化学性质：                                                                                                             

产品描述：                                                                                                            

rac-Rotigotine Hydrochloride 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 receptorin 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.

[1]. 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. [2]. 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. [3]. 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. [4]. 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. [5]. 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.

特别提醒：