Block by 5-hydroxytryptamine of neuronal acetylcholine receptor channels expressed in Xenopus oocytes

Ken Nakazawa; Takami Akiyama; Kazuhide Inoue

doi:10.1007/BF02071882

Block by 5-hydroxytryptamine of neuronal acetylcholine receptor channels expressed in Xenopus oocytes

Ken Nakazawa, Takami Akiyama, Kazuhide Inoue

Research output: Contribution to journal › Article › peer-review

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Abstract

1. Effects of 5-hydroxytryptamine (5-HT) on neuronal nicotinic acetylcholine (ACh) receptor channels were investigated by expressing cloned channel subunits in Xenopus oocytes. 2. When channels were expressed with a combination of α₃ and β₄ subunits, 5-HT (10 to 300 μM) reversibly inhibited an inward current activated by 100 μM ACh in a concentration-dependent manner. The inhibition was also observed when α₃ subunit was combined with β₂ subunit instead of β₄ subunit, or β₄ subunit was combined with α₂ or α_4-1 subunit instead of α₃ subunit to express channels. 3. Compounds known to antagonize at 5-HT receptors (LY53857, metoclopramide and propranolol) exhibited an agonistic effect: they inhibited the ACh-activated current. 4. The results suggest that 5-HT inhibits recombinant neuronal nicotinic receptor channels through a binding-site distinct from conventional 5-HT receptors. The binding-site may not be attributed to a unique type of channel subunits.

Original language	English
Pages (from-to)	495-500
Number of pages	6
Journal	Cellular and molecular neurobiology
Volume	15
Issue number	4
DOIs	https://doi.org/10.1007/BF02071882
Publication status	Published - Aug 1 1995
Externally published	Yes

All Science Journal Classification (ASJC) codes

Cellular and Molecular Neuroscience
Cell Biology

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10.1007/BF02071882

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title = "Block by 5-hydroxytryptamine of neuronal acetylcholine receptor channels expressed in Xenopus oocytes",

abstract = "1. Effects of 5-hydroxytryptamine (5-HT) on neuronal nicotinic acetylcholine (ACh) receptor channels were investigated by expressing cloned channel subunits in Xenopus oocytes. 2. When channels were expressed with a combination of α3 and β4 subunits, 5-HT (10 to 300 μM) reversibly inhibited an inward current activated by 100 μM ACh in a concentration-dependent manner. The inhibition was also observed when α3 subunit was combined with β2 subunit instead of β4 subunit, or β4 subunit was combined with α2 or α4-1 subunit instead of α3 subunit to express channels. 3. Compounds known to antagonize at 5-HT receptors (LY53857, metoclopramide and propranolol) exhibited an agonistic effect: they inhibited the ACh-activated current. 4. The results suggest that 5-HT inhibits recombinant neuronal nicotinic receptor channels through a binding-site distinct from conventional 5-HT receptors. The binding-site may not be attributed to a unique type of channel subunits.",

author = "Ken Nakazawa and Takami Akiyama and Kazuhide Inoue",

year = "1995",

month = aug,

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doi = "10.1007/BF02071882",

language = "English",

volume = "15",

pages = "495--500",

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T1 - Block by 5-hydroxytryptamine of neuronal acetylcholine receptor channels expressed in Xenopus oocytes

AU - Nakazawa, Ken

AU - Akiyama, Takami

AU - Inoue, Kazuhide

PY - 1995/8/1

Y1 - 1995/8/1

N2 - 1. Effects of 5-hydroxytryptamine (5-HT) on neuronal nicotinic acetylcholine (ACh) receptor channels were investigated by expressing cloned channel subunits in Xenopus oocytes. 2. When channels were expressed with a combination of α3 and β4 subunits, 5-HT (10 to 300 μM) reversibly inhibited an inward current activated by 100 μM ACh in a concentration-dependent manner. The inhibition was also observed when α3 subunit was combined with β2 subunit instead of β4 subunit, or β4 subunit was combined with α2 or α4-1 subunit instead of α3 subunit to express channels. 3. Compounds known to antagonize at 5-HT receptors (LY53857, metoclopramide and propranolol) exhibited an agonistic effect: they inhibited the ACh-activated current. 4. The results suggest that 5-HT inhibits recombinant neuronal nicotinic receptor channels through a binding-site distinct from conventional 5-HT receptors. The binding-site may not be attributed to a unique type of channel subunits.

AB - 1. Effects of 5-hydroxytryptamine (5-HT) on neuronal nicotinic acetylcholine (ACh) receptor channels were investigated by expressing cloned channel subunits in Xenopus oocytes. 2. When channels were expressed with a combination of α3 and β4 subunits, 5-HT (10 to 300 μM) reversibly inhibited an inward current activated by 100 μM ACh in a concentration-dependent manner. The inhibition was also observed when α3 subunit was combined with β2 subunit instead of β4 subunit, or β4 subunit was combined with α2 or α4-1 subunit instead of α3 subunit to express channels. 3. Compounds known to antagonize at 5-HT receptors (LY53857, metoclopramide and propranolol) exhibited an agonistic effect: they inhibited the ACh-activated current. 4. The results suggest that 5-HT inhibits recombinant neuronal nicotinic receptor channels through a binding-site distinct from conventional 5-HT receptors. The binding-site may not be attributed to a unique type of channel subunits.

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DO - 10.1007/BF02071882

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JO - Cellular and Molecular Neurobiology

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IS - 4

ER -

Block by 5-hydroxytryptamine of neuronal acetylcholine receptor channels expressed in Xenopus oocytes

Abstract

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