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Pimavanserin

Cat. No. M3659
Pimavanserin Structure
Synonym:

ACP-103

Size Price Availability Quantity
5mg USD 70 In stock
10mg USD 100 In stock
100mg USD 420 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Pimavanserin displays nanomolar potency as a 5-HT2A receptor inverse agonist, selectivity for 5-HT2A over 5-HT2C receptors, and no meaningful activity at any other G-protein coupled receptor. Pimavanserin demonstrates robust activity in preclinical models of schizophrenia and PDP, and do not worsen motoric symptoms, in contrast to the APDs tested. Pimavanserin showes highly significant benefits in the primary endpoint, the scale for assessment of positive symptoms-PD, a scale adapted for use in PDP. Pimavanserin is safe and well-tolerated with long-term use.

Customer Product Validations & Biological Datas
Source Neurochem Res (2014). Figure 3. Pimavanserin
Method immunofluorescence
Cell Lines animals with bilateral lesions of the SN
Concentrations
Incubation Time 24 h
Results Notably, pimavanserin not only reversed the psychosis-like behaviors, but did so without augmenting motor problems or blocking the ability of L-DOPA to improve motor behavior
Source Neurochem Res (2014). Figure 2. Pimavanserin
Method R-SATTM assays
Cell Lines NIH 3T3 cells
Concentrations 3 μM
Incubation Time
Results Pimavanserin is a potent, selective 5-HT2A inverse agonist, with selectivity over 5-HT2C receptors in binding and functional assays and little to no activity at other GPCRs in contrast to the available APDs
Protocol
Cell Experiment
Cell lines NIH-3T3 cells
Preparation method Receptor Selection and Amplification Technology.
In brief, NIH-3T3 cells were grown to 80% confluence in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% bovine calf serum (Hyclone Laboratories, Logan, UT) and 1% penicillin/streptomycin/glutamine (Invitrogen, Carlsbad, CA). Cells were transfected in roller bottles for 18 h with the relevant G protein-coupled receptor gene and the gene for β-galactosidase. After transfection, cells were trypsinized, harvested, and frozen. Aliquots of frozen cell batches were thawed and tested for response to reference agonists and inverse agonists ensuring pharmacologically appropriate responses. To initiate an assay, cells were thawed rapidly and prepared in DMEM contained 0.4% calf serum (Hyclone Laboratories), 30% UltraCulture (BioWhittaker, Rockland, ME), and 1% penicillin/streptomycin/glutamine, and then they were added to half-area 96-well microtiter plates containing either test compounds or reference ligands. After 5 days in culture, media were removed from the wells, and the cells were incubated at room temperature in 200 μl of phosphate-buffered saline, pH 7.4, with 3.5 mM o-nitrophenyl-β-d-galactopyranoside (Sigma-Aldrich, St. Louis, MO) and 0.5% Nonidet P-40 (Sigma-Aldrich). After 2 to 4 h, the plates were read at 420 nm on a plate-reader (Bio-Tek Instruments, Winooski, VT).
Concentrations 0~10 μM
Incubation time 5 days
Animal Experiment
Animal models DOI head-twitch experiments in rats and Non-Swiss albino mice
Formulation 0.9% saline
Dosages 1, 3 or 10 mg/kg
Administration s.c. or p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 427.55
Formula C25H34FN3O2
CAS Number 706779-91-1
Purity >98%
Solubility DMSO
Storage at -20°C
References

On the Discovery and Development of Pimavanserin: A Novel Drug Candidate for Parkinson's Psychosis.
Hacksell U, et al. Neurochem Res. 2014 Mar 30. PMID: 24682754.

Pimavanserin for patients with Parkinson's disease psychosis: a randomised, placebo-controlled phase 3 trial.
Cummings J, et al. Lancet. 2014 Feb 8;383(9916):533-40. PMID: 24183563.

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.
Vanover KE, et al. J Pharmacol Exp Ther. 2006 May;317(2):910-8. PMID: 16469866.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Pimavanserin, ACP-103 supplier, 5-HT Receptor, inhibitors

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