SB 699551 is a selective 5-ht5a receptor antagonist (pKi values are 8.3, < 6.0, < 6.0, < 6.0, < 5.5 and < 5.5 for 5-ht5a, 5-HT1B/D, 5-HT2A, 5-HT2C, 5-HT1A and 5-HT7 receptors respectively).
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产品名称 | 5-HT ↓ ↑ | 5-HT1 ↓ ↑ | 5-HT2 ↓ ↑ | 5-HT3 ↓ ↑ | 5-HT5 ↓ ↑ | 5-HT6 ↓ ↑ | 5-HT7 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Desvenlafaxine |
++
5-HT, Ki: 40.2 nM |
98% | |||||||||||||||||
Lamotrigine |
+
5-HT (human platelets), IC50: 240 μM 5-HT (rat brain synaptosomes), IC50: 474 μM |
99%+ | |||||||||||||||||
Venlafaxine | ✔ | 99%+ | |||||||||||||||||
Fluvoxamine maleate | ✔ | 99% | |||||||||||||||||
Iloperidone | ✔ | 99%+ | |||||||||||||||||
Ziprasidone HCl | ✔ | 98+% | |||||||||||||||||
Atomoxetine HCI |
+
5-HT, Ki: 77 nM |
98% | |||||||||||||||||
Dapoxetine HCl | ✔ | 99%+ | |||||||||||||||||
Trazodone | ✔ | 98+% | |||||||||||||||||
Clomipramine HCl | ✔ | 99%+ | |||||||||||||||||
Mirtazapine | ✔ | 99+% | |||||||||||||||||
Escitalopram oxalate |
+++
5-HT, Ki: 0.89 nM |
99%+ | |||||||||||||||||
Duloxetine | ✔ | 98+% | |||||||||||||||||
Sertraline HCl |
++
5-HT, Ki: 13 nM |
99%+ | |||||||||||||||||
Citalopram HBr |
+++
serotonin reuptake, IC50: 1.8 nM |
99%+ | |||||||||||||||||
Latrepirdine 2HCl | ✔ | GluR | 99%+ | ||||||||||||||||
Fluoxetine hydrochloride | ✔ | 98% | |||||||||||||||||
Paroxetine hydrochloride | ✔ | AChR | 99%+ | ||||||||||||||||
BMY 7378 |
++
5-HT1A, pIC50: 6.4 5-HT1D, pIC50: 5.9 |
+
5-HT2, pIC50: 5.5 |
97% | ||||||||||||||||
Flibanserin |
+++
5-HT1A, Ki: 1 nM |
+
5-HT2A, Ki: 49 nM |
98% | ||||||||||||||||
LY310762 |
+
5-HT1D, Ki: 249 nM |
99%+ | |||||||||||||||||
Cyclobenzaprine HCI | ✔ | 99% | |||||||||||||||||
Blonanserin |
+++
5-HT2, Ki: 3.98 nM |
99%+ | |||||||||||||||||
Cyproheptadine HCl |
++++
5-HT2, IC50: 0.6 nM |
99+% | |||||||||||||||||
Olanzapine | ✔ | 99+% | |||||||||||||||||
Pimavanserin hemitartrate |
+++
5-HT2A, pIC50: 8.7 |
99% | |||||||||||||||||
Ketanserin |
+++
5-HT2C (Rat), Ki: 50 nM 5-HT2C (Human), Ki: 2.5 nM |
99%+ | |||||||||||||||||
Loxapine succinate |
++
5-HT2 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM |
99% | |||||||||||||||||
Agomelatine | ✔ | 99%+ | |||||||||||||||||
Clozapine | ✔ | 99%+ | |||||||||||||||||
Amitriptyline |
+
5-HT2, Ki: 235 nM |
SERT | 98% | ||||||||||||||||
PRX-08066 maleate |
+++
5-HT2B, IC50: 3.4 nM |
98+% | |||||||||||||||||
RS-127445 |
++++
5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5 |
99%+ | |||||||||||||||||
Sarpogrelate HCl |
++++
5-HT2A, Kd: 2.1 nM 5-HT2C, Kd: 1.1 nM |
98% | |||||||||||||||||
Tropisetron | ✔ | 99% | |||||||||||||||||
Palonosetron | ✔ | 98+% | |||||||||||||||||
Ramosetron HCl |
++++
5-HT3 receptor, Ki: 0.091 nM |
99%+ | |||||||||||||||||
Ondansetron | ✔ | 99% | |||||||||||||||||
Granisetron | ✔ | 98% | |||||||||||||||||
Alosetron HCl | ✔ | 98% | |||||||||||||||||
Ondansetron hydrochloride dihydrate | ✔ | 99%+ | |||||||||||||||||
VUF10166 |
++++
5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM |
99%+ | |||||||||||||||||
Azasetron hydrochloride |
++++
5-HT3, IC50: 0.33 nM |
98% | |||||||||||||||||
Asenapine maleate |
+++
5-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6 |
++++
5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46 |
+++
5-HT5A, pKi: 8.84 |
++++
5-HT6, pKi: 9.6 |
++++
5-HT7, pKi: 9.94 |
99%+ | |||||||||||||
Risperidone |
++
5-HT1D, Ki: 84.6 nM 5-HT1B, Ki: 14.9 nM |
++++
5-HT2C, Ki: 12 nM 5-HT2A, Ki: 61.9 nM |
+
5-HT5A, Ki: 206 nM |
++
5-HT7, Ki: 6.6 nM |
99%+ | ||||||||||||||
SB 271046 HCl |
+++
5-HT6, pKi: 8.92 |
99%+ | |||||||||||||||||
Intepirdine |
++++
5-HT6, pKi: 9.63 |
99%+ | |||||||||||||||||
SB-269970 HCl |
++
5-HT7, pKi: 8.3 |
98+% | |||||||||||||||||
BRL 15572 |
++
5-HT1B, pKi: 6.1 5-HT1D, pKi: 6 |
++
5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2 |
+
5-HT6, pKi: 5.9 |
+
5-HT7, pKi: 6.3 |
98% | ||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | SB-699551 is a 5-HT5A receptor antagonist. SB-699551 (0.1 mg/kg) decreased lever-press conditioned responses (CR) during short-term (STM; 1.5-h) or (3.0 mg/kg) long-term memory (LTM; 24-h); relative to the vehicle animals. SB-699551 (0.3 mg/kg) alone also produced amnesia-like effect[1]. SB-699551-A showed an anxiolytic-like property in the ultrasonic vocalization test[2]. SB-699551 has efficiency in ameliorating ketamine-induced impairments on the ASST (attentional set-shifting task) and NORT (ovel object recognition task)[3]. SB-699551 ((1-10mg/kg, i.p.) nor SB-269970 (5-HT(7) antagonist, 1-10mg/kg, i.p.) reduced the 5-HTP (5-hydroxytryptophan) and HAL(haloperidol)-induced bradykinesia or catalepsy[4]. SB-699551 significantly reduced the antinociceptive effect of both WIN 55,212-2 and morphine[5]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.71mL 0.34mL 0.17mL |
8.55mL 1.71mL 0.86mL |
17.10mL 3.42mL 1.71mL |
CAS号 | 864741-95-7 |
分子式 | C34H47Cl2N3O |
分子量 | 584.663 |
别名 | SB-699551 |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 120 mg/mL(205.25 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |