Evaluation of [11C]metergoline as a PET radiotracer for 5HTR in nonhuman primates

Journal Article · Tue Apr 20 00:00:00 EDT 2010 · Bioinorganic and Medicinal Chemistry

DOI:https://doi.org/10.1016/j.bmc.2010.04.039· OSTI ID:1014331

Hooker, J M; Hooker, J M; Kim, S W; Reibel, A T; Alexoff, D; Xu, Y; Shea, C

Metergoline, a serotonin receptor antagonist, was labeled with carbon-11 in order to evaluate its pharmacokinetics and distribution in non-human primates using positron emission tomography. [{sup 11}C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by pretreatment with metergoline and altanserin throughout the cortex. Non-specific binding and insensitivity to changes in synaptic serotonin limit its potential as a PET radiotracer. However, the characterization of [{sup 11}C]metergoline pharmacokinetics and binding in the brain and peripheral organs using PET improves our understanding of metergoline drug pharmacology.

• Research Organization: Brookhaven National Lab. (BNL), Upton, NY (United States)
• Sponsoring Organization: DOE - OFFICE OF SCIENCE
• DOE Contract Number: DE-AC02-98CH10886
• OSTI ID: 1014331
• Report Number(s): BNL-94446-2010-JA; R&D Project: MO-085; KP1602010; TRN: US1102728
• Journal Information: Bioinorganic and Medicinal Chemistry, Vol. 18, Issue 22; ISSN 0968-0896
• Country of Publication: United States
• Language: English

Related Subjects

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
59 BASIC BIOLOGICAL SCIENCES
BRAIN
CARBON 11
DISTRIBUTION
EVALUATION
LABELLING
ORGANS
PHARMACOLOGY
PRIMATES
RECEPTORS
SEROTONIN
POSITRON COMPUTED TOMOGRAPHY
TRACER TECHNIQUES
UPTAKE
metergoline
carbon-11
PET
serotonin
altanserin