化合物 T22872
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- CAS号:
- 874882-92-5
- 英文名:
- Isamoltane Hemifumarate
- 英文别名:
- 中文名:
- 化合物 T22872
- 中文别名:
- 化合物 T22872
- CBNumber:
- CB14806410
- 分子式:
- C20H26N2O6
- 分子量:
- 390.44
- MOL File:
- 874882-92-5.mol
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化合物 T22872化学性质
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储存条件:
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Store at -20°C
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溶解度:
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Soluble to 10 mM in water with gentle warming
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形态:
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Powder
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化合物 T22872性质、用途与生产工艺
Isamoltane hemifumarate 是一种选择性的 5-HT1B 受体拮抗剂，抑制 [125I]ICYP 与大鼠脑膜中 5-HT1B 识别位点结合的 IC50 值为 39 nM。Isamoltane hemifumarate 也是一种 β- 肾上腺素受体配体，IC50 值为 8.4 nM。Isamoltane hemifumarate 具有抗焦虑活性。
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β-adrenoceptor
8.4 nM (IC
50
)
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5-HT
1B
Receptor
39 nM (IC
50
)
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Isamoltane exhibits 27-fold selectivity for the 5-HT
1B
receptor over 5-HT
1A
(IC
50
=1070 nM) in rat brain membranes.
Isamoltane (0.01-10 µM) increases the [
3
H]-overflow elicited by electrical stimulation in a concentration-dependent manner in rat cortical slices.
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.
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Animal Model:
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Male Sprague-Dawley rats (200-300 g)
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Dosage:
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0.3, 1, 3, 10, 30 mg/kg
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Administration:
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I.p.
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Result:
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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.
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化合物 T22872
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