FG 7142: is this validated tool to study anxiety now forgotten?

  • R. HorowskiEmail author
Psychiatry and Preclinical Psychiatric Studies - SHORT COMMUNICATION


We describe the first human experience with FG 7142, a drug which in a phase I study has caused severe anxiety attacks and which therefore could be a validated tool for further experimental studies of anxiety.


FG 7142 Anxiety attacks 



I have to thank my good friend Peter Riederer, founder and president of WASAD because he has asked me to publish this short communication. Christian Riederer helped me a lot with this publication. This work is dedicated to Moussa B H Youdim, an outstanding scientist and very good friend, on the occasion of his 80th birthday.


  1. Adamec RE (1998) Evidence that NMDA-dependent limbic neural plasticity in the right hemisphere mediates pharmacological stressor (FG-7142)-induced lasting increases in anxiety-like behavior: study 3-the effects on amygdala efferent physiology of the block of NMDA receptors prior to injection of FG-7142 and its relationship to behavioral change. J Psychopharmacol 12:227–238CrossRefGoogle Scholar
  2. Braestrup C, Nielsen M, Olsen CE (1980) Urinary and brain beta-carboline-B-carboxylates as potent inhibitors of brain benzodiazepine receptors. Proc Natl Accad Sci USA Biol Sci 77:2288–2292CrossRefGoogle Scholar
  3. Braestrup C, Schmiechen R, Neef G, Nielsen M (1982) Benzodiazepine receptor ligands, memory and information processing. Science 216:1224–1243CrossRefGoogle Scholar
  4. Cravley JN, Ninan PT, Pickar D, Chrousos GP, Linnoila M, Skolnick P, Paul SM (1985) Neuropharmacological antagonism of the beta-carboline induced ‘anxiety’ response in rhesus monkeys. J Neurosci 5:477–485CrossRefGoogle Scholar
  5. Dorow R, Duka T (1986) Anxiolytic and anxiogenic β-carbolines: tools for the study of anxiety mechanisms. Adv Biochem Psychopharmacol 41:211–225PubMedGoogle Scholar
  6. Dorow R, Horowski R, Paschelke G, Amin M (1983) Severe anxiety induced by FG 7142, a beta-carboline ligand for benzodiazepine receptors. Lancet 2:98–99CrossRefGoogle Scholar
  7. Dorow R, Berenberg D, Duka T, Sauerbrey N (1987) Amnestic effect of lormetazepam and their reversal by the benzodiazepine antagonist Ro 15–1788. Psychopharmacol (Berl) 93:507–514CrossRefGoogle Scholar
  8. File SE, Pellow S, Braestrup C (1985) Effects of the beta-carboline, FG 7142, in the social interaction test of anxiety and the holeboard: correlations between behaviour and plasma concentrations. Pharmacol Biochem Behav 22:941–944CrossRefGoogle Scholar
  9. Horowski R, Dorrow R (2002) Anxiogenic, not psychotogenic, properties of the partial inverse benzodiazepine receptor agonist FG 7142 in man. Psychopharmacology 162:223–224CrossRefGoogle Scholar
  10. Plato (ca. 350 BC) (2015) Nomoi/Laws 1 and 2 line 649a. Clarendon Platon Series, OxfordGoogle Scholar
  11. Sarter M, Bruno JP, Bengtsson GG (2001) Psychotogenic properties of benzodiazepine receptor inverse agonists. Psychopharmacology 156:1–13CrossRefGoogle Scholar
  12. Stephens DN, Turski L (1993) Kindling to the benzodiazepine receptor inverse agonist, FG 7142: evidence for involvement of NMDA- but not non-NMDA-glutaminergic receptors. Neuropharmacology 32:1011–1017CrossRefGoogle Scholar
  13. Takamatsu H, Noda A, Kurumadji A, Murakami Y, Tastsumi M, Ichose R, Nishimura S (2003) A PET study following treatment with a pharmacological stressor, FG 7142, in conscious rhesus monkeys. Brain Res 980:275–280CrossRefGoogle Scholar
  14. Thiebot MH, Richard G, Puech AJ (1988) Anxiogenic properties of beta-CCE and FG 7142: a review of promises and pitfalls. Psychopharmacology (Berlin) 94:452–463CrossRefGoogle Scholar
  15. Zewde AM, Yu F, Nayak S, Tallarida C, Reitz AB, Kry LG, Rawls SM (2018) PLDT (planarian light/dark test): an invertebrate assay to quantify defensive responding and sticky anxiety-like effects. J Neurosci Methods 293:284–288CrossRefGoogle Scholar

Copyright information

© Springer-Verlag GmbH Austria, part of Springer Nature 2020

Authors and Affiliations

  1. 1.Antaxios GmbHWildenbruchGermany

Personalised recommendations