Journal of Medicinal Chemistry p. 2262 - 2265 (1994)
Update date:2022-09-26
Topics:
Zimmerman, Dennis M.
Gidda, Jaswant S.
Cantrell, Buddy E.
Schoepp, Darryle D.
Johnson, Bryan G.
Leander, J. David
Structure-activity relationship studies were pursued within N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines in an effort to discover a peripherally selective opioid antagonist with high activity following systemic administration.Altering the size and the polarity of the N-substituent led to the discovery of 3 (LY246736).Compound 3 has high affinity for opioid receptors (Ki = 0.77, 40, and 4.4 nM for μ, κ, and δ receptors, respectively).It is a potent μ receptor antagonist following parenteral and oral administration and distributes selectively (>200-fold selectivity) to peripheral receptors.Thus, 3 has properties suitable for the clinical investigation of μ opioid receptor involvement in GI motility disorders.
View MoreSICHUAN ZHONGBANG NEW MATERIAL CO., LTD
website:http://www.zhongbangst.com
Contact:86-830-2585019
Address:sichuan,china
Zhuzhou Farshine Chemical Industry Co., Ltd
Contact:0086-731-28482786
Address:No. 1,Shui Xian Road, He Tang Dictrict,Hunan-412000,China
Rizhao Lanxing Chemical Indusrial Co.,Ltd
Contact:86-633-2616708
Address:NO.15 West road Shenglan, Lanshan district, Rizhao City
Shenzhen Sunrising Industry Co., ltd.
Contact:+86 755 86571158 / 86571159 / 86571160
Address:2108 ZHENYE INT. BUSINESS CENTER,NO.3101-90 QIANHAI RD, NANSHAN,SHENZHEN, CHINA
MTT Pharma & Bio-technology Co.,Ltd
Contact:+86-21-58407925
Address:Room2019, Building C, Tomson Center, No.158, Zhang Yang Road, Shanghai, China
Doi:10.1016/S0040-4039(00)74721-6
(1992)Doi:10.1016/j.dyepig.2010.01.016
(2010)Doi:10.1007/s10870-013-0450-x
(2013)Doi:10.1016/j.jphotochem.2012.06.009
(2012)Doi:10.1055/s-0034-1379933
(2015)Doi:10.1016/S0040-4039(00)60567-1
(1993)