Inhibition of neurotransmitter and hormone transport into secretory vesicles by 2-(4-phenylpiperidino)cyclohexanol and 2-bromo-α-ergocryptine

Both compounds act as uncouplers and dissipate the electrochemical gradient of protons

Yoshinori Moriyama, Kosuke Amakatsu, Hiroshi Yamada, Mi Yeon Park, Masamitsu Futai

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

2-(4-Phenylpiperidino)cyclohexanol (AH-5183) and 2-bromo-α-ergocryptine, known inhibitors of the transport of acetylcholine and l-glutamate, respectively, into synaptic vesicles, inhibited the ATP-dependent uptake of dopamine in parallel with the dissipation of the electrochemical gradient of protons in chromaffin granule membrane vesicles. These compounds induced the release of accumulated dopamine from the vesicles. They also inhibited the ATP-dependent formation of the electrochemical gradient of protons in liposomes reconstituted with chromaffin H+-ATPase without affecting the activities for ATP hydrolysis, and ATP-dependent uptakes of dopamine, γ-aminobutyrate, and glutamate into synaptic vesicles. These results indicated that 2-(4-phenylpiperidino)cyclohexanol and 2-bromo-α-ergocryptine acted as uncouplers in the secretory vesicles.

Original languageEnglish
Pages (from-to)233-238
Number of pages6
JournalArchives of Biochemistry and Biophysics
Volume290
Issue number1
DOIs
Publication statusPublished - 1991
Externally publishedYes

Fingerprint

Secretory Vesicles
Neurotransmitter Agents
Protons
Adenosine Triphosphate
Hormones
Dopamine
Synaptic Vesicles
Glutamic Acid
Chromaffin Granules
Aminobutyrates
Proton-Translocating ATPases
Liposomes
Acetylcholine
Hydrolysis
Membranes
ergocryptine
vesamicol

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

Cite this

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title = "Inhibition of neurotransmitter and hormone transport into secretory vesicles by 2-(4-phenylpiperidino)cyclohexanol and 2-bromo-α-ergocryptine: Both compounds act as uncouplers and dissipate the electrochemical gradient of protons",
abstract = "2-(4-Phenylpiperidino)cyclohexanol (AH-5183) and 2-bromo-α-ergocryptine, known inhibitors of the transport of acetylcholine and l-glutamate, respectively, into synaptic vesicles, inhibited the ATP-dependent uptake of dopamine in parallel with the dissipation of the electrochemical gradient of protons in chromaffin granule membrane vesicles. These compounds induced the release of accumulated dopamine from the vesicles. They also inhibited the ATP-dependent formation of the electrochemical gradient of protons in liposomes reconstituted with chromaffin H+-ATPase without affecting the activities for ATP hydrolysis, and ATP-dependent uptakes of dopamine, γ-aminobutyrate, and glutamate into synaptic vesicles. These results indicated that 2-(4-phenylpiperidino)cyclohexanol and 2-bromo-α-ergocryptine acted as uncouplers in the secretory vesicles.",
author = "Yoshinori Moriyama and Kosuke Amakatsu and Hiroshi Yamada and Park, {Mi Yeon} and Masamitsu Futai",
year = "1991",
doi = "10.1016/0003-9861(91)90614-O",
language = "English",
volume = "290",
pages = "233--238",
journal = "Archives of Biochemistry and Biophysics",
issn = "0003-9861",
publisher = "Academic Press Inc.",
number = "1",

}

TY - JOUR

T1 - Inhibition of neurotransmitter and hormone transport into secretory vesicles by 2-(4-phenylpiperidino)cyclohexanol and 2-bromo-α-ergocryptine

T2 - Both compounds act as uncouplers and dissipate the electrochemical gradient of protons

AU - Moriyama, Yoshinori

AU - Amakatsu, Kosuke

AU - Yamada, Hiroshi

AU - Park, Mi Yeon

AU - Futai, Masamitsu

PY - 1991

Y1 - 1991

N2 - 2-(4-Phenylpiperidino)cyclohexanol (AH-5183) and 2-bromo-α-ergocryptine, known inhibitors of the transport of acetylcholine and l-glutamate, respectively, into synaptic vesicles, inhibited the ATP-dependent uptake of dopamine in parallel with the dissipation of the electrochemical gradient of protons in chromaffin granule membrane vesicles. These compounds induced the release of accumulated dopamine from the vesicles. They also inhibited the ATP-dependent formation of the electrochemical gradient of protons in liposomes reconstituted with chromaffin H+-ATPase without affecting the activities for ATP hydrolysis, and ATP-dependent uptakes of dopamine, γ-aminobutyrate, and glutamate into synaptic vesicles. These results indicated that 2-(4-phenylpiperidino)cyclohexanol and 2-bromo-α-ergocryptine acted as uncouplers in the secretory vesicles.

AB - 2-(4-Phenylpiperidino)cyclohexanol (AH-5183) and 2-bromo-α-ergocryptine, known inhibitors of the transport of acetylcholine and l-glutamate, respectively, into synaptic vesicles, inhibited the ATP-dependent uptake of dopamine in parallel with the dissipation of the electrochemical gradient of protons in chromaffin granule membrane vesicles. These compounds induced the release of accumulated dopamine from the vesicles. They also inhibited the ATP-dependent formation of the electrochemical gradient of protons in liposomes reconstituted with chromaffin H+-ATPase without affecting the activities for ATP hydrolysis, and ATP-dependent uptakes of dopamine, γ-aminobutyrate, and glutamate into synaptic vesicles. These results indicated that 2-(4-phenylpiperidino)cyclohexanol and 2-bromo-α-ergocryptine acted as uncouplers in the secretory vesicles.

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U2 - 10.1016/0003-9861(91)90614-O

DO - 10.1016/0003-9861(91)90614-O

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EP - 238

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JF - Archives of Biochemistry and Biophysics

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