Preliminary evaluation of 2-[4-[3-tert-butylamino)-2-hydroxypropoxy]phenyl]-3-methyl-6-me thoxy-4(3H)-quinazolinone ([+/-]HX-CH 44) as a selective beta1-adrenoceptor ligand for PET

(+/-)-3-[11C]Methyl-2-[4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-6 -methoxy-4(3H) quinazolinone ([+/-]-[11C]HX-CH 44) was labeled with carbon-11 using [11C]iodomethane with the corresponding N-demethylated precursor. Then, 30-90 mCi (1.10-3.33 GBq) of pure [11C]HX-CH 44 were obtained 30 min af...

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Bibliographic Details
Published in:Nuclear medicine and biology 1999-01, Vol.26 (1), p.105-109
Main Authors: Valette, H, Dollé, F, Guenther, I, Demphel, S, Rasetti, C, Hinnen, F, Fuseau, C, Crouzel, C
Format: Article
Language:English
Subjects:
Adrenergic beta-Antagonists - blood
Adrenergic beta-Antagonists - pharmacology
Animals
Carbon Radioisotopes
Dogs
Heart - diagnostic imaging
Ligands
Lung - diagnostic imaging
Propanolamines - blood
Propanolamines - pharmacology
Quinazolinones
Radiopharmaceuticals - chemical synthesis
Rats
Rats, Sprague-Dawley
Receptors, Adrenergic, beta-1 - analysis
Receptors, Adrenergic, beta-1 - drug effects
Tomography, Emission-Computed
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Summary:(+/-)-3-[11C]Methyl-2-[4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-6 -methoxy-4(3H) quinazolinone ([+/-]-[11C]HX-CH 44) was labeled with carbon-11 using [11C]iodomethane with the corresponding N-demethylated precursor. Then, 30-90 mCi (1.10-3.33 GBq) of pure [11C]HX-CH 44 were obtained 30 min after end of bombardment with specific radioactivities of 500-1,400 mCi/micromol (18.5-51.8 GBq/micromol). Myocardial uptake in dogs was 0.340+/-0.043 pmol/mL tissue per nanomole injected, 10-15 min postinjection. Heart-to-lung ratio was 3 from the 5th to the 30th minute. Only 35% of the myocardial radioactivity could be displaced. Tissue uptake could not be blocked with appropriate compounds. Therefore, (+/-)-[11C]HX-CH 44 does not appear to be a suitable ligand for the study of myocardial beta1-adrenoceptors in positron emission tomography.
ISSN:0969-8051