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Research ArticleCARDIOVASCULAR

Z-338 Facilitates Acetylcholine Release from Enteric Neurons Due to Blockade of Muscarinic Autoreceptors in Guinea Pig Stomach

Masayuki Ogishima, Muneshige Kaibara, Shigeru Ueki, Tadashi Kurimoto and Kohtaro Taniyama
Journal of Pharmacology and Experimental Therapeutics July 2000, 294 (1) 33-37;
Masayuki Ogishima
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Muneshige Kaibara
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Shigeru Ueki
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Tadashi Kurimoto
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Kohtaro Taniyama
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Abstract

The mechanism by which Z-338, a novel gastroprokinetic agent, stimulates gastric motility was studied in relation to muscarinic receptors in the guinea pig. Z-338 (3–30 μM) enhanced electrically stimulated contractions and the release of acetylcholine (ACh) that was tetrodotoxin sensitive and extracellular Ca2+ dependent, in gastric strips. Membrane-binding assay revealed that Z-338 possessed binding affinity for muscarinic M1and M2, but not M3 receptors. InXenopus oocytes expressing M1 and M2 muscarinic receptors, Z-338 did not produce any response, but inhibited ACh-induced outward currents, thereby indicating that Z-338 acts on the M1 and M2muscarinic receptors as an antagonist. The M1 receptor antagonist pirenzepine (0.5 μM) and M2 receptor antagonist AF-DX 116 (1 μM) also enhanced electrically stimulated release of ACh. These results indicate that Z-338 facilitates ACh release from cholinergic nerve terminals by blocking muscarinic M1 and M2 autoreceptors, which regulate the release of ACh.

Footnotes

  • Send reprint requests to: Kohtaro Taniyama, M.D., Ph.D., Department of Pharmacology, Nagasaki University School of Medicine, Nagasaki 852-8523, Japan. E-mail: taniyama{at}net.nagasaki-u.ac.jp

  • ↵1 This study was supported by grants from the Ministry of Education, Science, Sports and Culture, Japan.

  • Abbreviations:
    Z-338
    N-(N′,N′-diisopropylaminoethyl)-[2-(2-hydroxy-4,5-dimethoxy-benzoylamino)-1,3-thiazole-4-yl] carboxyamide monohydrochloride trihydrate
    5-HT
    5-hydroxytryptamine
    ACh
    acetylcholine
    NMS
    N-methyl scopolamine
    GIRK1
    G protein-gated inward rectifying K+ channel
    AF-DX 116
    11,2-(diethylamino)methyl-1-piperidinyl-acetyl-5,11-dihydro-6H-pyrido-2,3b-1,4-benzodiazepine-6-one
    TTX
    tetrodotoxin
    • Received September 20, 1999.
    • Accepted March 10, 2000.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 294 (1)
Journal of Pharmacology and Experimental Therapeutics
Vol. 294, Issue 1
1 Jul 2000
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Research ArticleCARDIOVASCULAR

Z-338 Facilitates Acetylcholine Release from Enteric Neurons Due to Blockade of Muscarinic Autoreceptors in Guinea Pig Stomach

Masayuki Ogishima, Muneshige Kaibara, Shigeru Ueki, Tadashi Kurimoto and Kohtaro Taniyama
Journal of Pharmacology and Experimental Therapeutics July 1, 2000, 294 (1) 33-37;

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Research ArticleCARDIOVASCULAR

Z-338 Facilitates Acetylcholine Release from Enteric Neurons Due to Blockade of Muscarinic Autoreceptors in Guinea Pig Stomach

Masayuki Ogishima, Muneshige Kaibara, Shigeru Ueki, Tadashi Kurimoto and Kohtaro Taniyama
Journal of Pharmacology and Experimental Therapeutics July 1, 2000, 294 (1) 33-37;
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