Preparation and pharmacological characterization of [76Br]-meta-bromobenzylguanidine ([76Br]MBBG)

Loc'h, Christian, Mardon, Karine, Valette, Heric, Brutesco, Catherine, Merlet, Pascal, Syrota, Andre and Maziere, Bernard (1994) Preparation and pharmacological characterization of [76Br]-meta-bromobenzylguanidine ([76Br]MBBG). Nuclear Medicine and Biology, 21 1: 49-55. doi:10.1016/0969-8051(94)90128-7


Author Loc'h, Christian
Mardon, Karine
Valette, Heric
Brutesco, Catherine
Merlet, Pascal
Syrota, Andre
Maziere, Bernard
Title Preparation and pharmacological characterization of [76Br]-meta-bromobenzylguanidine ([76Br]MBBG)
Formatted title
Preparation and pharmacological characterization of [76Br]-meta-bromobenzylguanidine ([76Br]MBBG)
Journal name Nuclear Medicine and Biology   Check publisher's open access policy
ISSN 0969-8051
1872-9614
Publication date 1994-01
Sub-type Article (original research)
DOI 10.1016/0969-8051(94)90128-7
Volume 21
Issue 1
Start page 49
End page 55
Total pages 7
Place of publication Philadelphia, PA, United States
Publisher Elsevier
Language eng
Abstract [76Br]-meta-Bromobenzylguanidine ([76Br]MBBG) was prepared from the iodinated analog (MIBG) and [76Br]NH4 using a Cu+-assisted halogen exchange reaction. [76Br]MBBG was produced in a 60–65% radiochemical yield with a specific activity of 20 MBq/nmol. In rats, biodistribution kinetic studies showed a high uptake of [76Br]MBBG in heart tissues with its maximum of 5% ID/g at 2 h p.i.; whereas 4 h p.i., the maximum of the heart-to-lung concentration ratio of 8 was observed. Metabolic studies in rats indicated that [76Br]MBBG was rapidly metabolized in plasma. However in heart tissue, 25 h p.i., 85% of the radioactivity still represented unchanged radiotracer. Pharmacological studies in rats showed that the myocardial uptake of [76Br]MBBG was similar to that of norepinephrine. After pretreatment of the rats, the uptake of [76Br]MBBG was reduced 4 h p.i. to the following values: after desipramine (DMI) to 37%, after dexamethasone (DXM) to 88% and after 6-hydroxydopamine (6-OHDA) to 16%. These preliminary results suggest that [76Br]MBBG can be useful for the assessment of heart catecholamine reuptake disorders with PET.
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ
Additional Notes Available online 12 March 2004

Document type: Journal Article
Sub-type: Article (original research)
Collection: Centre for Advanced Imaging Publications
 
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Created: Fri, 26 Nov 2010, 10:07:25 EST by Dr Karine Mardon on behalf of Centre for Advanced Imaging