The opioid peptide dynorphin directly blocks NMDA receptor channels in the rat

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Abstract

1. The actions of dynorphin on N-methyl-D-aspartate (NMDA) responses were examined in acutely dissociated trigeminal neurons in rat. Whole-cell and single-channel currents were recorded using the patch clamp technique. 2. Dynorphins reduced NMDA-activated currents (I(NMDA)). The IC50 was 0.25 μM for dynorphin (1-32), 1.65 μM for dynorphin (1-17) and 1.8 μM for dynorphin (1-13). 3. The blocking action of dynorphin is voltage independent. 4. The inhibitory action of dynorphin cannot be blocked by high concentration of the non-selective opioid receptor antagonist naloxone, nor by the specific κ-opioid receptor antagonist nor-Binaltorphimine (nor-BNI). 5. Single-channel analyses indicate that dynorphin reduces the fraction of time the channel is open without altering the channel conductance. 6. We propose that dynorphin acts directly on NMDA receptors.

Original languageEnglish (US)
Pages (from-to)575-581
Number of pages7
JournalJournal of Physiology
Volume482
Issue number3
StatePublished - 1995

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Dynorphins
Opioid Peptides
N-Methyl-D-Aspartate Receptors
N-Methylaspartate
Narcotic Antagonists
Patch-Clamp Techniques
Naloxone
Inhibitory Concentration 50
Neurons

ASJC Scopus subject areas

  • Physiology

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The opioid peptide dynorphin directly blocks NMDA receptor channels in the rat. / Chen, L.; Gu, Yanping; Huang, Li-Yen.

In: Journal of Physiology, Vol. 482, No. 3, 1995, p. 575-581.

Research output: Contribution to journalArticle

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abstract = "1. The actions of dynorphin on N-methyl-D-aspartate (NMDA) responses were examined in acutely dissociated trigeminal neurons in rat. Whole-cell and single-channel currents were recorded using the patch clamp technique. 2. Dynorphins reduced NMDA-activated currents (I(NMDA)). The IC50 was 0.25 μM for dynorphin (1-32), 1.65 μM for dynorphin (1-17) and 1.8 μM for dynorphin (1-13). 3. The blocking action of dynorphin is voltage independent. 4. The inhibitory action of dynorphin cannot be blocked by high concentration of the non-selective opioid receptor antagonist naloxone, nor by the specific κ-opioid receptor antagonist nor-Binaltorphimine (nor-BNI). 5. Single-channel analyses indicate that dynorphin reduces the fraction of time the channel is open without altering the channel conductance. 6. We propose that dynorphin acts directly on NMDA receptors.",
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T1 - The opioid peptide dynorphin directly blocks NMDA receptor channels in the rat

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N2 - 1. The actions of dynorphin on N-methyl-D-aspartate (NMDA) responses were examined in acutely dissociated trigeminal neurons in rat. Whole-cell and single-channel currents were recorded using the patch clamp technique. 2. Dynorphins reduced NMDA-activated currents (I(NMDA)). The IC50 was 0.25 μM for dynorphin (1-32), 1.65 μM for dynorphin (1-17) and 1.8 μM for dynorphin (1-13). 3. The blocking action of dynorphin is voltage independent. 4. The inhibitory action of dynorphin cannot be blocked by high concentration of the non-selective opioid receptor antagonist naloxone, nor by the specific κ-opioid receptor antagonist nor-Binaltorphimine (nor-BNI). 5. Single-channel analyses indicate that dynorphin reduces the fraction of time the channel is open without altering the channel conductance. 6. We propose that dynorphin acts directly on NMDA receptors.

AB - 1. The actions of dynorphin on N-methyl-D-aspartate (NMDA) responses were examined in acutely dissociated trigeminal neurons in rat. Whole-cell and single-channel currents were recorded using the patch clamp technique. 2. Dynorphins reduced NMDA-activated currents (I(NMDA)). The IC50 was 0.25 μM for dynorphin (1-32), 1.65 μM for dynorphin (1-17) and 1.8 μM for dynorphin (1-13). 3. The blocking action of dynorphin is voltage independent. 4. The inhibitory action of dynorphin cannot be blocked by high concentration of the non-selective opioid receptor antagonist naloxone, nor by the specific κ-opioid receptor antagonist nor-Binaltorphimine (nor-BNI). 5. Single-channel analyses indicate that dynorphin reduces the fraction of time the channel is open without altering the channel conductance. 6. We propose that dynorphin acts directly on NMDA receptors.

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