SKF 82958 ((±)-SKF 82958) ((±)-SKF 82958) 是一种多巴胺 D1 受体完全激动剂 (K0.5=4 nM)，对 D1 的选择性优于对 D2 受体 (K0.5=73 nM) ）。
SKF 82958 is a D1/D5 receptor full agonist. IC50 value:Target: D1/D5 receptorin vitro: Neuropeptide and immediate early gene expression in striatonigral neurons of the normosensitive striatum is induced by mixed D1 receptor SKF-82958, which induces behavioral activity and preprodynorphin (PPD) and substance P (SP) gene expression in medium spiny neurons in the dorsal, and especially, in the ventral striatum. in vivo:Quantitative in situ hybridization was used to examine the contribution of muscarinic receptors to the transynaptic regulation of striatal gene expression induced by D1receptor activation. The acute injection of the full D1 agonist, SKF-82958, would induce PPD, SP and PPE mRNA expression in the intact rat striatum.
[1]. Wang JQ, et al. The Full D1 Dopamine Receptor Agonist SKF-82958 Induces Neuropeptide mRNA in the Normosensitive Striatum of Rats: Regulation of D1/D2 Interactions by Muscarinic Receptors.J Pharmacol Exp Ther. 1997 May;281(2):972-82.
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