Química Nova (Jan 2006)

Polarizabilidade atômica efetiva alfad pode ditar a ionização de radioligantes 99Tc m - diaminoditiol alquilamínicos?

  • Gonçalves Marcos Moisés,
  • Fraceto Leonardo Fernandes,
  • Vila Marta Maria Duarte Carvalho,
  • Oliveira Robson Vicente Machado de

Journal volume & issue
Vol. 29, no. 5
pp. 1072 – 1077

Abstract

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Polarizability correlates well with organic ion stabilization in solution and can be defined as a measure of the relative ease of the distortion of the electronic cloud of a dipolar system exposed to an external electric field. The effective atomic polarizability, alphad, has a fundamental influence on chemical reactivity in the gas phase and in solution. In terms of chemical reactivity the charge is generated within the molecule as a positive charge due to protonation, ionization or resulting from the attack of a nucleophilic anion. In this paper, lipoidal diaminedithiol (DADT) perfusion radioligands based on 99Tc m and possessing an alkylamine side chain have been used to check the influence of alphad on their brain uptake. Some new DADT derivatives, respectively DADT-DIPA (diaminedithiol - diisopropylamine), DADT DIBA (diaminedithiol diisobutylamine), DADT-PR (diaminedithiol - branched pyperidine), have been designed to have high nitrogen alkylamine alphad values. In spite of the fact of higher alphad values having been correlated to higher brain uptakes, there isn't a clear mechanism able to trap these radioligands into the brain space.

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