Ethanol Inhibits the Binding of Substance P to Rat Brain Cortex NK1 Receptors |
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Authors: | Scarrone S. Cappelli A. Cupello A. Matarrese M. Moresco R. M. Fazio F. |
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Affiliation: | (1) Istituto di Bioimmagini e Fisiologia Molecolare, CNR, Italy;(2) Dipartimento Farmaco Chimico Tecnologico, Università di Siena, Via A. Moro, 53100 Siena, Italy |
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Abstract: | The binding of 125I-labeled substance P (SP) to rat brain cortex membranes has been studied Under control conditions and in the presence of ethanol. The binding of SP at low concentrations (20–1000 pM) gave two components, one with a KD value of 80 pM and another one with a KD of 500 pM. The higher-affinity component is due to NK1 receptors, as confirmed by the inhibition Of the SP binding by the rodent NK1 specific agonist [Sar9 Met(O2)11]SP. Ethanol (1.7 mM) added to the binding assays inhibited by more than 50% the specific binding at a very low SP concentration (20 pM); however, it had no effect at SP concentrations ranging from 50 to 120 pM. This suggests a decrease by ethanol of the affinity of SP to the NK1 receptors involved in this binding component. The ethanol effect disappeared at [EtOH] 0.17 mM. |
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Keywords: | Substance P NK1 receptors binding inhibition ethanol |
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