Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay.
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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 | Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00086294 | Parkinson's Disease ... 展开 >> Dyskinesias 收起 << | Phase 2 | Completed | - | United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 << |
NCT03152292 | - | Recruiting | September 2021 | - | |
NCT00087542 | Hallucinations ... 展开 >> Psychoses Parkinson's Disease 收起 << | Phase 2 | Completed | - | United States, California ... 展开 >> Fountain Valley, California, United States, 92708 Sunnyvale, California, United States, 94089 United States, Connecticut Danbury, Connecticut, United States, 06810 United States, Florida Pompano Beach, Florida, United States, 33060 Tampa, Florida, United States, 33606 United States, Georgia Atlanta, Georgia, United States, 30329 United States, Kansas Kansas City, Kansas, United States, 66160 United States, Maryland Elkridge, Maryland, United States, 21075 United States, New York Albany, New York, United States, 12205 United States, North Carolina Asheville, North Carolina, United States, 28806 United States, Pennsylvania Philadelphia, Pennsylvania, United States, 19107 United States, Rhode Island Pawtucket, Rhode Island, United States, 02860 United States, Tennessee Brentwood, Tennessee, United States, 37027 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.34mL 0.47mL 0.23mL |
11.69mL 2.34mL 1.17mL |
23.39mL 4.68mL 2.34mL |
CAS号 | 706779-91-1 |
分子式 | C25H34FN3O2 |
分子量 | 427.555 |
别名 | ACP-103 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 50 mg/mL(116.94 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 |