The α1-Adrenoceptor Is Inactivated by Alterations in Membrane Phospholipids
The influence of the membrane environment on the α1-adrenoceptor has been investigated by examining the effect of phospholipase digestion on the binding of [3H]prazosin to aortic and hepatic membranes. Membrane digestion by phospholipase A2 and phospholipase C was found to markedly reduce prazosin binding to the α1-adrenoceptor whereas phospholipase D had comparatively little effect. In addition, there were differences between membrane preparations since the aortic α1-adrenoceptor was less sensitive to phospholipase A2 and phospholipase C than the hepatic receptor. The results support a major role for hydrophobic groups and the negatively charged, hydrophilic phosphate moiety of phospholipids in the interaction between prazosin and the α1-adrenoceptor.
Shreeve, S. M.; and Valliere, Julia E.. 1992. The α1-Adrenoceptor Is Inactivated by Alterations in Membrane Phospholipids. European Journal of Pharmacology: Molecular Pharmacology. Vol.226(1). 29-33. https://doi.org/10.1016/0922-4106(92)90079-B PMID: 1327840 ISSN: 0922-4106