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Effects of trihexyphenidyl and L-dopa on brain muscarinic cholinergic receptor binding measured by positron emission tomography

Abstract

The effects of pharmacological intervention on brain muscarinic cholinergic receptor (mAChR) binding were assessed in seven patients with Parkinson's disease by positron emission tomography and carbon-11 labelled N-methyl-4-piperidyl benzilate ([[sup 11]C]NMPB). [[sup 11]C]NMPB was injected twice, approximately 2 hours apart, in each patient, to assess the effect of single doses of 4 mg of trihexyphenidyl (n=5) or 400 mg of L-dopa with 57 mg of benserazide (n=2) on the binding parameter of mAChRs (K[sub 3]). There was a mean 28% inhibition of K[sub 3] values in the brain in the presence of trihexyphenidyl, which was assumed to reflect mAChR occupancy. No significant change in K[sub 3] was observed in the presence of L-dopa. This study demonstrates the feasibility of measuring mAChR occupancy by an anticholinergic medication with PET.
Authors:
Shinotoh, H; Asahina, M; Hirayama, K; [1]  Inoue, O; Suhara, T; Tateno, Y [2] 
  1. Dept. of Neurology, School of Medicine, Chiba Univ., Chiba (Japan)
  2. Division of Clinical Research, National Inst. of Radiological Sciences, Chiba (Japan)
Publication Date:
Jan 01, 1994
Product Type:
Journal Article
Reference Number:
AIX-25-058233; EDB-94-125937
Resource Relation:
Journal Name: Journal of Neural Transmission, Parkinson's Disease and Dementia Section; (Austria); Journal Volume: 7
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE; BRAIN; POSITRON COMPUTED TOMOGRAPHY; DOPA; BIOLOGICAL EFFECTS; CARBON 11; DRUGS; KINETICS; NERVOUS SYSTEM DISEASES; RECEPTORS; AMINO ACIDS; AUTONOMIC NERVOUS SYSTEM AGENTS; BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; BODY; CARBON ISOTOPES; CARBOXYLIC ACIDS; CENTRAL NERVOUS SYSTEM; COMPUTERIZED TOMOGRAPHY; DIAGNOSTIC TECHNIQUES; DISEASES; EMISSION COMPUTED TOMOGRAPHY; EVEN-ODD NUCLEI; HYDROXY ACIDS; ISOTOPES; LIGHT NUCLEI; MEMBRANE PROTEINS; MINUTES LIVING RADIOISOTOPES; NERVOUS SYSTEM; NEUROREGULATORS; NUCLEI; ORGANIC ACIDS; ORGANIC COMPOUNDS; ORGANS; PROTEINS; RADIOISOTOPES; TOMOGRAPHY; 550601* - Medicine- Unsealed Radionuclides in Diagnostics
OSTI ID:
7000837
Country of Origin:
Austria
Language:
English
Other Identifying Numbers:
Journal ID: ISSN 0936-3076; CODEN: JNPSEJ
Submitting Site:
INIS
Size:
Pages: 35-46
Announcement Date:

Citation Formats

Shinotoh, H, Asahina, M, Hirayama, K, Inoue, O, Suhara, T, and Tateno, Y. Effects of trihexyphenidyl and L-dopa on brain muscarinic cholinergic receptor binding measured by positron emission tomography. Austria: N. p., 1994. Web. doi:10.1007/BF02252661.
Shinotoh, H, Asahina, M, Hirayama, K, Inoue, O, Suhara, T, & Tateno, Y. Effects of trihexyphenidyl and L-dopa on brain muscarinic cholinergic receptor binding measured by positron emission tomography. Austria. doi:10.1007/BF02252661.
Shinotoh, H, Asahina, M, Hirayama, K, Inoue, O, Suhara, T, and Tateno, Y. 1994. "Effects of trihexyphenidyl and L-dopa on brain muscarinic cholinergic receptor binding measured by positron emission tomography." Austria. doi:10.1007/BF02252661. https://www.osti.gov/servlets/purl/10.1007/BF02252661.
@misc{etde_7000837,
title = {Effects of trihexyphenidyl and L-dopa on brain muscarinic cholinergic receptor binding measured by positron emission tomography}
author = {Shinotoh, H, Asahina, M, Hirayama, K, Inoue, O, Suhara, T, and Tateno, Y}
abstractNote = {The effects of pharmacological intervention on brain muscarinic cholinergic receptor (mAChR) binding were assessed in seven patients with Parkinson's disease by positron emission tomography and carbon-11 labelled N-methyl-4-piperidyl benzilate ([[sup 11]C]NMPB). [[sup 11]C]NMPB was injected twice, approximately 2 hours apart, in each patient, to assess the effect of single doses of 4 mg of trihexyphenidyl (n=5) or 400 mg of L-dopa with 57 mg of benserazide (n=2) on the binding parameter of mAChRs (K[sub 3]). There was a mean 28% inhibition of K[sub 3] values in the brain in the presence of trihexyphenidyl, which was assumed to reflect mAChR occupancy. No significant change in K[sub 3] was observed in the presence of L-dopa. This study demonstrates the feasibility of measuring mAChR occupancy by an anticholinergic medication with PET.}
doi = {10.1007/BF02252661}
journal = {Journal of Neural Transmission, Parkinson's Disease and Dementia Section; (Austria)}
volume = {7}
journal type = {AC}
place = {Austria}
year = {1994}
month = {Jan}
}