123I-labeled AM251: a radioiodinated ligand which binds in vivo to mouse brain cannabinoid CB1 receptors

Gatley, S.John; Gifford, Andrew N.; Volkow, Nora D.; Lan, Ruoxi; Makriyannis, Alexandros

doi:10.1016/0014-2999(96)00279-8

Cited by 256Cannabis and Cannabinoid ResearchRadiopharmaceutical Chemistry and ApplicationsNeuropeptides and Animal Physiology

123I-labeled AM251: a radioiodinated ligand which binds in vivo to mouse brain cannabinoid CB1 receptors

Gatley, S.John, Gifford, Andrew N., Volkow, Nora D., Lan, Ruoxi, Makriyannis, Alexandros·1996·European Journal of Pharmacology

DOI 10.1016/0014-2999(96)00279-8

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Abstract

We have investigated the binding of 123I-labeled N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methy l-1 H-pyrazole-3-carboxamide (AM251), an analog of the cannabinoid receptor antagonist SR141716A [N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-me thyl-1 H-pyrazole-3-carboxamide] in the mouse brain. Following intravenous injection, the peak whole-brain uptake of about 1% of the administered activity occurred at about 2 h. By 8 h radioactivity in brain had declined to about half its peak value. High-performance liquid chromatographic analysis showed that > 70% of radioactivity extracted from brain at 2 h was still present as [123I]AM251. Co-injection of SR141716A inhibited the in vivo brain binding of [123I]AM251 dose dependently. At 2 mg/kg, the highest dose that could be tested, inhibition was 50% at 2 h post-administration. The ED50 value calculated assuming that 2 mg/kg gave near-maximal inhibition was about 0.1 mg/kg. In contrast to the brain, radioactivity in other major organs (blood, liver, kidney, heart and lung) was little affected by SR141716A. The regional binding of [123I]AM251 in the brain was consistent with the published distribution of cannabinoid receptors in rat brain, in that the order was hippocampus, striatum > cerebellum > brain stem. delta 9-Tetrahydrocannabinol co-administered intravenously at 10 mg/kg, a dose which induced catalepsy and decreased locomotor activity, decreased the 2 h brain uptake of [123I]AM251 by 10%, but this was not significant (P = 0.08). In in vitro binding assays with mouse hippocampal membranes, tetrahydrocannabinol inhibited binding of [123I]AM251 with an IC50 value of about 700 nM, compared with about 0.2 nM for SR141716A.

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Characterization and distribution of binding sites for [3H]-SR 141716A, a selective brain (CB1) cannabinoid receptor antagonist, in rodent brain
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Self-citation

Authors: Gatley, S. J., Gifford, A. N., Volkow, N. D., Lan, R., & Makriyannis, A.
Affiliations: Brookhaven National Laboratory (US)
University of Connecticut (US)
Corresponding author: Gatley, S.John
ORCID: Volkow, Nora D.
Makriyannis, Alexandros
Venue: European Journal of Pharmacology
Publisher: Elsevier BV
Published: 1996-07
Volume: 307
Issue: 3
Pages: 331-338
ISSN: 0014-2999 (ISSN-L)
DOI: 10.1016/0014-2999(96)00279-8
OpenAlex: W1979829009
Cited by: 252
References: 15
Citations by year: 2026: 2 · 2025: 3 · 2024: 2 · 2023: 3 · 2022: 1 · 2021: 4 · 2020: 3 · 2019: 2 · 2018: 7 · 2017: 1 · 2016: 8 · 2015: 12 · 2014: 8 · 2013: 13 · 2012: 11
FWCI: 1.49
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: European Journal of Pharmacology (publishedVersion)
PubMed (publishedVersion)
Funders: U.S. Department of Energy
Sanofi
National Institute on Drug Abuse (DA-06278, R01DA006278, DA07515, DA-03801)
Brookhaven National Laboratory
Topics: Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
Keywords: CB1 receptor, radioiodination, SR141716A, radioligand binding, brain receptor distribution, tetrahydrocannabinol, delta-9-tetrahydrocannabinol, hippocampus, striatum, cerebellum, brainstem
MeSH terms: Rimonabant, Animals, Brain, Cell Membrane, Chromatography, High Pressure Liquid, Hippocampus, Iodine Radioisotopes, Isotope Labeling, Male, Mice, Inbred Strains, Motor Activity, Piperidines, Protein Binding, Pyrazoles, Radioligand Assay, Receptors, Drug, Dronabinol, Tissue Distribution, Receptors, Cannabinoid, Mice

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123I-labeled AM251: a radioiodinated ligand which binds in vivo to mouse brain cannabinoid CB1 receptors

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