Chemical Biology and Drug Design p. 93 - 104 (2018)
Update date:2022-08-03
Topics:
Boulos, John F.
Jakubik, Jan
Boulos, John M.
Randakova, Alena
Momirov, Jelena
Muscarinic receptors are known to play important biological roles and are drug targets for several human diseases. In a pilot study, novel muscarinic antagonists were synthesized and used as chemical probes to obtain additional information of the muscarinic pharmacophore. The design of these ligands made use of current orthosteric and allosteric models of drug–receptor interactions together with chemical motifs known to achieve muscarinic receptor selectivity. This approach has led to the discovery of several non-competitive muscarinic ligands that strongly bind at a secondary receptor site. These compounds were found to be non-competitive antagonists that completely abolished carbachol activation in functional assays. Several of these compounds antagonized functional response to carbachol with great potency at M1 and M4 than at the rest of receptor subtypes.
View MoreShandong Topscience Biotech Co., Ltd.
Contact:0633-2619278
Address:No. 98 Lanshan West Road, Lanshan District, Rizhao, Shandong Province, P.R. of China
Contact:27-792-602929
Address:SIDNEY MUFAMADI STREET 009949 X44 0700 POLOKWANE,LIMPOPO
Contact:+86+21-58956006 15800617331
Address:402 Room, 150# Cailun Road, Zhangjiang high tech park, Shanghai
Contact:86-575-86132822,86-575-86085355
Address:No.418 Dadao West Road,Qixing Street,Xinchang, Zhejiang Province, China.
Chengdu Sino-Strong Pharmaceutical Co.,Ltd.
website:http://www.sino-strong.com.cn
Contact:+86-28-82666753
Address:459 West haike road,Cross-straits technological industry park, Wenjiang district,Chengdu, P.R.China
Doi:10.1016/0022-328X(93)80467-P
(1993)Doi:10.1002/psc.2589
(2014)Doi:10.1246/bcsj.67.455
(1994)Doi:10.1007/BF00846619
()Doi:10.1016/S1381-1169(99)00444-6
(2000)Doi:10.1021/jo402413g
(2014)