Multiple actions of SC 38249: the blocker of both voltage-operated and second messenger-operated Ca2+ channels also inhibits Ca2+ extrusion

Alberto Ciardo, Jacopo Meldolesi

Research output: Contribution to journalArticlepeer-review

Abstract

((±)-1,-2,3-bis-[(4-Methoxyphenyl)-methoxy]propyl)-1H-imidazole (SC 38249) and its 4-methoxyphenetyl analogue (SKF 96365) have been recently reported to block not only voltage-operated Ca2+ channels, but also the channels (second messenger-operated) that open after receptor activation of polyphosphoinositide hydrolysis in smooth muscle fibers and platelets. Fura-2 fluorescence studies in cerebellar neurons, glial and PC12 cells confirmed these effects of SC38249 and in addition demonstrated that the drug causes an inhibition of Ca2+ extrusion, presumably via the Ca2+ ATPase. This effect was particularly evident when [Ca2+]i was increased, regardless of treatment (glutamate or ionomycin). In contrast, the NMDA receptor channel activated by glutamate was not affected by SC 38249.

Original languageEnglish
Pages (from-to)417-421
Number of pages5
JournalEuropean Journal of Pharmacology: Molecular Pharmacology
Volume188
Issue number6
DOIs
Publication statusPublished - Jun 12 1990

Keywords

  • Ca channels (second messenger-operated)
  • Ca channels (voltage-operated)
  • Ca extrusion
  • Ca influx
  • NMDA receptors

ASJC Scopus subject areas

  • Pharmacology

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