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• W1999618333 abstract "We studied the receptor binding profile of 4-methoxyphenyl 4-(3,4,5-trimethoxybenzyl)-1-piperazine acetate monofumarate monohydrate (KB-5492), a novel anti-ulcer agent, for the σ receptor in guinea-pig brain membranes. KB-5492 selectively inhibited specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding to the σ receptor (IC50 = 3.15 μM) with a pseudo-Hill coefficient of 0.3. Computer-assisted analysis revealed that KB-5492 bound to high- and low-affinity sites. Although KB-5492 had weak affinity for α2-adrenoceptors at 10 μM, it was almost inactive at a concentration of 10 μM in 33 other binding assays for receptors, second messenger system and ion channels. σ Receptor ligands such as haloperidol, DTG, (+)-3-(3-hydroxyphenol)-N-(1-propyl)piperidine (3-PPP), rimcazole and (−)-3-PPP inhibited specific [3H]DTG binding and their IC50 values were 0.003, 0.044, 0.33, 0.67 and 1.03 μM, respectively. On the other hand, various anti-ulcer agents such as cetraxate, cimetidine, omeprazole, sofalcone, sucralfate, teprenone and troxipide could hardly displace specific [3H]DTG binding at 100 μM. Scatchard-Rosenthal analysis indicated that [3H]DTG bound to a single site, and KD and Bmax values for [3H]DTG were 87 .3 nM and 679.3 fmol/mg protein, respectively. KB-5492 significantly decreased the Bmax value, but did not affect the KD value . In contrast, haloperidol and DTG significantly increased the KD values, but did not affect the Bmax values. These findings indicate that KB-5492 selectively bound to the [3H]DTG-labeled σ receptor and that other anti-ulcer agents had little affinity for the σ receptor. Furthermore, KB-5492 inhibited specific [3H]DTG binding in a non-competitive manner." @default.
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• W1999618333 date "1994-05-01" @default.
• W1999618333 modified "2023-09-25" @default.
• W1999618333 title "Receptor binding profiles of KB-5492, a novel anti-ulcer agent, at σ receptors in guinea-pig brain" @default.
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• W1999618333 doi "https://doi.org/10.1016/0014-2999(94)90558-4" @default.
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