (2010) J. Chromatogr. B , vol.878 , pp. 2427
    • Su, C.1    Gullberg, H.2    Simko, H.3    Luthman, M.4    Edlund, P.-O.5    Lundbäck, T.6
  • 43
    • 84873100343 scopus 로고    scopus 로고
    • The liver:Harderian gland ratio was used as a measure of the degree of liver-targeting of a compound. For a more complete discussion, see Ref. 9
    • The liver:Harderian gland ratio was used as a measure of the degree of liver-targeting of a compound. For a more complete discussion, see Ref. 9
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    • 0000185537 scopus 로고    scopus 로고
    • Compound 10 also improved glucose clearance in eDIO mice following intraperitoneal challenge of glucose (42% and 82% improvement in glucose clearance at 30 and 100 mg/kg, respectively). This result suggests that the improvement in glucose clearance upon oral administration of inhibitor 10 is not due to effects on glucose absorption, see
    • Compound 10 also improved glucose clearance in eDIO mice following intraperitoneal challenge of glucose (42% and 82% improvement in glucose clearance at 30 and 100 mg/kg, respectively). This result suggests that the improvement in glucose clearance upon oral administration of inhibitor 10 is not due to effects on glucose absorption, see: R. Ling, M. Yoshida, and P.S. Mariano J. Org. Chem. 61 1996 4439
    • (1996) J. Org. Chem. , vol.61 , pp. 4439
    • Ling, R.1    Yoshida, M.2    Mariano, P.S.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.