Asc-549 Spiperone hydrochloride

Biological Description

5HT and D₂ -like receptor antagonist. IC₅₀ values are 1.6 and 15 nM at 5-HT₂ and 5-HT_1C receptors respectively. K_i values are 0.06, 0.6, 0.08, ~ 350, ~ 3500 nM for D₂, D₃, D₄, D₁ and D₅ receptors respectively. Potently enhances intracellular Ca²⁺ levels. Additionally activates Ca²⁺-activated Cl^-channels (CaCC) to induce Cl^- secretion.

Useful References

Liang et al (2009) Spiperone, identified through compound screening, activates calcium-dependent chloride secretion in the airway. Am J Physiol Cell Physiol. 296:C131-41. abstract



Woodward et al (1992) Actions of dopamine and dopaminergic drugs on cloned serotonin receptors expressed in Xenopus oocytes. Proc Natl Acad Sci U S A. 89:4708-12. abstract



Lu et al (2009) Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. BMC Pharmacol. 9:13. abstract



 

Chemical Information

8-[4-(4-Fluorophenyl)-4-oxobutyl]-1-phenyl-1,3,8-triazaspiro[4,5]decan-4-one hydrochloride

• Store at RT


• MW 431.94


• Soluble in water to 10 mM and in DMSO to 100mM


• C₂₃H₂₆FN₃O₂.HCl


• 749-02-0