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Rotigotine

CAS No. : 99755-59-6

MCE 站：Rotigotine

产品活性：Rotigotine (N-0437; N-0923) 是 dopamine receptor 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-0437; 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 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 (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-0437; 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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