SKF-83566

SKF-83566 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 (Ki=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 research of parkinson’s disease and nicotine craving alleviation[5].

Product Specifications

CAS Number

[99295-33-7]

UNSPSC

12352005

Target

5-HT Receptor; Adenylate Cyclase; Dopamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/skf-83566.html

Purity

99.86

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

OC1=C(Br)C=C2CCN(C)CC(C3=CC=CC=C3)C2=C1

Molecular Formula

C17H18BrNO

Molecular Weight

332.23

References & Citations

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