Title

Binding of σ receptor ligands and their effects on muscarine-induced Ca2+ changes in SH-SY5Y cells

Document Type

Journal Article

Publication Date

2-1-2002

Journal

European Journal of Pharmacology

Volume

436

Issue

1-2

DOI

10.1016/S0014-2999(01)01606-5

Keywords

σ Receptor; (+)-Pentazocine; Ca 2+; Haloperidol; Intracellular; Muscarine; SH-SY5Y neuroblastoma

Abstract

In human neuroblastoma SH-SY5Y cell preparations, σ1 receptor agonists (+)-pentazocine and 1S,2R-( -)-cis-N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl) cyclohexylamine (BD737) competed for [3H]haloperidol binding with Ki values of 67 ± 10 and 14 ± 10 nM, respectively. (+)-Pentazocine or BD737 up to 10 μM did not affect basal levels of intracellular Ca2+ concentration ([Ca2+]i) in these cells, but they significantly reduced muscarine-induced [Ca2+]i changes in a dose-related manner. However, the reduction by (+)-pentazocine was not reversed by the σ1 receptor antagonist haloperidol. Further studies showed (+)-pentazocine, BD737 and haloperidol could compete for [3H]quinuclidinyl benzilate binding in SH-SY5Y cells with Ki values of 0.51 ± 0.06, 0.32 ± 0.07 and 4.4 ± 2.3 μM, respectively. Thus, the inhibitory effects on muscarine-induced [Ca2+]i changes by (+)-pentazocine and BD737 in SH-SY5Y cells were likely due to blockade of muscarinic receptors, not due to σ1 receptor activation by these ligands. © 2002 Elsevier Science B.V. All rights reserved.

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