874882-92-5

中文名称化合物 T22872

英文名称 Isamoltane Hemifumarate

CAS 874882-92-5

分子式 C16H22N2O2.?C4H4O4

分子量 390.44

MOL 文件 874882-92-5.mol

874882-92-5 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T22872

物理化学性质

储存条件-20°C储存

溶解度Soluble to 10 mM in water with gentle warming

形态粉末

常见问题列表

生物活性

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。

靶点

β-adrenoceptor

8.4 nM (IC ₅₀ )

5-HT _1B Receptor

39 nM (IC ₅₀ )

体外研究

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.

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.