Table 2

125I-MCH/MCH competition binding and agonist-induced inositol phosphate production analysis of MCH receptor mutants transiently expressed in COS-7 cells

MCH ReceptorResidue Locus2-aIC50(nM)2-bEC50(nM ± S.E.M.)2-c
WT3318.5  ± 6.4
HA-tagged WT4630.0  ± 12.8
HA-D123AAsp 3.32NO2-d NO
HA-S126ASer 3.3545182.5  ± 95.5
HA-S171ASer 4.5343 69.0  ± 56.6
HA-S174ASer 4.5645 65.0  ± 7.1
HA-T209AThr 5.3943109.1  ± 48.7
HA-Q212AGln 5.4272151.0  ± 62.2
HA-Q276AGln 6.5551132.0  ± 48.7
HA-Q279AGln L6.5839 55.0  ± 50.2
HA-F289APhe 7.3135122.0  ± 45.0
HA-Y293ATyr 7.3550482.0  ± 396.0
HA-N294AAsn 7.3640 75.7  ± 8.0
  • 2-a Indexing nomenclature by Ballesteros and Weinstein (1995).

  • 2-b Single experiment determination in triplicate (used as a screen).

  • 2-c Average of duplicate determinations,n = 2 or 3.

  • 2-d NO, none observed.