Gustav Akk has a background in biophysics and pharmacology of ion channels. His current work focuses on the mechanisms of activation and modulation of transmitter-gated ion channels, particularly the GABAA receptor, under physiological and clinical conditions. The GABAA receptor is the major ionotropic inhibitory ion channel in the brain and an important component in the maintenance of excitato...

There is little doubt regarding the therapeutic possibilities of modulation of GABAA receptor function as exemplified by the clinical utility of benzodiazepines for half a century. The emerging understanding of the role of different GABAA receptor subtypes in mediating different physiological functions and pathological processes continues to offer opportunities for novel therapeutics. However, ...

Dohi, Akiko, ERK/MAPK Pathway Regulation of GABAA Receptor Function. Doctor of Philosophy (Pharmacology and Neuroscience), December, 2009, pp116, 23 illustrations, 6 supplemental illustrations, bibliography, 158 titles. GABAA receptor is a ligand-gated ion channel that conducts negatively charged chloride ions. Influx of this ion leads to hyperpolarization of neurons; thus, suppression of the n...

Polyclonal antibodies were raised to synthetic amino acid sequences of the bovine GABAA receptor qand as-subunits and purified by affinity chromatography on a column coupled with the respective peptide. Anti-peptide %(41&424) and anti-peptide aJ459-467) antibodies immunoprecipitated GABAA receptors and recognized a protein of 53 kDa (PJ and 59 kDa (P& respectively, in Western blots of GABAA rec...

objective(s):the mechanism of hypothermia action of acetaminophen (apap) remains unclear even 125 years after its synthesis. acetaminophen produces hypothermia. the mechanism of this reduction in core body temperature is not clear but evidence shows that it is not dependent on opioid and cannabinoid receptors. because of strong documents about the roles of gaba and benzodiazepine receptors in h...

Endogenous neurosteroids and neuroactive steroids have potent and widespread actions on the brain via inhibitory GABAA receptors. In recombinant receptors and genetic mouse models their actions depend on the α, β, and δ subunits of the receptor, especially on those that form extrasynaptic GABAA receptors responsible for non-synaptic (tonic) inhibition, but they also act on synaptically enriched...

Ligands acting at the benzodiazepine (BZ) site of g-aminobutyric acid type A (GABAA) receptors currently are the most widely used hypnotics. BZs such as diazepam (Dz) potentiate GABAA receptor activation. To determine the GABAA receptor subtypes that mediate the hypnotic action of Dz wild-type mice and mice that harbor Dz-insensitive a1 GABAA receptors [a1 (H101R) mice] were compared. Sleep lat...

Physiological properties of GABAA receptors from acutely dissociated rat dentate granule cells. Study of fast, GABAA receptor-mediated, inhibitory postsynaptic currents (IPSCs) in hippocampal dentate granule cells has suggested that properties of GABAA receptors influence the amplitude and time course of the IPSCs. This study describes the physiological properties of GABAA receptors present on ...

The high-affinity of [3H]gamma-aminobutyric acid (GABA) to GABAA receptors and [3H]baclofen to GABAB receptors were studied in the cerebellum of pyridoxine-deficient rats and compared to pyridoxine-supplemented controls. There was a significant increase in the maximal binding (Bmax) of both GABAA and GABAB receptors with no significant difference in their binding affinities (Kd). The changes ob...

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