[3H]-(+)-pentazocine binding to sigma recognition sites in human cerebellum

Cyrus P. Zabetian, Julie K. Staley, Donna D. Flynn, Deborah C. Mash

Research output: Contribution to journalArticlepeer-review

16 Scopus citations


The binding characteristics of the sigma-1 selective benzomorphan [3H]-(+)-pentazocine were determined in human cerebellar membranes. Saturation binding analysis revealed two affinity sites with a KDH of 1.4 ± 0.7 nM and a KDL of 33.6 ± 11.9 nM. Kinetic studies performed at 25°C demonstrated reversible binding with association with association and dissociation rate constants determined for two classes of sites. In saturation binding studies, the addition of (+)-SKF 10,047 occluded binding of [3H]-(+)-pentazocine to high affinity sigma binding sites. The affinity profile of ligands displacing [3H]-(+)-pentazocine was consistent with the labeling of sigma-1 recognition sites with haloperidol > (+)-pentazocine > (+)-SKF 10,047 > (+)-3-PPP > DTG > (-)-pentazocine > (-)-SKF 10,047. The potency of the putative D3 receptor-selective ligand (±)-7-OH-DPAT was close to that measured for (+)-pentazocine in displacement experiments. These data suggest that [3H]-(+)-pentazocine labels sigma-1 sites in human cerebellum under appropriate assay conditions.

Original languageEnglish (US)
Pages (from-to)PL389-PL395
JournalLife Sciences
Issue number20
StatePublished - 1994


  • 7-OH-DPAT
  • D3 dopamine receptors
  • kinetics
  • ligand binding
  • sigma-1 binding sites

ASJC Scopus subject areas

  • Pharmacology


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