125I] 3-quinuclidinyl 4-iodobenzilate: a high affinity, high specific activity radioligand for the M1 and M2-acetylcholine receptors |
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| Authors: | R E Gibson W J Rzeszotarski E M Jagoda B E Francis R C Reba W C Eckelman |
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| Affiliation: | George Washington University Medical Center, Section of Radiopharmaceutical Chemistry, Walter G. Ross Hall, 2300 Eye St., N.W., Washington, D.C. 20037, USA |
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| Abstract: | We have prepared a radioiodinated ligand which binds with high affinity to the muscarinic acetylcholine receptor (m-AChR). A derivative of 3-quinuclidinyl benzilate, [125I] labeled (R) 1-aza-bicyclo(2.2.2)oct-3-yl (R,S)-alpha-hydroxy-alpha-(4-[125I]iodophenyl)phenyl acetate (4- IQNB ) exhibits an affinity for the m-AChR from corpus striatum higher than that of (R) [3H] QNB. Additionally, [125I] 4- IQNB exhibits receptor selectivity for the M1 receptor since the affinity for the receptor from dog and rat heart is lower than that using dog or rat corpus striatum. |
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| Keywords: | Send Correspondence to: Section of Radiopharmaceutical Chemistry Walter G. Ross Hall Room 662 2300 Eye St. N.W. Washington D.C. 20037 USA |
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