PMID- 10087012
OWN - NLM
STAT- MEDLINE
DCOM- 19990421
LR  - 20131121
IS  - 0022-3565 (Print)
IS  - 0022-3565 (Linking)
VI  - 289
IP  - 1
DP  - 1999 Apr
TI  - Molecular and ligand-binding characterization of the sigma-receptor in the Jurkat
      human T lymphocyte cell line.
PG  - 251-60
AB  - The sigma binding site present in the Jurkat human T lymphocyte cell line was
      investigated. Jurkat cell membranes were found to have a single saturable binding
      site for [3H]haloperidol, a sigma ligand (dissociation constant, 3.9 +/- 0.3 nM).
      The binding of [3H]haloperidol was inhibited by several sigma ligands. Northern
      analysis and reverse transcription-polymerase chain reaction provided evidence
      for the expression of the recently cloned type 1 sigma-receptor (sigma-R1) in
      Jurkat cells. The sigma-R1 cDNA cloned from these cells was functional in
      heterologous expression systems. When expressed in mammalian cells, the
      cDNA-induced binding was saturable with dissociation constants of 1.9 +/- 0.3 nM 
      for [3H]haloperidol and 12 +/- 2 nM for (+)-pentazocine. The binding of
      [3H]progesterone, a putative endogenous ligand to sigma-R1, to the Jurkat cell
      sigma-receptor could be directly demonstrated by using heterologously expressed
      sigma-R1 cDNA. The binding of [3H]progesterone was saturable, with a dissociation
      constant of 88 +/- 7 nM. Progesterone and haloperidol interacted with the
      receptor competitively. Reverse transcription-polymerase chain reaction also
      produced evidence for the existence of an alternatively spliced sigma-R1 variant 
      in Jurkat cells. This splice variant was found to be nonfunctional in ligand
      binding assays. This constitutes the first report on the molecular
      characterization of the sigma-receptor in immune cells.
FAU - Ganapathy, M E
AU  - Ganapathy ME
AD  - Department of Medicine, Medical College of Georgia, Augusta, USA.
FAU - Prasad, P D
AU  - Prasad PD
FAU - Huang, W
AU  - Huang W
FAU - Seth, P
AU  - Seth P
FAU - Leibach, F H
AU  - Leibach FH
FAU - Ganapathy, V
AU  - Ganapathy V
LA  - eng
GR  - DA 10045/DA/NIDA NIH HHS/United States
GR  - GM 54122/GM/NIGMS NIH HHS/United States
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - J Pharmacol Exp Ther
JT  - The Journal of pharmacology and experimental therapeutics
JID - 0376362
RN  - 0 (Dopamine Antagonists)
RN  - 0 (Ligands)
RN  - 0 (Narcotic Antagonists)
RN  - 0 (RNA, Messenger)
RN  - 0 (Receptors, sigma)
RN  - 4G7DS2Q64Y (Progesterone)
RN  - 9007-49-2 (DNA)
RN  - J6292F8L3D (Haloperidol)
RN  - RP4A60D26L (Pentazocine)
SB  - IM
MH  - Alternative Splicing
MH  - Amino Acid Sequence
MH  - Blotting, Northern
MH  - Cell Membrane/metabolism
MH  - Cloning, Molecular
MH  - DNA/biosynthesis
MH  - Dopamine Antagonists/metabolism
MH  - Haloperidol/metabolism
MH  - HeLa Cells
MH  - Humans
MH  - Jurkat Cells
MH  - Ligands
MH  - Molecular Sequence Data
MH  - Narcotic Antagonists/metabolism
MH  - Pentazocine/metabolism
MH  - Progesterone/metabolism
MH  - RNA, Messenger/biosynthesis
MH  - Receptors, sigma/biosynthesis/genetics/*metabolism
MH  - Reverse Transcriptase Polymerase Chain Reaction
MH  - Vaccinia virus/genetics
EDAT- 1999/03/23 00:00
MHDA- 1999/03/23 00:01
CRDT- 1999/03/23 00:00
PHST- 1999/03/23 00:00 [pubmed]
PHST- 1999/03/23 00:01 [medline]
PHST- 1999/03/23 00:00 [entrez]
PST - ppublish
SO  - J Pharmacol Exp Ther. 1999 Apr;289(1):251-60.