Extracellular proton alters the divalent cation binding affinity in a cyclic nucleotide-gated channel pore |
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Authors: | SH Rho CS Park |
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Affiliation: | Department of Pediatrics, Tohoku University School of Medicine, Sendai 980-77, Japan. |
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Abstract: | The effects of zolpidem on the two forms of recombinant human GABAA receptors (alpha1beta2gamma2s and alpha3beta2gamma2s) at different temperatures were functionally investigated, using the whole-cell patch recording configuration. In both forms, zolpidem potentiated the response to GABA in a concentration-dependent manner. At 16 degrees C, the apparent dissociation constant (KD) values for the alpha1beta2gamma2s and alpha3beta2gamma2s forms were 3.7 x 10(-8) and 5.6 x 10(-7) M, respectively. When the temperature was increased to 36 degrees C, the KD values for the alpha1beta2gamma2s and alpha3beta2gamma2s forms were 2.1 x 10(-7) and 1.5 x 10(-6) M, respectively. Although the affinity ratio was reduced from 15.1 to 7.1-fold the selectivity of zolpidem for the alpha1beta2gamma2s still remained at 36 degrees C. |
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