Pimavanserin tartrate 是一种有效的5-HT 2A受体反向激动剂,pIC50和pKi值分别为8.73和9.3,用于治疗与帕金森病相关的精神病。
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Pimavanserin is an effective and specific serotonin 5-HT2A inverse agonist (pIC50: 8.73), used in the therapy of psychosis associated with Parkinson's disease.
体内活性
In rats, Pimavanserin (3 mg/kg, p.o.) attenuates DOI-induced head twitches. In mice, Pimavanserin (3 mg/kg, p.o.) significantly attenuates MK-801-induced hyperactivity. [1] In a rat model of parkinsonian tremor, Pimavanserin (40 mg/kg, i.p.) produces a significant overall reduction of tacrine-induced tremulous jaw movements. [2]
Cas No.
706782-28-7
分子式
C54H74F2N6O10
分子量
1005.215
别名
Nuplazid;匹莫范色林;ACP-103 tartrate;Pimavanserin;ACP-103;Pimavanserin tartrate
储存和溶解度
Ethanol:93 mg/mL (92.5 mM)
DMSO:93 mg/mL (92.5 mM)
H2O:92 mg/mL (91.5 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years