Block by apomorphine of acetylcholine receptor channels expressed in Xenopus oocytes

Ken Nakazawa, Takami Akiyama, Kazuhide Inoue

Research output: Contribution to journalArticle

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Abstract

Effects of apomorphine and other compounds related to dopamine receptors on nicotinic acetylcholine receptor channels were investigated by expressing functional channels in Xenopus oocytes. When channels were expressed with a combination of α3 and β4 subunits, acetylcholine activated an inward current, and apomorphine suppressed the current in a concentration-dependent manner with an IC50 value of about 3 μM. SKF38393 (R(+)-1-phehyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol; dopamine D1 receptor agonist; 3 and 30 μM), quinpirole (dopamine D2 receptor agonist; 30 μM), SCH23390 (R(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine; dopamine D1 receptor antagonist; 10 μM) or sulpiride (dopamine D2 receptor antagonist; 10 μM) also inhibited the acetylcholine-activated current whereas dopamine (100 μM) was ineffective. The inhibition by apomorphine of the acetylcholine-activated current was also apparent when α3 subunit was combined with β2 subunit instead of β4 subunit, or β4 subunit was combined with α2 or α4 subunit instead of α3 subunit to express channels. The results suggest that apomorphine blocks acetylcholine receptor channels through a binding site that is similar to, but cannot be included in dopamine receptors. The binding site may not be present in a single specific subunit.

Original languageEnglish
Pages (from-to)375-379
Number of pages5
JournalEuropean Journal of Pharmacology: Molecular Pharmacology
Volume269
Issue number3
DOIs
Publication statusPublished - Nov 15 1994
Externally publishedYes

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Apomorphine
Cholinergic Receptors
Xenopus
Oocytes
Acetylcholine
Dopamine D1 Receptors
Dopamine Agonists
Dopamine Receptors
Benzazepines
Binding Sites
2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine
Quinpirole
Sulpiride
Dopamine Antagonists
Dopamine D2 Receptors
Nicotinic Receptors
Inhibitory Concentration 50
Dopamine

All Science Journal Classification (ASJC) codes

  • Pharmacology

Cite this

Block by apomorphine of acetylcholine receptor channels expressed in Xenopus oocytes. / Nakazawa, Ken; Akiyama, Takami; Inoue, Kazuhide.

In: European Journal of Pharmacology: Molecular Pharmacology, Vol. 269, No. 3, 15.11.1994, p. 375-379.

Research output: Contribution to journalArticle

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