Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro

Theodore J. Wander, Albert Nelson, Okazaki Haruo Okazaki, Elliott Richelson

Research output: Contribution to journalArticlepeer-review

79 Scopus citations


Using radioligand binding techniques and human frontal cortex, we determined the equilibrium dissociation constants (KDs) of 25 antidepressants at the serotonin S1 (probably the S1A subtype) and serotonin S2 receptors using [3H]WB4101 and [3H]ketanserin, respectively. At the serotonin S1 receptor, the most and least potent antidepressants were trazodone (KD = 60 nM) and bupropion (KD = 170 μM), respectively. At the serotonin S2 receptor, the most and least potent antidepressants were amoxapine (KD = 0.6 nM) and bupropion (KD = 90 μM), respectively. Analysis of the data revealed a relationship between structure and serotonin S1 affinity for some tricyclic antidepressants. Buspirone, a new anxiolytic agent, possessed high affinity for the serotonin S1 receptor (KD = 3.8 nM).

Original languageEnglish (US)
Pages (from-to)115-121
Number of pages7
JournalEuropean Journal of Pharmacology
Issue number2-3
StatePublished - Dec 16 1986


  • (Human)
  • Antidepressants
  • Brain
  • Buspirone
  • Ketanserin
  • Serotonin S
  • Serotonin S

ASJC Scopus subject areas

  • Pharmacology


Dive into the research topics of 'Antagonism by antidepressants of serotonin S<sub>1</sub> and S<sub>2</sub> receptors of normal human brain in vitro'. Together they form a unique fingerprint.

Cite this