Binding of antipsychotic drugs at α1A- and α1B-adrenoceptors: risperidone is selective for the α1B-adrenoceptors

Andrew J. Sleight, Wouter Koek, Dennis C.H. Bigg

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53 Scopus citations


The binding of the antipsychotic drugs risperidone, (+)-butaclamol, clozapine, haloperidol, spiperone, thioridazine and YM-09151-2 was studied at the subtypes of the α1-adrenoceptor. Saturation experiments showed that [3H]prazosin labelled a single population of binding sites in the spleen (α1A and α1B) (dissociation constants (KD): 0.26 nM and 0.14 nM respectively). Prazosin displaced the radioligand in a monophasic manner in both the spleen and hippocampus whereas 5-methyl-urapidil, phentolamine and WB 4101 displaced the radioligand in a monophasic manner in the spleen but in a biphasic manner in the hippocampus. The affinity of these three compounds for the low affinity site in the hippocampus was similar to that observed in the spleen, suggesting that all three were selective for the α1A-adrenoceptor. Furthermore, the affinities for the α1A- and α1B-adrenoceptors calculated in this manner were in agreement with literature values. With the exception of risperidone, all the antipsychotic drugs tested failed to show selectivity for either of the α1-adrenoceptor subtypes. Risperidone was 120-fold more selective for the α1B-adrenoceptor with respect to the α1A-adrenoceptor (Ki values: 2.3 ± 1.2 nM and 283.6±174.1 nM respectively).

Original languageEnglish (US)
Pages (from-to)407-410
Number of pages4
JournalEuropean Journal of Pharmacology
Issue number2-3
StatePublished - Jul 20 1993
Externally publishedYes


  • Receptor binding
  • Risperidone
  • antipsychotics
  • α-Adrenoceptors
  • α-Adrenoceptors

ASJC Scopus subject areas

  • Pharmacology


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