Comparison of in vivo D-2 dopamine receptor binding of IBZM and NMSP in rat brain

Int J Rad Appl Instrum B. 1988;15(2):203-8. doi: 10.1016/0883-2897(88)90089-x.

Abstract

In vivo biodistribution of S- and R-isomers of [125I]IBZM in rats showed a significant initial brain uptake (3.20 and 2.67% dose/organ at 2 min, respectively). The wash-out from the brain was slower for the S-isomer. The striatum to cerebellum ratio for [125I]S-IBZM decreased with an increasing dose of cold carrier or spiperone, suggesting that the brain uptake is stereospecific and saturable, and may be related to the binding of D-2 dopamine receptors. In a dual isotope digital autoradiography study [125I]IBZM and [3H]NMSP(N-methylspiperone) show comparable regional cerebral distribution in rats.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzamides / pharmacokinetics*
  • Brain / diagnostic imaging
  • Brain / metabolism*
  • Iodine Radioisotopes
  • Male
  • Pyrrolidines / pharmacokinetics*
  • Rats
  • Receptors, Dopamine / metabolism*
  • Receptors, Dopamine D2
  • Spiperone / analogs & derivatives*
  • Spiperone / pharmacokinetics
  • Tomography, Emission-Computed
  • Tritium

Substances

  • Benzamides
  • Iodine Radioisotopes
  • Pyrrolidines
  • Receptors, Dopamine
  • Receptors, Dopamine D2
  • Tritium
  • Spiperone
  • 3-iodo-2-hydroxy-6-methoxy-N-((1-ethyl-2-pyrrolidinyl)methyl)benzamide
  • 3-N-methylspiperone