Pimavanserin-tartrate-ACP-103-tartrate-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPimavanserin tartrateCat. No.: HY-14557ACAS No.: 706782-28-7Synonyms: ACP-103 tartrate分式: CHFNO分量: 1005.2作靶點(diǎn): 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 m

2、onth溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 75 mg/mL (74.61 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 0.9948 mL 4.9741 mL 9.9483 mL5 mM 0.1990 mL 0.9948 mL 1.9897 mL10 mM 0.0995 mL 0.4974 mL 0.9948 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，?/p>

3、制前請(qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.49 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (2.49 mM); Clear solution1

4、/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.49 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Pimavanserin tartrate (ACP-103)種有效的 5-HT 2A 受體反向激動(dòng)劑，pIC50 和 pKi 值分別為8.73和9.3。IC50 & Target pIC50: 8.73 (5-HT 2A) 1pKi: 9.3 (5-HT 2A) 1體外研究 Pimavans

5、erin tartrate competitively antagonizes the binding of 3Hketanserin to heterologously expressedhuman 5-HT 2A receptors with a mean pKi of 9.3 in membranes and 9.70 in whole cells. ACP- 103 displayspotent inverse agonist activity in the cell-based functional assay receptor selection and amplification

6、technology (R-SAT), with a mean pIC50 of 8.7. Pimavanserin tartrate demonstrates lesser affinity (mean pKiof 8.80 in membranes and 8.00 in whole cells, as determined by radioligand binding) and potency as aninverse agonist (mean pIC50 7.1 in R-SAT) at human 5-HT 2C receptors, and lacks affinity and

7、functionalactivity at 5-HT 2B receptors, dopamine D2 receptors, and other human monoaminergic receptors 1.體內(nèi)研究 Pimavanserin tartrate attenuates head-twitch behavior (3 mg/kg p.o.), and prepulse inhibition deficits (110mg/kg s.c.) induced by the 5-HT2A receptor agonist in rats and reduces the hyperac

8、tivity induced in mice bythe N-methyl-D-aspartate receptor noncompetitive antagonist, consistent with a 5-HT 2A receptormechanism of action in vivo and antipsychotic-like efficacy. Pimavanserin tartrate demonstrates 42.6% oralbioavailability in rats 1.PROTOCOLAnimal Rats: Thirty minutes before being

9、 placed in the startle apparatus, rats are treated with saline (s.c.), MDL-Administration 1 100,151 (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 afterthe pretreatment, rats are administered either DOI HCl (0.5 mg/kg s.c.) or 0.9% saline (s.c.). The

10、acousticstartle session lasted approximately 37 min. After 1 week, rats are tested again in the same acoustic/tactilestartle session in the exact order and at the same time as the previous week. The same pretreatment drug orvehicle is administered, and rats are crossed over to receive the treatment

11、opposite to that they received theprevious 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 spontaneousactivity, ACP-103 is administered alone (s.c. 60 min before session start or p.o. 60 min befor

12、e session start).For hyperactivity experiments, mice are treated with 0.3 mg/kg MK-801 (i.p.) 15 min presession (the peakdose for producing hyperactivity in an inverted-U dose-effect curve as determined in pilot experiments) incombination with vehicle or ACP-103. Motor activity data are collected du

13、ring a 15-min session in a lit room1MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Department Neuroscience. Virginia Commonwealth University. 2016 Oct.See more customer validations on HYPERLI

14、NK / www.MedChemEREFERENCES1. 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) receptorinverse agonist. J Pharmacol Exp Ther. 2006 May;317