Abstract:
:Binding of [3H]ethynylbicycloorthobenzoate ([3H]EBOB) to the gamma-aminobutyric acid type A (GABAA) receptor of cultured cerebellar granule neurons is inhibited by GABA, muscimol and 3-aminopropanesulfonic acid with IC50 values of 69-250 nM. Sensitivity to these GABA mimetics is lower by 3-4-fold for cerebellum and 10-20-fold for cerebral cortex, midbrain, and pons and medulla, a differential sensitivity by brain region and cell type consistent with earlier findings using tert-[35S]butylbicyclophosphorothionate and GABA. In contrast, the inhibitory potencies of two chloride channel blockers, alpha-endosulfan and picrotoxinin, do not differ in these assays. The hypothesis that this pharmacological profile is conferred by the alpha 6 subunit specific to cerebellar granule cells is supported by the finding that forskolin (which downregulates the alpha 6 subunit) but not the inactive dideoxyforskolin markedly decreases the sensitivity of [3H]EBOB binding to GABA without affecting inhibition by alpha-endosulfan.
journal_name
Neurosci Lettjournal_title
Neuroscience lettersauthors
Huang J,Casida JEdoi
10.1016/s0304-3940(97)00206-1subject
Has Abstractpub_date
1997-04-04 00:00:00pages
85-8issue
2eissn
0304-3940issn
1872-7972pii
S0304-3940(97)00206-1journal_volume
225pub_type
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