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TCS 1205 is a GABAA receptor positive allosteric modulator of the tryptamine family. It is a benzodiazepine site agonist selective for certain subunits.

Pharmacology

TCS 1205 acts at the benzodiazepine binding site, it is selective for the α1 and α2 subunits of the GABAA receptor.[1] In vivo, it has anxiolytic effects but no sedative effects.[2][3]

Chemistry

Despite acting at the benzodiazepine receptor, it does not contain the benzodiazepine structure, it could therefore be classed as a nonbenzodiazepine. The drug is a substituted tryptamine derivative.

References

  1. ^ “TCS 1205” (PDF). Certificate of Analysis. Tocris Bioscience.
  2. ^ “TCS 1205”. AbMole BioScience.
  3. ^ Taliani S, Cosimelli B, Da Settimo F, Marini AM, La Motta C, Simorini F, et al. (June 2009). “Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor”. Journal of Medicinal Chemistry. 52 (12): 3723–3734. doi:10.1021/jm9001154. PMID 19469479.