Preclinical pharmacology of ropinirole (SK&F 101468-A) a novel dopamine D2 agonist

S32504, a Novel Naphtoxazine Agonist at Dopamine D3/D2Receptors: I. Cellular, Electrophysiological, and Neurochemical Profile in Comparison with Ropinirole

“…In line with other dopaminergic agonists such as ropinirole (Eden et al, 1991), S32504 stereospecifically suppressed the activity of frontocortical, mesolimbic, and nigrostriatal dopaminergic pathways. Anatomical (Stanwood et al, 2000), pharmacological (Millan et al, 2000a,b), gene knockout (Sibley, 1999), and antisense (Ekman et al, 1998) studies support a major role of D 2 sites in the modulation of dopaminergic transmission (Levant, 1997;Millan et al, 2000b), and the D 2S isoform is principally involved (Centonze et al, 2002).…”

S32504, a Novel Naphtoxazine Agonist at Dopamine D3/D2 Receptors: II. Actions in Rodent, Primate, and Cellular Models of Antiparkinsonian Activity in Comparison to Ropinirole

“…One reason underlying this uncertainty is that all dopaminergic agonists therapeutically employed in the management of PD activate D 2 and D 3 receptors (Joyce, 2001;Millan et al, 2002;Newman-Tancredi et al, 2002). Indeed, even "preferential" agonists of D 3 versus D 2 receptors, such as ropinirole, engage D 2 receptors in vivo (Eden et al, 1991;Coldwell et al, 1999;Joyce, 2001;Millan et al, 2004a,b).…”

11C-Flumazenil positron emission tomography demonstrates reduction of both global and local cerebral benzodiazepine receptor binding in a patient with Stiff Person Syndrome

“…It has to be pointed out that an affection of GABA-A receptors due to drugs included in the medication of the patient (phenytoine, ropinirole and levothyroxine) has previously been described, but a significant effect related to the benzodiazepine receptor or a local receptor selectivity was not observed [2,8,17]. Moreover, there is no evidence available for long-term alterations of cerebral benzodiazepine receptor binding due to any of these drugs.…”