Rotigotine

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(In Vitro):Rotigotine (0.01-10 μM) slightly protects dopaminergic neurons against MPP+ toxicity dopamine, protects dopaminergic neurons against rotenone-induced cell death and significantly inhibits ROS production by rotenone.(In Vivo):Rotigotine (0.1-5 mg/kg; i.h.; for 14 days; male Sprague–Dawley rats) has antidepressant effect.

Rotigotine (0.01-10 μM) slightly protects dopaminergic neurons against MPP+ toxicity dopamine, protects dopaminergic neurons against rotenone-induced cell death and significantly inhibits ROS production by rotenone.

Rotigotine (0.1-5 mg/kg; i.h.; for 14 days; male Sprague–Dawley rats) has antidepressant effect. Animal Model:Male Sprague–Dawley rats Dosage:0.1, 0.5, 1, and 5 mg/kg Administration:Subcutaneous injection; for 14 days.Result:Had antidepressant effect at a dose of 1 mg/kg or less.

N-0923 | SPM 962

GPCR/G Protein

Dopamine Receptor

D2|D3

Neurological Disease

Parkinson Disease

99755-59-6

315.4729

C19H25NOS

>98% (HPLC)

10 mM in DMSO

CCCN(CCC1=CC=CS1)C2CCC3=C(C2)C=CC=C3O

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

(-20℃)

With Ice Pack

≥ 2 years