Synthesis and tissue distribution of four Se-labeled tertiary amines, potential brain pH imaging agents.
Four new tertiary amines: bis(3-N,N-dimethyl aminopropyl)selenide (PROMOSE), bis(3-N-(morpholino)propyl)selenide, N-methyl-selenomorpholine and N-phenyl-selenomorpholine structurally related to MOSE proposed by Kung and Blau, have been labeled through a radiochemical procedure suitable for both 75Se and 73Se. The radiochemical yields of the carrier added synthesis ranged between 64 and 85% for the four 75Se labelings and was 64% EOB time corrected for [73Se]PROMOSE. The chemical and radiochemical purities were higher than 99% after chromatographic purifications. The n-octanol/phosphate buffer partition coefficients (P) were measured at various pH (6.5-8) for each compound and the tissue distributions of PROMOSE in rats were also carried out. The experimental results showed a good correlation between the P = f(pH) function and the in vivo behaviour of the considered compound. PROMOSE was selected for further investigations as a brain pH indicator.
Plenevaux
A
A
Cyclotron Research Center, Liège University, Belgium.
Cantineau
R
R
Brihaye
C
C
Lemaire
C
C
Christiaens
L
L
Guillaume
M
M
D000588:Amines / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D000818:Animals; D001923:Brain Chemistry; D005260:Female; D006863:Hydrogen-Ion Concentration; D051381:Rats; D012643:Selenium / Q000493:pharmacokinetics*; D012644:Selenium Radioisotopes; D014018:Tissue Distribution
D000588:Amines; D012644:Selenium Radioisotopes; D012643:Selenium