Table 2

[3H]R214127 is specific for the mGlu1 receptor relative to the mGlu2, -3, -4, -5 or -6 receptor

SBmGlu1Wild-TypemGlu2mGlu3mGlu4mGlu5mGlu6
fmol/mg of protein
R193845 as blank6057  ± 1456650082380
Various blanksN.D.N.D.342-a 02-a 572-b 02-c 02-a

The specific binding of 20 nM [3H]R214127 to 40 μg of membranes from wild-type (CHO-dhfr) cells or from CHO-dhfr cells expressing rat mGlu2, -3, -4, -5, or -6 receptors is compared with binding of 10 nM [3H]R214127 to 20 μg of rat mGlu1a receptor CHO-dhfr membranes. Various compounds were used to define nonspecific binding. Specific binding (SB) data from rat mGlu1a receptor CHO-dhfrmembranes are the mean ± S.D. of three experiments performed in duplicate. Other SB data are the mean of duplicate determinations from one experiment.

  • N.D., not determined.

  • 2-a 1 mM glutamate was used to determine non-specific binding.

  • 2-b 0.1 mMl-serine-O-phosphate was used to determine nonspecific binding.

  • 2-c 10 μM MPEP was used to determine non-specific binding.