Autoradiography of 2‐[18F]F‐A‐85380 on nicotinic acetylcholine receptors in the porcine brain in vitro
Abstract
Noninvasive molecular imaging of subtypes of neuronal nicotinic acetylcholine receptors (nAChRs) will provide information on the role of these receptors in neurodegenerative diseases. The binding of the positron emission tomography ligand 2‐[18 F]F‐A‐85380 to nAChRs was investigated in the porcine brain by quantitative autoradiography in vitro. The high‐affinity binding of 2‐[18 F]F‐A‐85380 to each of the investigated 12 brain areas was saturable and apparently monophasic (e.g., apparent KD value of 1.72 nM in the thalamus). The highest density of specific binding sites was observed in the thalamus (1,158 fmol/mg protein), and the lowest density was measured in the cerebellar gray matter (11 fmol/mg protein). An attempt to assess nAChR subtype specificity of 2‐[18 F]F‐A‐85380 was made by competitive autoradiography. Binding of 2‐[18 F]F‐A‐85380 coincubated with 2‐F‐A‐85380, epibatidine, cytisine, or methyllycaconitine, respectively, indicated a specificity of 2‐[18 F]F‐A‐85380 to β2‐containing nAChRs in the porcine brain. The autoradiographic data confirmed the suitability of swine as a model for the evaluation of radioligands designed for imaging of nAChR subtypes in the living brain. Synapse 59:201–210, 2006. © 2005 Wiley‐Liss, Inc.
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[3H]2-FA-85380 binds selectively to β2-containing nAChRs.
“In contrast, [3H]2-FA-85380 binds selectively to b2-containing nAChRs (Brody et al, 2006; Deuther-Conrad et al, 2006; Vaupel et al, 2005).”
From Divergent Functional Effects of Sazetidine-A and Varenicline During Nicotine Withdrawal (2013) · cites this paper as Deuther-Conrad et al, 2006
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Self-citation
- Authors
- Deuther‐Conrad, W., Wevers, A., Becker, G., Schildan, A., Patt, M., Sabri, O., Steinbach, J., & Brust, P.
- Affiliations
- University of Cologne (DE)
- University Hospital Leipzig (DE)
- Corresponding author
- Deuther‐Conrad, Winnie
- ORCID
- Venue
- Synapse
- Publisher
- Wiley
- Published
- 2005-12-29
- Volume
- 59
- Issue
- 4
- Pages
- 201-210
- ISSN
- 0887-4476 (ISSN-L)
- 1098-2396
- OpenAlex
- W2004529323
- Cited by
- 12
- References
- 51
- Citations by year
- 2020: 1 · 2014: 2 · 2013: 2
- FWCI
- 0.63
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Synapse (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Pharmacological Receptor Mechanisms and Effects
- Keywords
- nicotinic acetylcholine receptors, receptor binding affinity, receptor density, thalamus, competitive binding, epibatidine, methyllycaconitine, cytisine, neurodegenerative diseases
- MeSH terms
- Animals, Autoradiography, Azetidines, Binding, Competitive, Brain, Female, Humans, Immunohistochemistry, Organ Culture Techniques, Pyridines, Receptors, Nicotinic, Swine, Positron-Emission Tomography
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