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Background  Many anesthetics modulate 3-transmembrane (such as NMDA) and 4-transmembrane (such as GABA A ) receptors. Clinical and experimental anesthetics exhibiting receptor family specificity often have low water solubility. We hypothesized that the molar water solubility of a hydrocarbon could be used to predict receptor modulation in vitro.    Methods  GABA A  (α 1 β 2 γ 2s ) or NMDA (NR1/NR2A) receptors were expressed in oocytes and studied using standard two-electrode voltage clamp techniques. Hydrocarbons from 14 different organic functional groups were studied at saturated concentrations, and compounds within each group differed only by the carbon number at the ω-position or within a saturated ring. An effect on GABA A  or NMDA receptors was defined as a 10% or greater reversible current change from baseline that was statistically different from zero.    Results  Hydrocarbon moieties potentiated GABA A  and inhibited NMDA receptor currents with at least some members from each functional group modulating both receptor types. A water solubility cut-off for NMDA receptors occurred at 1.1 mM with a 95% CI = 0.45 to 2.8 mM. NMDA receptor cut-off effects were not well correlated with hydrocarbon chain length or molecular volume. No cut-off was observed for GABA A  receptors within the solubility range of hydrocarbons studied.    Conclusions  Hydrocarbon modulation of NMDA receptor function exhibits a molar water solubility cut-off. Differences between unrelated receptor cut-off values suggest that the number, affinity, or efficacy of protein-hydrocarbon interactions at these sites likely differ.

Hydrocarbon molar water solubility predicts NMDA vs. GABAA receptor modulation