Picrotoxin is a plant alkaloid that is often used to block the activity of neuronal GABA and glycine receptors. However, the mechanism by which picrotoxin inhibits these receptors is still in debate. In this study, we investigated the picrotoxin inhibition on perch-rho subunits expressed heterologously in Xenopus laevis oocytes, and on native GABA(C) receptors of perch bipolar cells. Both compe...

Glutamate and gamma-aminobutyric acid (GABA) are major excitatory and inhibitory neurotransmitters in the vertebrate retina, "a genuine neural center" (Ramón y Cajal, 1964, Recollections of My Life, C.E. Horne (Translater) MIT Press, Cambridge, MA). Photoreceptors, generating visual signals, and bipolar cells, mediating signal transfer from photoreceptors to ganglion cells, both release glutama...

GABA receptor (GABAR) types C (GABACR) and A (GABAAR) are both GABA-gated chloride channels that are distinguished by their distinct competitive antagonist properties. The structural mechanism underlying these distinct properties is not well understood. In this study, using previously identified binding residues as a guide, we made individual or combined mutations of nine binding residues in th...

g-Aminobutyrate type C (GABAC) receptors are ligand-gated ion channels that are expressed preponderantly in the vertebrate retina and are characterized, among other things, by a very low rate of desensitization and resistance to the specific GABAA antagonist bicuculline. To examine which structural elements determine the nondesensitizing character of the human homomeric r1 receptor, we used a c...

We report a methodology for labeling the GABAc receptor on the surface membrane of intact cells. This work builds upon our earlier work with serotonin-conjugated quantum dots and our studies with PEGylated quantum dots to reduce nonspecific binding. In the current approach, a PEGylated derivative of muscimol was synthesized and attached via an amide linkage to quantum dots coated in an amphiphi...

GABA(C) receptors (GABA(C)Rs) are widely expressed in the mammalian subcortical visual system, particularly in the retina and superior colliculus (SC). GABA(C)Rs are composed of specific rho1-3 subunits the expression of which varies among visual structures. Thus rho1 subunits are most abundant in retina, and their loss eliminates GABA(C)R expression and function. In the SC, rho2 subunit expres...