Abstract
The detection of muscarinic receptor binding sites is a crucial step in many experimental conditions. Although in peripheral tissue, the radioligand binding (see appropriate chapter) allows to obtain well-defined receptor characteristic, and also is usable in some central nervous system regions, when trying to determine receptor binding in central nervous system regions with low density or with infinitesimally small receptor changes, the receptor autoradiography is a better method. The development of this method made important progress, and some different modes (phosphor imaging) are used nowadays. Here, we describe muscarinic receptor detection using different radioligands: [3H]-QNB, [3H]-NMS, [3H]-pirenzepine, and [3H]-AFDX-384. Specific attention is paid to the detection of subtypes of muscarinic receptors and the limits of the method are emphasized.
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Abbreviations
- 3H-QNB:
-
3H-quinuclidinyl benzilate, 3H-1-azabicyclo[2.2.2]oct-3-yl 2-hydroxy-2, 2-diphenylacetate
- 3H-NMS:
-
3H-N-methyl-scopolamine, 3H-(1R,2S,4R,5S,7R)-{[(2R)-3-hydroxy-2-phenylpropanoyl]oxy}s[19]-9,9-dimethyl-3-oxa-9-azoniatricyclo [3.3.1.02,4]nonane
- 3H-pirenzepine:
-
3H-11-[(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
- 3H-AFDX-384:
-
3H-N-(2-[(2R)-2-[(dipropylamino)methyl]piperidin-1-yl]ethyl)-6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide
- RT:
-
Room temperature
- MRs:
-
Muscarinic receptors
- GPCRs:
-
G protein-coupled receptors
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Acknowledgments
The research on this topic was supported by grant GAUK 328314 from Grant Agency of Charles University and by projects PRVOUK P25/1LF and PRVOUK P35/1LF.
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Farar, V., Myslivecek, J. (2016). Autoradiography Assessment of Muscarinic Receptors in the Central Nervous System. In: Myslivecek, J., Jakubik, J. (eds) Muscarinic Receptor: From Structure to Animal Models. Neuromethods, vol 107. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-2858-3_9
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DOI: https://doi.org/10.1007/978-1-4939-2858-3_9
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