Biochemical and pharmacological characterization of CGS 12066B, a selective serotonin-1B agonist

Robert F. Neale, Scott L. Fallon, William C. Boyar, Jan W F Wasley, Louis L. Martin, George A. Stone, Bruce S. Glaeser, Christopher M. Sinton, Michael Williams

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141 Scopus citations


CGS 12066B is a novel pyrroloquinoxaline with selectivity for the serotonin-1B (5HT1B) recognition site as assessed by binding, biochemical and electrophysiological studies. The compound had an IC50 value of 51 nM at the 5HT1B recognition site as determined using the binding of [3H]5HT in the presence of 1 μM spiperone. At the 5HT1A receptor the compound had an IC50 value of 876 nM, providing a 5HT1A/5HT1B ratio of 17 in contrast to the putative 5HT1B selective agent trifluoromethylphenylpiperazine (TFMPP) which had a corresponding ratio of 3.6. The compound had minimal affinity for α1-, α2- and β-adrenoceptors and for dopamine D-1 and D-2 receptors. CGS 12066B, in contrast to TFMPP, which was inactive, was found to inhibit dorsal raphe cell firing with an ED50 value of 358 nmol/kg i.v. The corresponding values for the 5HT1A selective agonists 8-OH-DPAT and ipsapirone were 1.3 and 33 nmol/kg. CGS 12066B was also effective in decreasing rat brain 5-HTP concentrations and inhibiting in vitro 5HT release. The data obtained indicate that CGS 12066B is a reasonably active 5HT1B site agonist, which due to its selectivity as compared to compounds such as TFMPP, will be a useful tool for evaluating the physiological role of such receptors in the mammalian CNS.

Original languageEnglish (US)
Pages (from-to)1-9
Number of pages9
JournalEuropean Journal of Pharmacology
Issue number1
Publication statusPublished - Apr 7 1987



  • (Binding)
  • 5HT recognition sites
  • Dorsal raphe cell firing

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Neale, R. F., Fallon, S. L., Boyar, W. C., Wasley, J. W. F., Martin, L. L., Stone, G. A., ... Williams, M. (1987). Biochemical and pharmacological characterization of CGS 12066B, a selective serotonin-1B agonist. European Journal of Pharmacology, 136(1), 1-9.