Bioorganic and Medicinal Chemistry Letters p. 1160 - 1162 (2007)
Update date:2022-08-04
Topics:
Mercer, Susan L.
Hassan, Hazem E.
Cunningham, Christopher W.
Eddington, Natalie D.
Coop, Andrew
P-Glycoprotein (P-gp) is an efflux transporter which is up-regulated at the blood-brain barrier in both morphine- and oxycodone-tolerant rats. Numerous studies have shown that many clinically employed opioid analgesics are substrates for P-gp, suggesting that up-regulation of P-gp may contribute to the development of central tolerance to opioids. The studies herein focus on the development of SAR for P-gp substrate activity in the meperidine series of compounds, and show that a meperidine analog of greater potency, N-phenylbutyl-N-normeperidine, has low activity as a P-gp substrate and has the potential to be utilized as a tool to study the contribution of P-gp to the development of central tolerance to opioids.
View MoreWuhan Better Organic Technology Inc.
Contact:13307163183
Address:Wuhan Economic&Technology Development Zone, Hubei
Laohekou huacheng Trade Co., Ltd.
Contact:+86-710-8360685
Address:No. 85, Beijing Road, Laohekou City, Hubei Province, China
Cerametek Materials(ShenZhen)Co., Ltd.
Contact:+86-755-2324.2554
Address:A3-#9, YongChuan Street, Suite 501
Hangzhou Donglou Bio-nutrient Co., Ltd.
Contact:+86-571-82225795,13967112289
Address:Louta Town, Xiaoshan,Hangzhou,Zhejiang
Zhejiang Rongkai Chemical Technology Co.,Ltd.
Contact:+86-578-8185786
Address:Shangjiang Industrial Zone,Suichang
Doi:10.1055/s-2001-15139
(2001)Doi:10.1002/jlcr.2580120106
(1976)Doi:10.1016/0040-4039(96)00301-2
(1996)Doi:10.1016/j.tet.2021.132129
(2021)Doi:10.1016/S0223-5234(03)00077-1
(2003)Doi:10.1016/S0040-4039(01)83135-X
(1977)