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Effects of dopaminergic drug treatments on in vivo radioligand binding to brain vesicular monoamine transporters

Abstract

The effects of various dopaminergic drug treatments on the in vivo regional brain distribution of high-affinity radioligands ([{sup 11}C]dihydrotetrabenazine and [{sup 11}C]methoxytetrabenazine) for the rat brain vesicular monoamine transporter (VMAT2) were determined. Acute treatments with reserpine (2 mg/kg i.p.), tetrabenazine (10 mg/kg i.v.) or related benzoisoquinolines significantly reduced radiotracer binding in vivo. In contrast, radiotracer distributions remained unchanged after treatments with other dopaminergic drugs, whether given by single injection (haloperidol, 1 mg/kg i.p., pargyline 80 mg/kg), repeatedly (pargyline, 80 mg/kg s.c., 14 days), or by continuous infusion (deprenyl, 10 mg/kg/day, 5 days; L-DOPA methyl ester 100 mg/kg/day, 5 days). Repeated injections of tetrabenazine (5 mg/kg i.p., twice daily, 3 days) did not alter in vivo radioligand binding measured after allowing drug washout from the brain. These studies support the proposal that in vivo PET imaging of VMAT2 radioligands in patients with extrapyramidal movement disorders will not be affected by concurrent use of L-DOPA or deprenyl.
Publication Date:
May 01, 1996
Product Type:
Journal Article
Resource Relation:
Journal Name: Nuclear Medicine and Biology; Journal Volume: 23; Journal Issue: 4; Other Information: PII: 0969805196000236; Copyright (c) 1996 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved; Country of input: International Atomic Energy Agency (IAEA); PBD: May 1996
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE; BRAIN; CARBON 11; DOPAMINE; IN VIVO; MICE; RADIOPHARMACEUTICALS; RATS; RESERPINE; TISSUE DISTRIBUTION
OSTI ID:
20379329
Country of Origin:
United Kingdom
Language:
English
Other Identifying Numbers:
Journal ID: ISSN 0969-8051; NMBIEO; TRN: GB03R1101059906
Submitting Site:
GBN
Size:
page(s) 467-471
Announcement Date:
Sep 23, 2003

Citation Formats

Kilbourn, Michael R, Frey, Kirk A, Vander Borght, Thierry, and Sherman, Phillip S. Effects of dopaminergic drug treatments on in vivo radioligand binding to brain vesicular monoamine transporters. United Kingdom: N. p., 1996. Web. doi:10.1016/0969-8051(96)00023-6.
Kilbourn, Michael R, Frey, Kirk A, Vander Borght, Thierry, & Sherman, Phillip S. Effects of dopaminergic drug treatments on in vivo radioligand binding to brain vesicular monoamine transporters. United Kingdom. https://doi.org/10.1016/0969-8051(96)00023-6
Kilbourn, Michael R, Frey, Kirk A, Vander Borght, Thierry, and Sherman, Phillip S. 1996. "Effects of dopaminergic drug treatments on in vivo radioligand binding to brain vesicular monoamine transporters." United Kingdom. https://doi.org/10.1016/0969-8051(96)00023-6.
@misc{etde_20379329,
title = {Effects of dopaminergic drug treatments on in vivo radioligand binding to brain vesicular monoamine transporters}
author = {Kilbourn, Michael R, Frey, Kirk A, Vander Borght, Thierry, and Sherman, Phillip S}
abstractNote = {The effects of various dopaminergic drug treatments on the in vivo regional brain distribution of high-affinity radioligands ([{sup 11}C]dihydrotetrabenazine and [{sup 11}C]methoxytetrabenazine) for the rat brain vesicular monoamine transporter (VMAT2) were determined. Acute treatments with reserpine (2 mg/kg i.p.), tetrabenazine (10 mg/kg i.v.) or related benzoisoquinolines significantly reduced radiotracer binding in vivo. In contrast, radiotracer distributions remained unchanged after treatments with other dopaminergic drugs, whether given by single injection (haloperidol, 1 mg/kg i.p., pargyline 80 mg/kg), repeatedly (pargyline, 80 mg/kg s.c., 14 days), or by continuous infusion (deprenyl, 10 mg/kg/day, 5 days; L-DOPA methyl ester 100 mg/kg/day, 5 days). Repeated injections of tetrabenazine (5 mg/kg i.p., twice daily, 3 days) did not alter in vivo radioligand binding measured after allowing drug washout from the brain. These studies support the proposal that in vivo PET imaging of VMAT2 radioligands in patients with extrapyramidal movement disorders will not be affected by concurrent use of L-DOPA or deprenyl.}
doi = {10.1016/0969-8051(96)00023-6}
journal = []
issue = {4}
volume = {23}
journal type = {AC}
place = {United Kingdom}
year = {1996}
month = {May}
}