Behavioral and biochemical evidence for serotonergic actions of tetrahydro-β-carbolines

Erik B. Nielsen, Francis J. White, Alice M. Holohean, Patrick M. Callahan, James B. Appel

Research output: Contribution to journalArticlepeer-review

12 Scopus citations


In two groups of rats trained to discriminate LSD (0.1 mg/kg or 0.24 mg/kg) from saline, tetrahydro-β-carboline (THBC; 1-12 mg/kg as free base) and its derivative 6-methoxy-THBC (1-12 mg/kg as free base) substituted partially for LSD. The substitution of THBC for 0.1 mg/kg of LSD was analyzed further with antagonism tests in 16 animals and was attenuated by the serotonin (5-HT) antagonist BC-105 (pizotifen; 3 mg/kg) but not by the dopamine (DA) antagonist haloperidol (0.1 mg/kg). It was abolished by pre-treatment with the 5-HT synthesis inhibitor p-chlorophenylalanine (100 mg/kg/day for 3 days). In addition, THBC was found to inhibit 3H-LSD binding to homogenates of rat frontal cortex with an IC50 value of 4 μM which is similar to that previously reported for other 5-HT agonists. These data indicate that THBCs exert potent 5-HT agonist actions. Since THBCs have recently been found in mammalian brain and other tissues, the present results are of interest in relation to a possible role of these substances in endogenous psychosis.

Original languageEnglish (US)
Pages (from-to)2433-2439
Number of pages7
JournalLife sciences
Issue number22
StatePublished - Nov 29 1982
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)


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