Ki | |||
---|---|---|---|
ERG2p S. cerevisiae [3H] Ifenprodil | ς1 Receptor C. porcellus (+)-[3H] Pentazocine | EBP H. sapiens [3H] Ifenprodil | |
nm | |||
Sterol isomerase inhibitors | |||
Fenpropimorph | 0.054-a | 0.0114-b | 44 ± 15 |
Tridemorph | 0.094-a | 0.0394-b | 1.3 ± 0.4 |
MDL28815 | 0.444-a | 0.484-b | <0.54 ± 0.104-c |
AY9944 | 5.84-a | 0.504-b | 12 ± 5 |
Triparanol | 1.54-a | 8.24-b | 14 ± 4 |
Tamoxifen | 1,4704-b | 344-b | 2.8 ± 1.0 |
Zuclomiphene | 1.64-b | 4.74-b | 3.0 ± 0.3 |
Enclomiphene | 1644-b | 7.74-b | 0.69 ± 0.11 |
Trifluperidol | 0.154-b | 0.834-b | 354 ± 50 |
Sterol biosynthesis inhibitors | |||
U18666A | 0.10 ± 0.02 | 1.1 ± 0.3 | 1.9 ± 0.8 |
BM15766 | 16,480 ± 3,140 | 680 ± 90 | 34,000 ± 8,200 |
Naftifine | 310 ± 25 | 880 ± 40 | 1,500 ± 40 |
Terbinafine | >50,000 | N.D. | >50,000 |
Tamoxifen analogues | |||
MDL5332 | 0.67 ± 0.24 | 3.2 ± 1.3 | 54 ± 27 |
Nafoxidine | 232 ± 101 | 30 ± 14 | 0.9 ± 0.3 |
cDNAs encoding the guinea pig ς1 receptor and the human EBP were expressed in yeast strain WA0 as described in Experimental Procedures. The affinities of the yeast ERG2p were determined as described (Moebius et al., 1996). Apparent slope factors close to 1 (0.80–1.20) were omitted for better clarity. Identical results as for the human EBP were obtained for the EBP from C. porcellus (not shown).