Paila, Yamuna Devi ; Pucadyil, Thomas J. ; Chattopadhyay, Amitabha (2005) The cholesterol-complexing agent digitonin modulates ligand binding of the bovine hippocampal serotonin1A receptor Molecular Membrane Biology, 22 (3). pp. 241-249. ISSN 0968-7688
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Official URL: http://informahealthcare.com/doi/abs/10.1080/09687...
Related URL: http://dx.doi.org/10.1080/09687860500093453
Abstract
The serotonin1A (5-HT1A) receptor is an important member of the superfamily of seven transmembrane domain G-protein-coupled receptors. We have examined the modulatory role of cholesterol on the ligand binding of the bovine hippocampal 5-HT1A receptor by cholesterol complexation in native membranes using digitonin. Complexation of cholesterol from bovine hippocampal membranes using digitonin results in a concentration-dependent reduction in specific binding of the agonist 8-OH-DPAT and antagonist p-MPPF to 5-HT1A receptors. The corresponding changes in membrane order were monitored by analysis of fluorescence polarization data of the membrane depth-specific probes, DPH and TMA-DPH. Taken together, our results point out the important role of membrane cholesterol in maintaining the function of the 5-HT1A receptor. An important aspect of these results is that non-availability of free cholesterol in the membrane due to complexation with digitonin rather than physical depletion is sufficient to significantly reduce the 5-HT1A receptor function. These results provide a comprehensive understanding of the effects of the sterol-complexing agent digitonin in particular, and the role of membrane cholesterol in general, on the 5-HT1A receptor function.
Item Type: | Article |
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Source: | Copyright of this article belongs to Informa Healthcare. |
Keywords: | 5-HT1A Receptor; Cholesterol; Digitonin; Fluorescence Polarization |
ID Code: | 7340 |
Deposited On: | 25 Oct 2010 11:46 |
Last Modified: | 16 May 2016 17:34 |
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