Cloning and characterization of a mouse sigma1 receptor

J Neurochem. 1998 Jun;70(6):2279-85. doi: 10.1046/j.1471-4159.1998.70062279.x.


A cDNA clone (S2-1a) isolated from a mouse brain cDNA library, using a guinea pig sigma1 cDNA as probe, has high homology to the predicted protein sequence of the guinea pig (88%) and human (90%) sigma1 receptors. Northern analysis revealed a major mRNA of approximately 1.8 kb in a wide range of mouse tissues, with highest levels in brain, liver, kidney, and thymus. Southern analysis and chromosomal mapping in the mouse suggested a single-copy gene in region A5-B2 of chromosome 4. Expression of the clone in MCF-7 and CHO cells led to a pronounced increase in (+)-[3H]pentazocine binding with a selectivity profile consistent with sigma1 receptors. In vitro translation yielded a protein of approximately 28 kDa, as did transfection of a probe containing the hemagglutinin (HA) epitope (S2-1a.HA) into CHO cells, as determined by western analysis using an antibody directed against HA. (+)-[3H]-Pentazocine binding to immunopurified HA-tagged receptor demonstrated conclusively that S2-1a.HA encodes a high-affinity (+)-[3H]pentazocine binding site with characteristics of a murine sigma1 receptor. An antisense oligodeoxynucleotide designed from S2-1a potentiated opioid analgesia in vivo.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Analgesics, Opioid / pharmacology
  • Animals
  • Brain / metabolism
  • CHO Cells
  • Chromosome Mapping
  • Cloning, Molecular*
  • Cricetinae
  • Gene Expression
  • Gene Library
  • Guinea Pigs
  • Humans
  • Male
  • Mice
  • Molecular Sequence Data
  • Narcotic Antagonists / metabolism
  • Oligonucleotides, Antisense / pharmacology
  • Organ Specificity
  • Pain Measurement
  • Pentazocine / metabolism
  • Polymerase Chain Reaction
  • Recombinant Proteins / biosynthesis
  • Recombinant Proteins / genetics
  • Recombinant Proteins / metabolism
  • Tumor Cells, Cultured


  • Analgesics, Opioid
  • Narcotic Antagonists
  • Oligonucleotides, Antisense
  • Recombinant Proteins
  • Pentazocine