PT - JOURNAL ARTICLE AU - Sven Sihver AU - Wiebke Sihver AU - Mats Bergström AU - A. Urban Höglund AU - Pernilla Sjöberg AU - Bengt Långström AU - Yasuyoshi Watanabe TI - Quantitative Autoradiography with Short-Lived Positron Emission Tomography Tracers: A Study on Muscarinic Acetylcholine Receptors with<em>N</em>-[<sup>11</sup>C]methyl-4-piperidylbenzilate DP - 1999 Aug 01 TA - Journal of Pharmacology and Experimental Therapeutics PG - 917--922 VI - 290 IP - 2 4099 - http://jpet.aspetjournals.org/content/290/2/917.short 4100 - http://jpet.aspetjournals.org/content/290/2/917.full SO - J Pharmacol Exp Ther1999 Aug 01; 290 AB - The present work demonstrates quantitative autoradiography by using positron emission tomography tracers and storage phosphorimaging plates. The uptake and association of [11C]N-methyl-4-piperidylbenzilate was measured in rat brain tissue cryosections of various thicknesses. The signal increased with increasing section thickness, but only in 10-μm-thick sections did the binding reach the steady state during a 50-min observation time. This violation of the equilibrium condition, potentially combined with perfusion limitations, leads to erroneous increased binding-site density and decreased affinity in the 25- and 50-μm-thick sections. For better imaging of receptor distribution it is reasonable to use thicker sections. For quantitative analysis of receptor-binding parameters, the specific properties of ligands at different thicknesses of cryosections need to be considered. Evidence is provided that the nonselective muscarinic antagonistN-methyl-4-piperidylbenzilate binds preferentially to the M4 subtype of muscarinic acetylcholine receptors. The American Society for Pharmacology and Experimental Therapeutics