TABLE 1

In vitro binding profiles of ligands for 5-HT2AR, 5-HT2BR, and 5-HT2CR

Ligand5-HT2 Receptor Family
h5-HT2ARh5-HT2BRh5-HT2CR
AgonistsaAffinity KiPotency EC50Affinity KiPotency EC50Affinity KiPotency EC50
nM
5-HT16311324.86
DOI0.780.9391.46.77.9
Lorcaserin112168174943159
MK 2121023N.E.61729598214
Ro 60-017536.34475.40.96.032
WAY 163909212N.E.210118510.58
  • N.E., no effect.

  • a Published studies employed radioligand binding assays to establish the affinity (Ki) of 5-HT (Knight et al., 2004), DOI (Knight et al., 2004), lorcaserin (Thomsen et al., 2008), MK 212 (Porter et al., 1999; Cussac et al., 2002; Knight et al., 2004), and Ro 60-0175 for the 5-HT2R subtypes in h5-HT2AR– or h5-HT2CR–expressing HEK-293 (Knight et al., 2004; Thomsen et al., 2008) or h5-HT2AR–, h5-HT2BR–,or h5-HT2CR–expressing CHO-K1 clonal cell lines (Porter et al., 1999; Cussac et al., 2002), whereas the affinity of WAY 163909 for each h5-HT2R subtype was established in stably transfected CHO-K1 cells (Dunlop et al., 2005). The potencies of 5-HT, MK 212, WAY 163909 were established using agonist-stimulated intracellular calcium release with a fluorometric imaging plate reader (Porter et al., 1999; Dunlop et al., 2005) in the cell types as described above. The potencies of DOI, lorcaserin, and Ro 60-0175 were established using [3H]inositol phosphate turnover (Cussac et al., 2002; Thomsen et al., 2008); the EC50 was determined relative to 10 µM of 5-HT.