rac-Rotigotine hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

多巴胺 D3 受体的非选择性激动剂 (Ki=0.71 nM)；对 D3 受体的选择性是 D2、D4 和 D5 受体的 10 倍，对 D3 受体的选择性是 D1 受体的 100 倍。

A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM); has 10-fold selectivity for the D3 receptor over the D2, D4, and D5 receptors and 100-fold selectivity for the D3 receptor over the D1 receptor; behaves as a full agonist of D1, D2, and D3 with similar potencies (EC50) in functional assay; also demonstrates significant affinity at α-adrenergic (α2B, Ki=27 nM) and serotonin receptors (5-HT1A Ki=30 nM); significantly attenuates MPTP-induced acute cell degeneration in mouse model.Parkinson's Disease Approved.

Rotigotine has a 10-fold selectivity for D3 (pKi=9.2) receptors compared with D2, D4 and D5 (pKi=8.5-8.0) and a 100-fold selectivity compared with D1 receptors (pKi=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 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.

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GPCR/G Protein

Dopamine Receptor

Dopamine Receptor

Neurological Disease

Parkinson Disease

102120-99-0

351.9338

C19H26ClNOS

>98% (HPLC)

10 mM in DMSO

OC1=C2CCC(N(CCC)CCC3=CC=CS3)CC2=CC=C1.[H]Cl

1-Naphthalenol, 5,6,7,8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years