具有组胺 H(3)受体和去甲肾上腺素转运体双重抑制作用的二芳基二胺类化合物和 4-(3-(甲氨基)-1-苯基丙基)-6-(2-(吡咯烷-1-基)乙氧基)萘-1-醇在疼痛中的疗效。
Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.
机构信息
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064-6100, United States.
出版信息
J Med Chem. 2010 Nov 11;53(21):7869-73. doi: 10.1021/jm100666w.
PMID:20945906
Abstract
A series of compounds was designed as dual inhibitors of the H(3) receptor and the norepinephrine transporter. Compound 5 (rNET K(i) = 14 nM; rH(3)R K(i) = 37 nM) was found to be efficacious in a rat model of osteoarthritic pain.
摘要
设计了一系列化合物作为 H(3)受体和去甲肾上腺素转运体的双重抑制剂。化合物 5（rNET K(i) = 14 nM；rH(3)R K(i) = 37 nM）在骨关节炎疼痛的大鼠模型中表现出疗效。
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