Channelpedia

PubMed 20801039


Referenced in: none

Automatically associated channels: Kv11.1



Title: 9-Dihydroerythromycins as non-antibiotic motilin receptor agonists.

Authors: Yaoquan Liu, Yong Li, Yue Chen, Hao Zheng, Mark Claypool, David C Myles, Christopher W Carreras

Journal, date & volume: Bioorg. Med. Chem. Lett., 2010 Oct 1 , 20, 5658-61

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/20801039


Abstract
A series of 9-dihydroerythromycin A and B analogues with modification of the desosamine nitrogen have been synthesized and screened for motilin agonist activity, antibiotic activity, tachyphylaxis and hERG channel current inhibition. Small alkyl groups resulted in the potency while compounds with a primary or secondary amine resulted in the low motilin agonist potency. Several compounds were identified as non-antibiotic motilin receptor agonists with minimal tachyphylaxis and low hERG interaction.