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SKF-83566 (hydrobromide)

CAT: 0804-HY-103430Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-103430Size:1 Each
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Description
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 (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 the research of parkinson’s disease and nicotine craving alleviation[5].
CAS Number
108179-91-5
UNSPSC
12352005
Hazard Statement
H302-H315-H319-H335
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-hydrobromide.html
Solubility
10 mM in DMSO
Smiles
OC1=C(Br)C=C2CCN(C)CC(C3=CC=CC=C3)C2=C1.[H]Br
Molecular Formula
C17H19Br2NO
Molecular Weight
413.15
Precautions
P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501
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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
D1 Receptor; D5 Receptor; α-1 microglobulin