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Overview
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Background
Siramesine（Lu 28-179）is a specific agonist of sigma (σ) receptor [1].Siramesine（Lu 28-179）has been reported to specific bind to σ2 receptor in human cortical and rat brain homogenates with Kd values of 1.1±0.2nM, 2.2 ±0.4nM and moderate capacity Bmax values of 26±3 fmol mg tissue-1,50±12 fmol mg tissue-1, respectively. In addition, Siramesine has shown the ligand selectivity profile of [3H]Lu28-179 binding to rat and human brain membranes with Ki values of 4.4±1.7nM and 8.6±0.6 nM, respectively. Apart from these, Siramesine has been revealed to displace [3H]DTG binding with very high affinity and [3H](+)pentazocine binding of σ2-sites. The IC50 of Siramesine inhibited the [3H]DTG binding is 0.19nM [1].
[1] Søby KK1, Mikkelsen JD, Meier E, Thomsen C. Lu 28-179 labels a sigma(2)-site in rat and human brain. Neuropharmacology. 2002 Jul;43(1):95-100.
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