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  • Title: Binding of [3H]FH-510 to sigma ligand recognition sites in guinea-pig brain membranes.
    Author: Tanaka M, Kaku S, Muramatsu M, Otomo S.
    Journal: Eur J Pharmacol; 1993 Jul 06; 238(1):93-100. PubMed ID: 8104804.
    Abstract:
    We examined the characteristics of the binding of radiolabeled 5,8-dimethyl-4-(2-di-n-propylaminoethyl)carbazol monohydrochloride ([3H]FH-510), a highly potent and selective sigma ligand, to guinea-pig brain membranes. [3H]FH-510 showed saturable and reversible binding to sigma binding sites. The association rate constant (k+1) and dissociation rate constant (k-1) of [3H]FH-510 were 0.023 min-1.nM-1 and 0.081 min-1, respectively. Scatchard plot analysis showed a dissociation constant (Kd) and maximal number of binding sites (Bmax) of 6.0 +/- 0.63 nM and 1763.3 +/- 177.4 fmol/mg protein (n = 7), respectively. The rank order of potency (Ki) of several structurally dissimilar sigma ligands obtained for the displacement of [3H]FH-510 binding was highly correlated with that determined for [3H](+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ([3H](+)-3-PPP) binding. The binding of [3H]FH-510 was not influenced by histaminergic, dopaminergic, adrenergic, serotonergic or cholinergic agents at 10(-7) M. Higher [3H]FH-510 binding to brain regions was observed in the cerebellum and pons-plus-medulla. Except for the nuclear fraction, the highest level of [3H]FH-510 and [3H](+)-3-PPP binding to subcellular fractions was observed in the microsomal fraction. From these results, it is suggested that FH-510 selectively binds with high affinity to sigma binding sites in guinea-pig membranes.
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