(Rac)-Rotigotine  (Synonyms: N-0437)

(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

Ki: Dopamine receptor; 5-HT receptor^[1][2]

Rotigotine has a 10-fold selectivity for D3 (pK_i=9.2) receptors compared with D2, D4 and D5 (pK_i=8.5-8.0) and a 100-fold selectivity compared with D1 receptors (pK_i=7.2). In functional studies, Rotigotine behaves as full agonist at all dopamine receptors but notably the potency for stimulation of D1 receptors is similar to that for D2 and D3 receptors (pEC₅₀ respectively: 9.0, 9.4-8.6, 9.7)^[1].
Rotigotine (10 μM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. Rotigotine (0.01 μM) slightly protects dopaminergic neurons against MPP+ toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone^[4].
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MCE has not independently confirmed the accuracy of these methods. They are for reference only.

315.47

C₁₉H₂₅NOS

92206-54-7

固体

Brown to black

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [1]. Wood M, et al. Rotigotine is a potent agonist at dopamine D1 receptors as well as at dopamine D2 and D3 receptors. Br J Pharmacol. 2015 Feb;172(4):1124-35.  [Content Brief]

  [2]. Scheller D, et al. The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):73-86.  [Content Brief]

  [3]. Fenu S, et al. In vivo dopamine agonist properties of rotigotine: Role of D1 and D2 receptors. Eur J Pharmacol. 2016 Oct 5;788:183-91.  [Content Brief]

  [4]. Radad K, et al. Neuroprotective effect of rotigotine against complex I inhibitors, MPP+ and rotenone, in primary mesencephalic cell culture. Folia Neuropathol. 2014;52(2):179-86.  [Content Brief]