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[125I] 3-quinuclidinyl 4-iodobenzilate: a high affinity, high specific activity radioligand for the M1 and M2-acetylcholine receptors.

Authors
  • Gibson, R E
  • Rzeszotarski, W J
  • Jagoda, E M
  • Francis, B E
  • Reba, R C
  • Eckelman, W C
Type
Published Article
Journal
Life Sciences
Publisher
Elsevier
Publication Date
Jun 04, 1984
Volume
34
Issue
23
Pages
2287–2296
Identifiers
PMID: 6727565
Source
Medline
License
Unknown

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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