Table 2: Pharmacological features of ergoline DA agonists.

Ergoline derivativesNonergoline derivatives
BromocriptinePergolideCabergolineLisuride#PramipexoleRopiniroleRotigotinePiribedilApomorphine§

Tmax (hr)2.71~3 1.90.41.41.615–1810.17~1
Cmax (ng/ml)0.47 (5 mg)1.8 (138 μg)0.078 (2 mg)0.63 (0.4 mg)0.58 (0.2 mg)0.68 (0.4 mg)
t1/2 (hr)15 (8~20)15~42430.736.455~76.90.67
Protein binding (%)90~9690621590~9335~429210

D16.166.476.677.19<5<57.08<56.43
D28.30, 7.837.50, 7.599.21, 9.029.47, 9.186.02, 5.776.17, 6.037.876.88, 6.767.46, 7.08
D38.178.269.109.557.987.439.156.637.59
D46.437.237.258.346.896.078.41, 7.82, 8.226.528.36
D56.277.487.658.45<5<58.27<57.83
5-HT receptors1D > 1A > 2B1A > 2B > 2A2B > 2A > 1A1A > 1D > 2B1A > 1B > 1D1A > 1D > 2B1A ≫ 1D ≫ 2B1A > 2B2C > 1A > 2A
Adrenoreceptorsα1D > 1B > 1Aα2B > 2A > 2Cα2A > 2C > 1Bα2A > 2B = 2Cα2B > 2Aα2B > 2C > 2Aα2B > 2C > 1Aα2C > 2A > 1Dα2C > 1D > 2B

Abbreviations: Tmax, maximum drug concentration time; Cmax, maximum drug concentration; t1/2, half-life; All pharmacokinetic data are referred to package inserts of each medicines and/or Website of DailyMed (http://dailymed.nlm.nih.gov/dailymed/about.cfm) except specifically indicated. Values for affinity at D1-5, 5-HT, and adrenergic receptors are from [93, 94] (see also last footnote). The value of D2 indicates D2S and D2L, respectively.
#Pharmacokinetic data of lisuride are from [95].
Pharmacokinetic data are followed by transdermal administration.
§Pharmacokinetic data are followed by subcutaneous administration.
values of rotigotine are calculated based on Ki values (M) that are described in [93] . The value of D4 indicates D4.2, D4.4, and D4.7, respectively.