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- W1986036557 abstract "The σ receptor ligands (+) and (−)pentazocine and BD1008 (1–100μW) were added to rat forebrain synaptosomes. Their effects on intrasynaptosomal free calcium ([Ca2++]i) levels under basal conditions and after depolarisation with high potassium buffer (45 mM KCl), veratridine (25 μM) and 4-aminopyridine (4-AP, 1 mM) were determined. The σ figands elicited significant, concentration-dependent decreases in basal [Ca2+]ni levels with an order of potency (-)pentazocine > (+)pentazocine =13131008. The o. ligands (at the maximum effective concentrations) also significantly inhibited the rise in [Ca2+]; levels produced by depolarisation with KCI, veratridine and 4-AP The effect of (+) and (-)pentazocine (100 μM) to inhibit the depolarisation-dependent increase in [Ca2+]i levels was greater when veratridine and 4-aminopyridine were used to depolarise the synaptosomes than with KCI, whereas the effect of BD1008 (100 μW) was approximately equiputent using all three depolarising agents. However, BD1008 was more potent to inhibit the KC1-induced rise in [Ca2+]i compared to (+) and (-)pentazocine. The data demonstrate for the first time that a ligands decrease [Ca2+]i levels in rat forebrain synaptosomes and this suggests a possible mechanism for the changes to neuronal protein phosphorylation and neurotransmitter release previously observed with σ figands." @default.
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- W1986036557 title "Intrasynaptosomal free calcium levels in rat forebrain synaptosomes: modulation by sigma (σ) receptor ligands" @default.
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- W1986036557 doi "https://doi.org/10.1016/0304-3940(96)12711-7" @default.
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