SKF-82958 ((±)-SKF 82958) 是多巴胺

SKF-82958  (Synonyms: (±)-SKF-82958; Chloro-APB)

SKF-82958 ((±)-SKF 82958) 是多巴胺 D1 受体激动剂 (K_0.5=4 nM)，对 D1 受体有选择性(K_0.5=73 nM)。SKF-82958 诱导大鼠纹状体膜多巴胺 D1 受体依赖性腺苷酸环化酶活性(EC₅₀=491 nM)。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
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生物活性    
SKF-82958 ((±)-SKF 82958) is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM)[1].

体内研究
(In Vivo)    
SKF-82958 ((±)-SKF 82958) (0.003-0.1 mg/kg; i.p.) results in dose-dependent increases in responding on the SKF-82958 appropriate lever, with full substitution following administration of the SKF-82958 training dose 0.03 mg/kg. Increasing the dose of SKF-82958 also results in a significant reduction in response rate[2].
SKF-82958 (0.5-2.0 mg/kg; i.p) significantly suppresses pilocarpine-induced jaw movements[3].


Animal Model:    Male Sprague-Dawley rats[3]
Dosage:    0.5-2.0 mg/kg
Administration:    I.p
Result:    Significantly reduced the number of tremulous jaw movements induced by 4.0 mg/kg pilocarpine.

分子量    
329.82

Formula    
C19H20ClNO2

CAS 号    
80751-65-1

运输条件    
Room temperature in continental US; may vary elsewhere.

储存方式    
Please store the product under the recommended conditions in the Certificate of Analysis.
 

参考文献

[1]. Mottola DM, et al. Conformational analysis of D1 dopamine receptor agonists: pharmacophore assessment and receptor mapping. J Med Chem. 1996;39(1):285-296.  [Content Brief] [2]. Haile CN, et al. The dopamine D(1) receptor agonist SKF-82958 serves as a discriminative stimulus in the rat. Eur J Pharmacol. 2000;388(2):125-131.  [Content Brief] [3]. Mayorga AJ, et al. Striatal and nigral D1 mechanisms involved in the antiparkinsonian effects of SKF-82958 (APB): studies of tremulous jaw movements in rats. Psychopharmacology (Berl). 1999;143(1):72-81.  [Content Brief]