Department of Pharmaceutical Chemistry, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.
Bioorg Med Chem. 2010 Feb;18(3):1204-12. doi: 10.1016/j.bmc.2009.12.039. Epub 2009 Dec 21.
In order to investigate the molecular features involved in sigma receptors (sigma-Rs) binding, new compounds based on arylalkylaminoalcoholic, arylalkenyl- and arylalkylaminic scaffolds were synthesized and their affinity towards sigma(1)- and sigma(2)-Rs subtypes was evaluated. The most promising compounds were also screened for their affinity at micro-opioid, delta-opioid and kappa-opioid receptors. Biological results are herein presented and discussed.
为了研究涉及 sigma 受体(sigma-Rs)结合的分子特征,合成了基于芳基烷基氨基醇、芳烯基和芳基烷基胺骨架的新化合物,并评估了它们对 sigma(1)-和 sigma(2)-Rs 亚型的亲和力。最有前途的化合物也被筛选其对微阿片受体、德尔塔阿片受体和kappa 阿片受体的亲和力。本文呈现并讨论了生物学结果。