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

SKF-82958 ((±)-SKF 82958) is a dopamine D1 receptor full agonist (K_0.5=4 nM), displays selective for D1 over D2 receptors (K_0.5=73 nM). SKF-82958 induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC₅₀=491 nM)^[1].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

329.82

C₁₉H₂₀ClNO₂

80751-65-1

OC1=C(O)C=C2C(C3=CC=CC=C3)CN(CC=C)CCC2=C1Cl

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

• [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]