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

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

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

11 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 language	English
Journal	Life Sciences
Volume	64
Issue number	8
Publication status	Published - 1999 Jan 15
Externally published	Yes

Keywords

Biperiden
Human
Muscarinic cholinergic receptor
Positron emission tomography

ASJC Scopus subject areas

Pharmacology

Cite this

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title = "Muscarinic receptor occupancy by biperiden in living human brain",

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.",

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

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T1 - Muscarinic receptor occupancy by biperiden in living human brain

AU - Sudo, Yasuhiko

AU - Suhara, Tetsuya

AU - Suzuki, Kazutoshi

AU - Okubo, Yoshiro

AU - Yoshikawa, Kyosan

AU - Uchida, Sunao

AU - Sassa, Takeshi

AU - Okauchi, Takashi

AU - Sasaki, Yasuhito

AU - Matsushita, Masaaki

PY - 1999/1/15

Y1 - 1999/1/15

N2 - 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.

AB - 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.

KW - Biperiden

KW - Human

KW - Muscarinic cholinergic receptor

KW - Positron emission tomography

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Muscarinic receptor occupancy by biperiden in living human brain

Abstract

Keywords

ASJC Scopus subject areas

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