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Isamoltane hemifumarate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Isamoltane hemifumarate图片
CAS NO:874882-92-5
包装:5mg

产品介绍
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。
生物活性

Isamoltane hemifumarate is a selective antagonist of5-HT1Breceptor, with anIC50of 39 nM for inhibits the binding of [125I]ICYP to 5-HT1Brecognition sites in rat brain membranes. Isamoltane hemifumarate is also aβ-adrenoceptorligand, with anIC50of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity[1].

IC50& Target[1]

β-adrenoceptor

8.4 nM (IC50)

5-HT1BReceptor

39 nM (IC50)

体外研究
(In Vitro)

Isamoltane exhibits 27-fold selectivity for the 5-HT1Breceptor over 5-HT1A(IC50=1070 nM) in rat brain membranes[1].
Isamoltane (0.01-10 μM) increases the [3H]-overflow elicited by electrical stimulation in a concentration-dependent manner in rat cortical slices[1].

体内研究
(In Vivo)

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[1].

Animal Model:Male Sprague-Dawley rats (200-300 g)[1]
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.
分子量

332.40

Formula

C16H22N2O2.1/2C4H4O4

CAS 号

874882-92-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.