Muscarinic receptor occupancy by biperiden in living human brain

Yasuhiko Sudo, Tetsuya Suhara, Kazutoshi Suzuki, Yoshiro Okubo, Kyosan Yoshikawa, Sunao Uchida, Takeshi Sassa, Takashi Okauchi, Yasuhito Sasaki, Masaaki Matsushita

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

Anticholinergic drug is often used to treat extrapyramidal symptoms. We measured muscarinic cholinergic receptor (mAchR) occupancy by the oral administration of biperiden in eight healthy subjects using positron emission tomography (PET) and [11C]N-methyl-4-piperidylbenzilate (NMPB). After the baseline scan each subject underwent one or two post-dose PET scans, mAchR occupancy was 10-45% in the frontal cortex three hours after the oral administration of 4 mg of biperiden. The occupancy correlated with the plasma concentration of biperiden in a curvilinear manner.

Original languageEnglish
JournalLife Sciences
Volume64
Issue number8
Publication statusPublished - 1999 Jan 15
Externally publishedYes

Keywords

  • Biperiden
  • Human
  • Muscarinic cholinergic receptor
  • Positron emission tomography

ASJC Scopus subject areas

  • Pharmacology

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  • Cite this

    Sudo, Y., Suhara, T., Suzuki, K., Okubo, Y., Yoshikawa, K., Uchida, S., Sassa, T., Okauchi, T., Sasaki, Y., & Matsushita, M. (1999). Muscarinic receptor occupancy by biperiden in living human brain. Life Sciences, 64(8).