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

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

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

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
Volume31
Issue number22
DOIs
StatePublished - Nov 29 1982
Externally publishedYes

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Carbolines
Lysergic Acid Diethylamide
Pizotyline
Serotonin Receptor Agonists
Rats
Serotonin
Fenclonine
Serotonin Antagonists
Dopamine Antagonists
Frontal Lobe
Haloperidol
Psychotic Disorders
Inhibitory Concentration 50
Brain
Animals
Substitution reactions
Tissue
Derivatives

ASJC Scopus subject areas

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

Cite this

Behavioral and biochemical evidence for serotonergic actions of tetrahydro-β-carbolines. / Nielsen, Erik B.; White, Francis J.; Holohean, Alice M.; Callahan, Patrick Michael; Appel, James B.

In: Life Sciences, Vol. 31, No. 22, 29.11.1982, p. 2433-2439.

Research output: Contribution to journalArticle

Nielsen, Erik B. ; White, Francis J. ; Holohean, Alice M. ; Callahan, Patrick Michael ; Appel, James B. / Behavioral and biochemical evidence for serotonergic actions of tetrahydro-β-carbolines. In: Life Sciences. 1982 ; Vol. 31, No. 22. pp. 2433-2439.
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