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. 2008 Nov 26;9(12):2333–2356. doi: 10.3390/ijms9122333

Table 4.

Displacement of D and S ligands from DS-MIP and rat hypothalamus by ergot derivatives.

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
a).

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.

b).

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.