SKF-83566 hydrobromide is a potent,?blood-brain permeable and orally active D1-like dopamine receptor (D1DR)?antagonist and a weaker competitive antagonist at the vascular 5-HT₂?receptor (K_i=11 nM)^[1][3]. SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC₅₀?of 5.7 μM^[2]. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC₂) over AC₁ and AC₅ in the isolated rabbit thoracic aorta^[4]. SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation^[5].

SKF-83566 (0.1 μM-10 μM) causes a concentration-dependent increase in peak evoked extracellular DA concentration ([DA]_o)?evoked by single-pulse stimulation, with a maximum 65% increase in peak evoked [DA]_o with 5 μM. The EC₅₀ value of this effect of SKF-83566 is 1.3 μM^[2].
SKF-83566 inhibited [³H]DA uptake with an IC₅₀?of 5.73 μM. Moreover, SKF-83566 more potently inhibits the binding of [³H]CFT, a cocaine analog, with an IC₅₀?of 0.51 μM in [³H]DA uptake and [³H]CFT binding studies.
Similarly, in LLc-PK-rDAT cell, SKF-83566 also inhibits [³H]CFT binding with an IC₅₀?of 0.77 μM in LLc-PK-rDAT cell membrane preparations^[2].

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

SKF 83566 hydrobromide (oral administration; 20 μg/mL; 7 days) alone has no effects on altering LTP (115%). However, combinnation of SKF 83566 and nicotine significantly blocks the enhancement of long-term synaptic potentiation (LTP) induced by pretreatment with nicotine (SKF 83566+nicotine+cocaine, 120%; nicotine+cocaine, 143%)^[1].

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

413.15

C₁₇H₁₉Br₂NO

108179-91-5

Room temperature in continental US; may vary elsewhere.

• [1]. Yan-You Huang, et al.D1/D5 Receptors and Histone Deacetylation Mediate the Gateway Effect of LTP in Hippocampal Dentate Gyrus.  [Content Brief]

  [2]. Melissa A Stouffer, et al. SKF-83566, a D1-dopamine Receptor Antagonist, Inhibits the Dopamine Transporter. J Neurochem. 2011 Sep;118(5):714-20.  [Content Brief]

  [3]. E H Ohlstein, et al. SCH 23390 and SK&F 83566 are antagonists at vascular dopamine and serotonin receptors. Eur J Pharmacol. 1985 Jan 22;108(2):205-8.  [Content Brief]

  [4]. Jason M Conley, et al. Development of a high-throughput screening paradigm for the discovery of small-molecule modulators of adenylyl cyclase: identification of an adenylyl cyclase 2 inhibitor. J Pharmacol Exp Ther. 2013 Nov;347(2):276-87  [Content Brief]

  [5]. Yan-You Huang, et al. D1/D5 receptors and histone deacetylation mediate the Gateway Effect of LTP in hippocampal dentate gyrus. Learn Mem. 2014 Feb 18;21(3):153-60. doi: 10.1101/lm.032292.113.  [Content Brief]