| 名称 | Sarizotan |
| 描述 | Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors. It has shown potent activity with IC 50 values of 6.5 nM for rat 5-HT 1A , 0.1 nM for human 5-HT 1A , 15.1 nM for rat D 2 , 17 nM for human D 2 , 6.8 nM for human D 3 , and 2.4 nM for human D 4.2 . |
| 体外活性 | Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC 50 value of 150 nM (E max 40% at 1 mM)[1]. |
| 体内活性 | Sarizotan (3, 10 mg/kg, po) at the higher dose slightly decreases 5-HT in the striatum and its metabolite 5-HIAA in frontal cortex and hippocampus. Sarizotan (10 mg/kg, po) substantially increases the DA metabolites DOPAC and HVA in the striatum and frontal cortex[1]. Sarizotan represents a new approach for the treatment of extrapyramidal motor complications such as l-DOPA-induced dyskinesia in Parkinson’s disease[1]. Sarizotan (10 ng and 1 μg, local administration) attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats[2]. Animal Model: Male Sprague-Dawley rats weighing 220-240 g (exhibiting a vigorous rotational response)[2]. Dosage: 1 ng, 10 ng and 1 μg in 0.3 μL solution. Administration: Administered via an injection cannula inserted to the guide cannula through the STN (V -8.4 mm from skull) with the injection cannula connected to a 10-μL syringe and mounted on a microinfusion pump for 22 consecutive days. Result: On day 23, the subthalamic administration of Sarizotan at the higher doses tested (10 ng and 1 μg) significantly decreased the total dyskinesia score in levodopa-treated rats in comparison with the rats treated only with levodopa (p<0.05, p<0.01, respectively). |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 关键字 | EMD128130 | EMD-128130 | Sarizotan |
| 相关产品 | Cefaclor monohydrate | Trifluoperazine dihydrochloride | Cinchonidine | Oxolinic acid | Citicoline | Alverine citrate | Dapoxetine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Clozapine N-Oxide | 1,8-Cineole | Octopamine hydrochloride |
