Ontology highlight
ABSTRACT:
SUBMITTER: Govind AP
PROVIDER: S-EPMC5546804 | biostudies-other | 2017 Jul
REPOSITORIES: biostudies-other
Govind Anitha P AP Vallejo Yolanda F YF Stolz Jacob R JR Yan Jing-Zhi JZ Swanson Geoffrey T GT Green William N WN
eLife 20170718
To better understand smoking cessation, we examined the actions of varenicline (Chantix) during long-term nicotine exposure. Varenicline reduced nicotine upregulation of α4β2-type nicotinic receptors (α4β2Rs) in live cells and neurons, but not for membrane preparations. Effects on upregulation depended on intracellular pH homeostasis and were not observed if acidic pH in intracellular compartments was neutralized. Varenicline was trapped as a weak base in acidic compartments and slowly released, ...[more]