Isamoltane hemifumarate

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CAS NO:	874882-92-5
包装:	5mg

产品介绍

Isamoltane hemifumarate 是一种选择性的5-HT_1B受体拮抗剂，抑制 [¹²⁵I]ICYP 与大鼠脑膜中 5-HT_1B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-HT_1Breceptor, with anIC₅₀of 39 nM for inhibits the binding of [¹²⁵I]ICYP to 5-HT_1Brecognition 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-HT_1BReceptor

39 nM (IC₅₀)

体外研究
(In Vitro)

Isamoltane exhibits 27-fold selectivity for the 5-HT_1Breceptor over 5-HT_1A(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.