Metabolites of orally active NO-independent pyrazolopyridine stimulators of soluble guanylate cyclase

被引:64
作者
Straub, A
Benet-Buckholz, J
Fröde, R
Kern, A
Kohlsdorfer, C
Schmitt, P
Schwarz, T
Siefert, HM
Stasch, JP
机构
[1] Bayer AG, Pharma Res Ctr, Inst Med Chem, D-42096 Wuppertal, Germany
[2] Bayer AG, Cent Res, Div Struct Res, D-51368 Leverkusen, Germany
[3] Bayer AG, Pharma Res Ctr, Dept Drug Metab & Isotope Chem, D-42096 Wuppertal, Germany
[4] Bayer AG, Pharma Res Ctr, Dept Preclin Pharmacokinet, D-42096 Wuppertal, Germany
[5] Bayer AG, Pharma Res Ctr, Inst Cardiovasc Res, D-42096 Wuppertal, Germany
关键词
D O I
10.1016/S0968-0896(02)00034-2
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The pyrazolopyridine stimulators of soluble guanylate cyclase BAY 41-2272 and 41-8543 were oxidised in rats and dogs at their 5-pyrimidinyl-cyclopropyl and -morpholino residue. These metabolites activate the soluble guanylate cyclase, induce vaso-elaxation and thereby may contribute to the in vivo activity of BAY 41-2272 and BAY 41-8543. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1711 / 1717
页数:7
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