α4β2^* Nicotinic Cholinergic Receptor Target Engagement in Parkinson Disease Gait-Balance Disorders.

ABSTRACT:

Objective

Attentional deficits following degeneration of brain cholinergic systems contribute to gait-balance deficits in Parkinson disease (PD). As a step toward assessing whether α4β2* nicotinic acetylcholine receptor (nAChR) stimulation improves gait-balance function, we assessed target engagement of the α4β2* nAChR partial agonist varenicline.

Methods

Nondemented PD participants with cholinergic deficits were identified with [¹⁸ F]fluoroethoxybenzovesamicol positron emission tomography (PET). α4β2* nAChR occupancy after subacute oral varenicline treatment was measured with [¹⁸ F]flubatine PET. With a dose selected from the nAChR occupancy experiment, varenicline effects on gait, balance, and cognition were assessed in a double-masked placebo-control

SUBMITTER: Albin RL 

PROVIDER: S-EPMC9013471 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature