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 journalArticle

77 Citations (Scopus)

Abstract

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
Volume132
Issue number2-3
DOIs
StatePublished - Dec 16 1986

Fingerprint

Serotonin 5-HT2 Receptors
Antidepressive Agents
Bupropion
Serotonin Receptors
Serotonin
Brain
Amoxapine
Trazodone
Buspirone
Ketanserin
Tricyclic Antidepressive Agents
Anti-Anxiety Agents
Frontal Lobe
In Vitro Techniques

Keywords

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

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro. / Wander, Theodore J.; Nelson, Albert; Haruo Okazaki, Okazaki; Richelson, Elliott.

In: European Journal of Pharmacology, Vol. 132, No. 2-3, 16.12.1986, p. 115-121.

Research output: Contribution to journalArticle

Wander, Theodore J. ; Nelson, Albert ; Haruo Okazaki, Okazaki ; Richelson, Elliott. / Antagonism by antidepressants of serotonin S1 and S2 receptors of normal human brain in vitro. In: European Journal of Pharmacology. 1986 ; Vol. 132, No. 2-3. pp. 115-121.
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