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[(35)S]GTPγS autoradiography for studies of opioid receptor functionality
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences.
2015 (English)In: Methods in Molecular Biology, ISSN 1064-3745, E-ISSN 1940-6029, Vol. 1230, 169-176 p.Article in journal (Refereed) Published
Abstract [en]

The opioid receptors have been an interesting target for the drug industry for decades. These receptors were pharmacologically characterized in the 1970s and several drugs and peptides have emerged over the years. In 2012, the crystal structures were also demonstrated, with new data on the receptor sites, and thus new possibilities will appear. The role of opioids in the brain has attracted considerable interest in several diseases, especially pain and drug dependence. The opioid receptors are G-protein-coupled receptors (GPCR) that are Gi-coupled which make them suitable for studying the receptor functionality. The [(35)S]GTPγS autoradiography assay is a good option that has the benefit of generating both anatomical and functional data in the area of interest. It is based on the first step of the signaling mechanism of GPCRs. When a ligand binds to the receptor GTP will replace GDP on the α-subunit of the G protein, leading to a dissociation of the βγ-subunit. These subunits will start a cascade of second messengers and subsequently a physiological response.

Place, publisher, year, edition, pages
2015. Vol. 1230, 169-176 p.
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Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-241196DOI: 10.1007/978-1-4939-1708-2_13PubMedID: 25293324OAI: oai:DiVA.org:uu-241196DiVA: diva2:777784
Available from: 2015-01-08 Created: 2015-01-08 Last updated: 2018-01-11Bibliographically approved

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Grönbladh, AlfhildHallberg, Mathias

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