Modulatory effects of phosphatidylserine on the binding of muscarinic cholinergic receptor ligands. Studies in vitro and in vivo.

摘要: The modulation of the binding muscarinic cholinergic receptor ligands by phosphatidylserine purified from bovine cerebral cortex (BC-PS) was examined in vitro and vivo. enrichment cortical synaptosomal membranes with BC-PS, using a fusion technique, produced concentration-dependent decrease affinity (increase K d ) [3H]quinuclidinyl benzylate (3H-QNB) specific to acetylcholine receptors (mAChR), without changes their maximal number (Bmax). Similar results were observed when [3H]oxotremorine (3H-OXO) used label high subpopulation mAChR. On other hand, preincubation BC-PS liposomes nonoptimum condition (at pH 7.4) did not alter properties both radioligands. Fusion experiments pure preparation spinal cord revealed similar decrement of3H-QNB binding. Five day’s intraperitoneal (i.p.) administration 15 mg/kg rats increased sites for3H-OXO. Scatchard analysis no apparent dissociation constant. This modification is selective relation neural structure studied. Thus, treatment modify3H-OXO hippocampal formation cerebellum. In contrast, parallel antagonist3H-QNB showed alteration i.p. mg/kg/d phosphatidylcholine (BC-PC) quite those obtained BC-PS. These indicate that mAChR are under modulatory action (PS) (PC), suggest this endogenous phospholipids may play regulatory role on possible implications these findings effects PC or PS neurological disorders involving central functions discussed.