Novel non-benzodiazepine anxiolytics

  title={Novel non-benzodiazepine anxiolytics},
  author={Morton E. Goldberg and Andre I. Salama and Jitendra B. Patel and Jeffrey B. Malick},
Pharmacology of pyrazolopyridines
Limited anxiolytic-like effects of non-benzodiazepine hypnotics in rodents
The present experiments demonstrate that, although selective ω 1-BZD receptor hypnotics display anxiolytic-like activity, the effects are generally weaker than those observed with non-selective ω-BzD receptor selective hypnotics such as triazolam or zopiclone.
Fenobam: A Clinically Validated Nonbenzodiazepine Anxiolytic Is a Potent, Selective, and Noncompetitive mGlu5 Receptor Antagonist with Inverse Agonist Activity
The non-GABAergic activity of fenobam, coupled with its robust anxiolytic activity and reported efficacy in human in a double blind placebo-controlled trial, supports the potential of developing mGlu5 receptor antagonists with an improved therapeutic window over benzodiazepines as novel anxIOlytic agents.
Behavioral effects of non‐opioid antitussive anticonvulsants
The non‐opioid antitussive anticonvulsants were devoid of significant behavioral effects at the ED50 does and did not possess the anxiolytic activity of benzodiazepine or barbiturate anticonVulsants.
Can drug effects on anxiety and convulsions be separated?
  • S. Pellow
  • Psychology
    Neuroscience & Biobehavioral Reviews
  • 1985
Enhancement of GABA binding by the benzodiazepine partial agonist CGS9896.
Pro‐ and anti‐convulsant drug effects in combination with the convulsant benzodiazepine Ro 5–4864
  • S. Pellow, S. File
  • Biology, Chemistry
    The Journal of pharmacy and pharmacology
  • 1985
The effects of several compounds believed to act at the GABA‐benzodiazepine receptor complex and which have anticonvulsant or proconvulsant properties when administered in combination with picrotoxin and pentetrazol were investigated in combination without affecting convulsions induced by Ro 5–4864.
Recent developments in 5HT-related pharmacology of animal models of anxiety
  • C. Gardner
  • Biology, Psychology
    Pharmacology Biochemistry and Behavior
  • 1986


Selective antagonists of benzodiazepines
The main properties of a representative of this novel class of specific benzodiazepine antagonists are described, whose unique pharmacological activity is to prevent or abolish in a highly selective manner at the receptor level all the characteristic centrally mediated effects of active Benzodiazepines.
GABAergic modulation of benzodiazepine binding site sensitivity
GA can modulate the responsiveness of this BZ binding site since the addition of GABA to cortical membranes in vitro results in an increased affinity of the 3H-diazepam binding site for its ligand.
Enhancement of 3H-diazepam binding by SQ 65,396: A novel anti-anxiety agent