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

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18 Citations (Scopus)


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
Issue number1
Publication statusPublished - 1991
Externally publishedYes


ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

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