TABLE 1

Half-life and pharmacological profile of the dopamine agonists tested in clinical trials cited in this article

Affinities are provided as the pKi [except for l-DOPA, where affinities are provided as the pIC50 (half-maximal inhibitory concentration)] and are from Sokoloff et al., 1990, Sunahara et al., 1991, Van Tol et al., 1991, Newman-Tancredi et al., 1997, Millan et al., 2002, Newman-Tancredi et al., 2002, Scheller et al., 2009, and Alachkar et al., 2010, whereas half-lives are from Taylor and Laverty, 1969, Cedarbaum, 1987, Gancher et al., 1987, Uitti and Ahlskog, 1996, Wright et al., 1997, Fariello, 1998, Kaye and Nicholls, 2000, Stocchi et al., 2001, and Cawello et al., 2009. Values for dopamine and l-DOPA are provided for comparison purposes. Because the drugs A-77,636 and ABT-431 (adrogolide) are not used in clinic, they are not included.

Half-LifeD1D2D3D4D5
hours
Apomorphine (Apokyn)0.756.43D2S (7.46), D2L (7.08)7.598.367.83
Bromocriptine (Parlodel)3–86.16D2S (8.30), D2L (7.83)8.176.436.27
Cabergoline (Dostinex)65–1106.67D2S (9.21), D2L (9.02)9.107.257.65
Dopamine1.25–4.85.63D2: 6.327.607.556.64
l-DOPA (Sinemet)1.5–25.59D2: 6.04<5
Lisuride (Dopergin)1–77.19D2S (9.47), D2L (9.18)9.558.348.45
Pergolide (Permax)3–46.47D2S (7.50), D2L (7.59)8.267.237.48
Pramipexole (Mirapex)10–16< 5D2S (6.02), D2L (5.77)7.986.89<5
Ropinirole (Requip)5–6< 5D2S (6.17), D2L (6.03)7.436.07<5
Rotigotine (Neupro)4–77.087.779.14D4.2 (8.41), D4.4 (7.82), D4.7 (8.22)8.20