title: Phosphatidylinositol 4,5-bisphosphate induced flunitrazepam sensitive-GABAA receptor increase in synaptosomes from chick forebrain.
abstract: The flunitrazepam sensitive-GABA(A) receptor density was increased by cytochalasins C and D at 37 degrees C suggesting that microfilament depolymerization induces exposure to the radioligand of a GABA(A) receptor in synaptosomes (Pharm Biochem Behav 72 (2002) 497). Similarly, phosphatidylinositol-4,5-bisphosphate (1-5 microM), but not a mixture of phospholipids, induced an increase of GABA(A) receptors in synaptosomes. Furthermore, N-ethyl maleimide, an inactivator of the sensitive fusion protein, which interacts with GABA(A) receptor, abolished the receptor increase induced by phosphatidylinositol-4,5-bisphosphate. Together, the results suggest that phosphatidylinositol-4,5-bisphosphate, acts via microfilament depolymerization increasing the binding of the radioligand to receptors possibly by modulation of their interaction with proteins involved in trafficking and docking mechanisms.
authors.affiliation: Cátedra de Química Biológica, Departamento de Química, Facultad de Ciencias Exactas Físicas y Naturales, Universidad Nacional de Córdoba. Av, Vélez Sarsfield 1611, Córdoba, Argentina. aarce@efn.uncor.edu
authors.forename: Mariana Paula
authors.initials: MP
authors.lastname: Cid
authors.forename: Nancy Alicia
authors.initials: NA
authors.lastname: Salvatierra
authors.forename: Augusto
authors.initials: A
authors.lastname: Arce
mesh_terms: D000818:Animals; D002645:Chickens / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005033:Ethylmaleimide / Q000494:pharmacology; D005445:Flunitrazepam / Q000494:pharmacology*; D018757:GABA Modulators / Q000494:pharmacology*; D066298:In Vitro Techniques; D007700:Kinetics; D019269:Phosphatidylinositol 4,5-Diphosphate / Q000494:pharmacology*; D016548:Prosencephalon / Q000187:drug effects / Q000378:metabolism*; D011869:Radioligand Assay; D011963:Receptors, GABA-A / Q000187:drug effects*; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism*
chemical_list: D004791:Enzyme Inhibitors; D018757:GABA Modulators; D019269:Phosphatidylinositol 4,5-Diphosphate; D011963:Receptors, GABA-A; D005445:Flunitrazepam; D005033:Ethylmaleimide