Abstract
The [18F] isotope-labelled CB1 inverse agonist 3 was elaborated and synthesized for positron emission tomography scanning studies. After immediate purification and calibration with its unlabeled counterpart, compound 3 was intravenously injected in mice and revealed that its distribution percentage in brain over 90-min scans among five region of interests, including brain, liver, heart, thigh muscle and kidney was lower than 1%, thus providing direct evidence to justify itself as a peripherally restricted CB1 antagonist.
Keywords:
Blood-brain barrier; Cannabinoid-1 antagonist; Peripherally restricted CB1 inverse agonist; Positron emission tomography.
Copyright © 2018. Published by Elsevier Ltd.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Cannabinoid Receptor Agonists / chemical synthesis
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Cannabinoid Receptor Agonists / chemistry
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Cannabinoid Receptor Agonists / pharmacokinetics
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Cannabinoid Receptor Agonists / pharmacology*
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Drug Inverse Agonism
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Fluorine Radioisotopes
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Isotope Labeling
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Male
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Mice, Inbred C57BL
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Positron-Emission Tomography / methods
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Pyrazoles / chemical synthesis
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Pyrazoles / chemistry
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Pyrazoles / pharmacokinetics
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Pyrazoles / pharmacology*
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Receptor, Cannabinoid, CB1 / agonists*
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Receptor, Cannabinoid, CB1 / antagonists & inhibitors
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry
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Sulfonamides / pharmacokinetics
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Sulfonamides / pharmacology*
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Thiophenes / chemistry
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Thiophenes / pharmacokinetics
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Thiophenes / pharmacology*
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Tissue Distribution
Substances
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Cannabinoid Receptor Agonists
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Fluorine Radioisotopes
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Pyrazoles
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Receptor, Cannabinoid, CB1
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Sulfonamides
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Thiophenes
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Fluorine-18