Receptor Subtype | Brain Regional Localization | BZD Pharmacology Classic BZDs/Zolpidem | Pharmacological Effects Mediated by Classic BZDs in the CNS |
---|---|---|---|
α1βγ2 | Cerebral cortex (throughout), substantia nigra pars reticulata, hippocampus (DG, CA1-CA2), cerebellum | +++/+++ | Sedation, anterograde amnesia, antimyoclonic and anticonvulsive activity, muscle relaxation |
α2βγ2 | Cerebral cortex, hippocampus (throughout) | +++/++ | Anxiolysis, muscle relaxation |
α3βγ2 | Temporal neocortex, motor cortex IV–VI, substantia nigra, hippocampus (CA1, subiculum, DG) | +++/++ | Anxiolysis, muscle relaxation |
α4βγ2 | Cerebral cortex, thalamus | −/− | − |
α4βδ | Motor cortex III–IV, hippocampus (DG), thalamus, cerebellar granule cells | −/− | − |
α5βγ2 | Motor cortex IV–VI, hippocampus (CA1-CA3, DG) | +++/+ | Memory impairment, muscle relaxation |
α6βγ2 | Cerebellar granule cells | −/− | −/− |
α6βδ | Cerebellar granule cells | −/− | − |
DG, dentate gyrus; +++, high sensitivity; ++, intermediate sensitivity; +, very low sensitivity; −, insensitive.