کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365691 | 981570 | 2007 | 4 صفحه PDF | دانلود رایگان |

Novel NR2B antagonists with an amide tether were found by an approach to avoid pharmacophoric similarity to dofetilide. Structure–activity relationship investigation led to N-[cis-4-hydroxy-4-(5-hydroxypyridin-2-yl)cyclohexyl]-3-henylpropanamide 14e as an orally active NR2B-subtype selective N-methyl-d-aspartate (NMDA) receptor antagonist with very weak HERG (human ether-a-go-go related gene) binding (IC50 > 30 μM). This compound exhibited potent in vivo anti-allodynic activity in the mouse partial sciatic nerve ligation (PSL) model (minimum effective dose = 10 mg/kg, po).
Structure–activity relationship investigation led to N-[cis-4-hydroxy-4-(5-hydroxypyridin-2-yl)cyclohexyl]-3-phenylpropanamide 14e as an orally active NR2B-subtype selective N-methyl-d-aspartate (NMDA) receptor antagonist with very weak HERG binding (IC50 > 30 μM).Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 20, 15 October 2007, Pages 5533–5536