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Rotigotine Hydrochloride

CAS No. : 125572-93-2

MCE 站：Rotigotine Hydrochloride

产品活性：Rotigotine Hydrochloride (N-0923 Hydrochloride) 是 dopamine receptor 纯激动剂，是 5-HT1A receptor 的部分激动剂，以及 α2B-adrenergic receptor 的拮抗剂，K_i 值分别为 0.71?nM (dopamine D3 receptor)，4-15?nM (D2，D5，D4 receptors)，83?nM (dopamine D1 receptor)。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Dopamine Receptor  |  Adrenergic Receptor  |  5-HT Receptor

In Vitro: Rotigotine (N-0923) 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 (N-0923) 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). Rotigotine (N-0923) (10 ?M) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. Rotigotine (0.01 ?M) slightly protects dopaminergic neurons against MPP⁺ toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone.

In Vivo: In primed rats, Rotigotine (N-0923) (0.035, 0.1 and 0.35 mg/kg) induces contralateral turning behavior in a dose dependent manner. In drug naive rats, the turning behavior induced by Rotigotine, either alone or in combination with SCH 39166, is reduced compared to primed rats.

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