产品
编 号：F492165
分子式：C16H22N2O2.1/2C4H4O4
分子量：332.4
分子式：C16H22N2O2.1/2C4H4O4
分子量：332.4
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CAS No: 874882-92-5
产品详情
生物活性：
Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity.
体内研究：
Isamoltane (0.3-30 mg/kg; i.p) does not alter the accumulation of 5-HTP in the rat hippocampus, and increases 5-HT synthesis in cortical tissue. Isamoltane reduces 5-HTP accumulation in the striatum.Animal Model:Male Sprague-Dawley rats (200-300 g)
Dosage:0.3, 1, 3, 10, 30 mg/kg
Administration: I.p.
Result:38% reduction of 5-HTP accumulation was found with 30 mg/ kg in the striatum.Did not alter the accumulation of 5-HTP in the hippocampus.Increased 5-HT synthesis at 0.3, 1 and 3 mg/kg in cortical tissue.
体外研究：
Isamoltane exhibits 27-fold selectivity for the 5-HT1B receptor over 5-HT1A (IC50=1070 nM) in rat brain membranes.Isamoltane (0.01-10 μM) increases the [3H]-overflow elicited by electrical stimulation in a concentration-dependent manner in rat cortical slices.
Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity.
体内研究：
Isamoltane (0.3-30 mg/kg; i.p) does not alter the accumulation of 5-HTP in the rat hippocampus, and increases 5-HT synthesis in cortical tissue. Isamoltane reduces 5-HTP accumulation in the striatum.Animal Model:Male Sprague-Dawley rats (200-300 g)
Dosage:0.3, 1, 3, 10, 30 mg/kg
Administration: I.p.
Result:38% reduction of 5-HTP accumulation was found with 30 mg/ kg in the striatum.Did not alter the accumulation of 5-HTP in the hippocampus.Increased 5-HT synthesis at 0.3, 1 and 3 mg/kg in cortical tissue.
体外研究：
Isamoltane exhibits 27-fold selectivity for the 5-HT1B receptor over 5-HT1A (IC50=1070 nM) in rat brain membranes.Isamoltane (0.01-10 μM) increases the [3H]-overflow elicited by electrical stimulation in a concentration-dependent manner in rat cortical slices.
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