Published 1990 | Version v1
Book

Iomazenil: pharmacological and animal data

  • 1. Paul Scherrer Inst. (PSI), Villigen (Switzerland)
  • 2. Hoffmann-La Roche (F.) and Co., Basel (Switzerland)

Description

The flumazenil analogue Ro 16-0154 (Iomazenil), a benzodiazepine partial inverse agonist, has been labelled by halogen exchange to enable SPECT investigations of central benzodiazepine receptors in human brain. The purified 123I-Ro 16-0154 was found to be stable in rat brain preparations and to be metabolized in rat liver preparations. Its pharmacological properties were comparable to those of flumazenil with the exception of the antagonism of diazepam versus pentylenetetrazol. Biodistribution in rats (1 h p.i.) resulted in a high brain to blood ratio of 16. Clinical studies revealed images of the bezodiazepine receptor density in the brain. (author) 9 figs., 3 tabs., 27 refs

Additional details

Publishing Information

Publisher
Editiones <Roche>.
Imprint Place
Basel (Switzerland)
ISBN
3-907946-37-3
Imprint Title
Iomazenil and other brain receptor tracers for SPECT
Imprint Pagination
135 p.
Journal Page Range
p. 9-29.

Conference

Title
6. Boettstein colloquium.
Dates
10-11 Nov 1989.
Place
Wuerenlingen/Villigen (Switzerland).