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  • Pimavanserin tartrate
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Pimavanserin tartrate

A 5-HT2A inverse agonist

价格
0-4490
Pimavanserin tartrate的二维码

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  • 货号: ajce58080
  • CAS: 706782-28-7
  • 别名: 匹莫范色林L-酒石酸盐,ACP-103 hemitartrate
  • 分子式: C54H74F2N6O10
  • 分子量: 502.59
  • 纯度: >98%
  • 溶解度: DMSO: ≥ 75 mg/mL (74.61 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

Pimavanserin is an inverse agonist of the serotonin (5-HT) receptor subtype 5-HT2A (IC50 = 1.86 nM; Ki = 0.5 nM).1 It is selective for 5-HT2A over a panel of 65 ion channels, enzymes, and receptors (Kis = >100 nM). Pimavanserin reduces head-twitch behavior and prepulse inhibition deficits induced by the 5-HT2A receptor agonist DOI in rats at doses of 3 mg/kg, p.o. and 1-10 mg/kg, s.c., respectively. It also exhibits antipsychotic-like activity, reducing hyperactivity induced by (+)-MK-801 in mice. Pimavanserin acts synergistically with haloperidol or risperidone to suppress (+)-MK-801-induced hyperactivity and attenuates haloperidol- and risperidone-induced catalepsy in rats.2 Formulations containing pimavanserin have been used for the treatment of psychosis in Parkinson's disease.3


1.Vanover, K.E., Weiner, D.M., Makhay, M., et al.Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine2A receptor inverse agonistJ. Pharmacol. Exp. Ther.318(2)910-918(2006) 2.Gardell, L.R., Vanover, K.E., Pounds, L., et al.ACP-103, a 5-hydroxytryptamine 2A receptor inverse agonist, improves the antipsychotic efficacy and side-effect profile of haloperidol and risperidone in experimental modelsJ. Pharmacol. Exp. Ther.322(2)862-870(2007) 3.Goldman, J.G., and Holden, S.Treatment of psychosis and dementia in Parkinson's diseaseCurr. Treat. Options. Neurol.16(3)281(2014)

Protocol

Animal experiment:

Rats: Thirty minutes before being placed in the startle apparatus, rats are treated with saline (s.c.), MDL-100,151 (1.0 mg/kg s.c.), or one of three doses of ACP-103 (1.0, 3.0, or 10.0 mg/kg s.c.). Five minutes after the pretreatment, rats are administered either DOI HCl (0.5 mg/kg s.c.) or 0.9% saline (s.c.). The acoustic startle session lasted approximately 37 min. After 1 week, rats are tested again in the same acoustic/tactile startle session in the exact order and at the same time as the previous week. The same pretreatment drug or vehicle is administered, and rats are crossed over to receive the treatment opposite to that they received the previous week (e.g., DOI HCl for week 1, 0.9% saline for week 2)[1]. Mice: Non-Swiss albino mice are used for locomotor activity experiments. For determination of spontaneous activity, ACP-103 is administered alone (s.c. 60 min before session start or p.o. 60 min before session start). For hyperactivity experiments, mice are treated with 0.3 mg/kg MK-801 (i.p.) 15 min presession (the peak dose for producing hyperactivity in an inverted-U dose-effect curve as determined in pilot experiments) in combination with vehicle or ACP-103. Motor activity data are collected during a 15-min session in a lit room[1]

参考文献:

[1]. Vanover KE, et al. Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP- 103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist. J Pharmacol Exp Ther. 2006 May;317(2):910-8.

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