Ki | |||||
---|---|---|---|---|---|
ERG2p S. cerevisiae | ς1 Receptor C. porcellus | EBP | |||
H. sapiens | M. musculus | C. porcellus | |||
nm | |||||
(+) -Emopamil | 653-b | 13 ± 5 | 19 ± 4 | 77 ± 16 | 2.3 ± 0.6 |
(−) -Emopamil | 743-a | 46 ± 4 | 20 ± 2 | 23 ± 6 | 10 ± 3 |
(+) -Verapamil | 2,900 ± 500 | 15,100 ± 4,300 | 4,070 ± 1,120 | 3,630 ± 250 | 890 ± 110 |
(−) -Verapamil | >50,000 | 3,500 ± 1,100 | 2,690 ± 400 | 1,520 ± 100 | 2,900 ± 350 |
Trifluoperazine | 5003-a | 203 ± 4 | 3.6 ± 0.3 | 7.7 ± 2.0 | 3.9 ± 0.8 |
Opipramol | 173-a | 1.9 ± 0.6 | 3.8 ± 1.2 | 47 ± 11 | 8.5 ± 0.5 |
Amiodarone | 623-a | 11 ± 1 | 35 ± 6 | 60 ± 11 | 16 ± 1 |
Haloperidol | 0.53-a | 1.6 ± 0.3 | 350 ± 30 | 435 ± 40 | 250 ± 40 |
Ditolylguanidine | 1,9803-a | 44 ± 13 | 14,400 ± 950 | 4,300 ± 850 | 10,600 ± 2,900 |
L690404 | 4.73-b | 2.5 ± 0.3 | 2.3 ± 0.3 | N.D. | 1.0 ± 0.1 |
cDNAs encoding the guinea pig ς1 receptor and EBP from humans, mouse, and guinea pig were expressed in yeast strain WA0 as described in Experimental Procedures. Apparent slope factors were close to 1 (0.80–1.20) and were omitted for better clarity.