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Ethanol Inhibits the Binding of Substance P to Rat Brain Cortex NK1 Receptors

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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 K D value of 80 pM and another one with a K D 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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Authors and Affiliations

  1. Istituto di Bioimmagini e Fisiologia Molecolare, CNR, Italy

    S. Scarrone, A. Cupello, M. Matarrese & F. Fazio

  2. Dipartimento Farmaco Chimico Tecnologico, Università di Siena, Via A. Moro, 53100, Siena, Italy

    A. Cappelli & R. M. Moresco

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  1. S. Scarrone
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  2. A. Cappelli
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  3. A. Cupello
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  4. M. Matarrese
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  5. R. M. Moresco
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  6. F. Fazio
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Correspondence to A. Cupello.

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Scarrone, S., Cappelli, A., Cupello, A. et al. Ethanol Inhibits the Binding of Substance P to Rat Brain Cortex NK1 Receptors. Neurochem Res 28, 1159–1162 (2003). https://doi.org/10.1023/A:1024216109472

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