For research use only. Not Intended for Therapeutic Use!
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rac-Rotigotine Hcl is a high potency and selectivity agonist for D-2 receptor with Ki of 0.69 nM.
IC50 Value: 0.69 nM(Ki)
Target: D-2 receptor
in vitro: rac-Rotigotine showed high potency (Ki = 0.69 nM) and selectivity for D-2 receptors as compared to its potency and selectivity at various other neuronal receptors (Ki in nM): D-1 (678) dopamine, alpha 1-(534) and alpha 2-(195) adrenoceptor, S1-(6940) and S2-(5900) serotonin and muscarine (2660). Very low activity (Ki greater than 10(-5) M) was seen at the beta-adrenoceptor, A1-adenosine, GABAA and benzodiazepine receptors. Furthermore, rac-Rotigotine inhibited the calcium-dependent release of [3H]dopamine (IC50: 4 nM) and [3H]acetylcholine (IC50: 6.3 nM) from rabbit striatal slices in the nanomolar range. These effects of rac-Rotigotine were mediated through activation of D-2 dopamine autoreceptors and D-2 dopamine heteroreceptors, respectively.
in vivo: Presynaptic dopaminergic activity in vivo was measurable as an inhibition of the locomotor activity of mice, and in this model rac-Rotigotine was more effective than apomorphine. Moreover, the effect of rac-Rotigotine could be antagonized by sulpiride but not by yohimbine. rac-Rotigotine was equipotent with apomorphine in inducing circling behaviour in 6-OHDA-lesioned rats. rac-Rotigotine had almost no serotonergic activity in vivo.
. Belluzzi et al (2004) N-0923, a selective dopamine D2 receptor agonist, is efficacious in rat and monkey models of Parkinson/'s disease. Mov.disord. 9 147.
. Scheller et al (2009) The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson/'s disease. Naunyn.Schmiedebergs.Arch.Pharmacol. 379 73.
. Oertel W, Lewitt P, Giladi N, Ghys L, Grieger F, Boroojerdi B.Treatment of patients with early and advanced Parkinson/'s disease with rotigotine transdermal system: Age-relationship to safety and tolerability.Parkinsonism Relat Disord. 2012 Sep 3.
. Rocchi C, Pierantozzi M, Pisani V, Marfia GA, Di Giorgio A, Stanzione P, Bernardi G, Stefani A.The Impact of Rotigotine on Cardiovascular Autonomic Function in Early Parkinson/'s Disease.Eur Neurol. 2012 Aug 28;68(3):187-192. Abstract
. Wang A, Wang L, Sun K, Liu W, Sha C, Li Y.Preparation of Rotigotine-Loaded Microspheres and Their Combination Use with L-DOPA to Modify Dyskinesias in 6-OHDA-Lesioned Rats.Pharm Res. 2012 Sep;29(9):2367-76.