874882-92-5
中文名稱
化合物 T22872
英文名稱
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 結(jié)構(gòu)式
常見問題列表
生物活性
Isamoltane hemifumarate 是一種選擇性的 5-HT1B 受體拮抗劑，抑制 [125I]ICYP 與大鼠腦膜中 5-HT1B 識別位點(diǎn)結(jié)合的 IC50 值為 39 nM。Isamoltane hemifumarate 也是一種 β- 腎上腺素受體配體，IC50 值為 8.4 nM。Isamoltane hemifumarate 具有抗焦慮活性。靶點(diǎn)
|
β-adrenoceptor 8.4 nM (IC 50 ) |
5-HT 1B Receptor 39 nM (IC 50 ) |
體外研究
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.
體內(nèi)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. |