Table 4.
Ergot |
Ki (μM)
|
|||
---|---|---|---|---|
D ligand |
S ligand |
|||
DS-MIPa) | Rat hypothalamusb) | DS-MIPa) | Rat hypothalamusb) | |
Terguride | 0.14 ± 0.01 | 0.00003 ± 0.000005 | 7.79 ± 0.17 | 0.0013 ± 0.0001 |
Pergolide | 0.20 ± 0.01 | 0.0007 ± 0.0001 | 12.78 ± 0.09 | 0.0060 ± 0.0002 |
Agroclavine | 0.40 ± 0.01 | 0.0015 ± 0.0002 | 5.31 ± 0.22 | 0.0012 ± 0.0001 |
Ergonovine | 69.57 ± 0.51 | 0.0025 ± 0.0001 | 14.74 ± 0.29 | 0.0012 ± 0.0001 |
Ergocryptine | 124.88 ± 1.22 | 0.0028 ± 0.0002 | 24.85 ± 0.69 | 0.0100 ± 0.0004 |
Ergocristine | 141.08 ± 1.47 | 0.0076 ± 0.0001 | 19.33 ± 0.60 | 0.0068 ± 0.0002 |
Ergocornine | 216.60 ± 2.59 | 0.0104 ± 0.0002 | 27.25 ± 0.78 | 0.0200 ± 0.0001 |
Displacement studies using 25 mg of polymer particulate with ergot concentration ranging from 0.02 to 500 μg/mL (0.03–890.20 μM) and 6.25 μg of D (or S) in a final volume of 5 mL (D = 6.60 μM, S = 5.90 μM) were performed at room temperature (28 ± 1 °C) as described in the Experimental Section. Mean ± SD, n = 3.
Displacement studies using 10 mg of protein with ergot concentration ranging from 0.1 to 500 μg/mL (0.16–890.20 μM) and 0.25 μmole of D (or S) in a final volume of 1 mL (250 μM) were performed at 37 °C as described in the Experimental Section. Mean ± SD, n = 4.