Li Fu-Nan, Kim Nam-Jung, Nam Yeon-Hee, Kim Seung-Hee, Seo Seung-Yong, Jeong Yeon-Su, Kim Sun-Young, Park Young-Ho, Suh Young-Ger
College of Pharmacy, Seoul National University, Seoul 151-742, Korea.
Arch Pharm Res. 2009 Sep;32(9):1201-10. doi: 10.1007/s12272-009-1903-9. Epub 2009 Sep 26.
Synthesis and structure-activity relationship of N-benzyl-3-phenylpropanamides as transient receptor potential vanilloid 1 (TRPV1) antagonists are described. A variety of substituents such as halide, ester, nitro, and alkyl groups at 2 or 3-position of 4-(methylsulfonylamino) benzyl unit were examined. These compounds exhibited potent 45Ca2+ uptake inhibition in rat DRG neuron via TRPV1 blockade. Especially compound 28c, has been identified as a potent antagonist with IC50 of 38 nM.
描述了作为瞬时受体电位香草酸受体1（TRPV1）拮抗剂的N-苄基-3-苯基丙酰胺的合成及其构效关系。研究了4-（甲基磺酰氨基）苄基单元2-位或3-位的各种取代基，如卤化物、酯、硝基和烷基。这些化合物通过阻断TRPV1在大鼠背根神经节神经元中表现出有效的45Ca2+摄取抑制作用。特别是化合物28c，已被鉴定为一种有效的拮抗剂，IC50为38 nM。
