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- Title
Quantification of smoking-induced occupancy of beta2-nicotinic acetylcholine receptors: estimation of nondisplaceable binding.
- Authors
Esterlis, Irina; Cosgrove, Kelly P; Batis, Jeffery C; Bois, Frederic; Stiklus, Stephanie M; Perkins, Evgenia; Seibyl, John P; Carson, Richard E; Staley, Julie K
- Abstract
5-(123)I-iodo-85380 ((123)I-5-IA) is used to quantitate high-affinity nicotinic acetylcholine receptors (beta(2)-nAChRs) on human SPECT scans. The primary outcome measure is V(T)/f(P), the ratio at equilibrium between total tissue concentration (free, nonspecifically bound, and specifically bound) and the free plasma concentration. Nondisplaceable uptake (free plus nonspecific) of (123)I-5-IA has not been measured in human subjects. Nicotine has high affinity for beta(2)*-nAChRs (nAChRs containing the beta(2)* subunit, for which * represents other subunits that may also be part of the receptor) and displaces specifically bound (123)I-5-IA. In this study, we measured nicotine occupancy and nondisplaceable binding in healthy smokers after they had smoked to satiety.
- Publication
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2010, Vol 51, Issue 8, p1226
- ISSN
1535-5667
- Publication type
Journal Article
- DOI
10.2967/jnumed.109.072447