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Radioiodinated D-(+)-N1-ethyl-2-iodolysergic acid diethylamide: A ligand for in vitro and in vivo studies of serotonin receptors
Abstract
Radioiodinated D-(+)-N1-ethyl-2-iodolysergic acid diethylamide ([125I]-EIL) has been evaluated as a ligand for in vitro and in vivo studies of cerebral serotonin 5-HT2 receptors. [125I]-EIL exhibited high affinity (KD = 209 pM) for 5-HT2 receptors with a high degree of specific binding (80-95%) in membranes from rat prefrontal cortex. The regional distribution of [125I]-EIL binding in vivo to seven areas of mouse brain correlated significantly (Rs = 0.93) with known densities of 5-HT2 receptors. In vivo specificity, defined by tissue to cerebellum radioactivity ratios, reached a maximum for frontal cortex at 6 hr (21.2) and persisted through 16 hr (8.8). Ketanserin, a 5-HT2 receptor antagonist, fully inhibited binding in a dose dependent fashion in all brain regions except cerebellum. By contrast, blockers for dopamine D2, alpha- or beta-adrenergic receptors did not significantly inhibit radioligand binding in any region. [125I]-EIL selectively labels 5-HT2 receptors in vivo with the highest specificity of any serotonergic ligand reported to date, indicating that [123I]-EIL should prove applicable to single photon emission computed tomography studies in living brain.
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[125I]-EIL had very high affinity for 5HT2A receptors in rat cerebral cortex, with a KD of 0.2 nM.
“It had very high affinity for 5HT2A receptors in rat cerebral cortex, with a dissociation constant (KD) of 0.2 nM [69].”
From Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans. (2021) · cites this paper as [69]
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Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans.
Cumming, P., Scheidegger, M., Dornbierer, D., Palner, M., Quednow, B. B., & Martin-Soelch, C. (2021) · Molecules · doi:10.3390/molecules26092451 · Cited by 43
Metadata
- Authors
- Lever, J. R., Scheffel, U. A., Musachio, J. L., Stathis, M., & Wagner, H. N.
- Affiliations
- Johns Hopkins University (US)
- Corresponding author
- Lever, John R.
- Venue
- Life Sciences
- Publisher
- Elsevier BV
- Published
- 1991-01
- Volume
- 48
- Issue
- 15
- Pages
- PL73-PL78
- ISSN
- 0024-3205 (ISSN-L)
- OpenAlex
- W1971853271
- Cited by
- 13
- References
- 0
- Citations by year
- 2021: 1 · 2016: 1 · 2015: 2
- FWCI
- 0.39
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Life Sciences (publishedVersion)
- PubMed (publishedVersion)
- Funders
- U.S. Department of Health and Human Services
- National Institutes of Health (1f31da005428-01, 5p01ca032845-39)
- National Institute on Drug Abuse (1F31DA05428)
- National Cancer Institute (CA 32845)
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Keywords
- 5-HT2 receptor, radioligands, receptor binding affinity, ketanserin, prefrontal cortex, neuroimaging, single photon emission computed tomography
- MeSH terms
- Animals, Brain, Brain Mapping, Ligands, Lysergic Acid Diethylamide, Radioligand Assay, Receptors, Adrenergic, Receptors, Dopamine, Receptors, Serotonin, Mice, Rats
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