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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147 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
StatePublished - Apr 7 1987


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

ASJC Scopus subject areas

  • Pharmacology


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