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SKF 38393 hydrobromide

Names

[ CAS No. ]:
20012-10-6

[ Name ]:
SKF 38393 hydrobromide

[Synonym ]:
SKF 38393 hydrobromide
(±)-SKF 38393 hydrobromide
SKF 38393
(±)-1-phenyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol hydrobromide
(+/-)-1-phenyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol hydrobromide
7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrobromide
(+)-Muscarine iodide

Biological Activity

[Description]:

SKF 38393 hydrobromide is a selective agonist of the dopamine D1 receptor (D1DR) with an IC50 of 110 nM[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor
Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor
Research Areas >> Neurological Disease

[Target]

D1 Receptor:110 nM (IC50)


[In Vitro]

SKF 38393 hydrobromide induces a similar change in cytomorphology and increases the levels of media cAMP[2]. SKF-38393 hydrochloride (10 μM; 1 hour) induces increased threonine-phosphorylation of DA- and cAMP-regulated phosphoprotein of Mr 32 kD (DARPP-32) in cultured GC cells[2]. Western Blot Analysis[2] Cell Line: GC cells Concentration: 10 μM Incubation Time: 1 hour Result: Induced increased threonine-phosphorylation of DA- and cAMP-regulated phosphoprotein of Mr 32 kD (DARPP-32) in cultured GC cells.

[In Vivo]

SKF 38393 hydrobromide (10 mg/kg; i.p.) blocks the 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) -induced depletion of glutathione[3]. SKF 38393 hydrobromide attenuates MPTP-induced depletion of dopamine[3]. SKF 38393 hydrobromide enhances the activity of superoxide dismutase and hence mimics the action of Selegiline[3]. SKF 38393 hydrobromide enhances the frequency but not the amplitude of tetrodotoxin-resistant excitatory postsynaptic currents which argues for a presynaptic locus of D1 action[4]. Animal Model: Balb/c mice (20-25 g)[3] Dosage: 5 mg/kg, 10 mg/kg Administration: Intraperitoneal injection Result: Blocked the MPTP-induced depletion of glutathione and attenuated MPTP-induced depletion of dopamine.

[References]

[1]. Altar CA, et al. Picomolar affinity of 125I-SCH 23982 for D1 receptors in brain demonstrated with digital subtraction auto radiography. J Neurosci. 1987 Jan;7(1):213-222.

[2]. Mayerhofer A, et al. Functional Dopamine-1 Receptors and DARPP-32 Are Expressed in Human Ovary and Granulosa Luteal Cells in Vitro. J Clin Endocrinol Metab. 1999 Jan;84(1):257-64.

[3]. Muralikrishnan D, et al. SKF-38393, a dopamine receptor agonist, attenuates 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced neurotoxicity. Brain Res. 2001 Feb 23;892(2):241-7.

[4]. Bouron A, et al. The D1 dopamine receptor agonist SKF-38393 stimulates the release of glutamate in the hippocampus. Neuroscience. 1999;94(4):1063-70.

Chemical & Physical Properties

[ Molecular Formula ]:
C16H18BrNO2

[ Molecular Weight ]:
336.22400

[ Exact Mass ]:
335.05200

[ PSA ]:
52.49000

[ LogP ]:
3.66230

Related Compounds