Pimavanserin tartrate free base · Synonyms: ACP 103

Pimavanserin hemitartrate is a potent and brain-penetrant5-HT 2A receptor inverse agonist.

For research use only. Not for human or veterinary use.

Target 5-HT Receptor

Research area Neurological Disease

Purity >99% Stock Inquire

Data Sheet SDS COA

Pimavanserin tartrate structure

CAS No.: 706782-28-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
1 g	USD 250.00	BP-02080-1g	In stock	Get quote
5 g	USD 750.00	BP-02080-5g	In stock	Get quote
10 g	Inquire	BP-02080-10g	In stock	Inquire

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Description

Pimavanserin (ACP-103) hemitartrate is a potent and brain-penetrant5-HT 2A receptor inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively.

Biological activity

In Vitro Pimavanserin hemitartrate competitively antagonizes the binding of [3H]ketanserin to heterologously expressed human 5-HT 2A receptors with a mean pKi of 9.3 in membranes and 9.70 in whole cells. Pimavanserin hemitartrate displays potent inverse agonist activity in the cell-based functional assay receptor selection and amplification technology (R-SAT), with a mean pIC50 of 8.7. Pimavanserin hemitartrate demonstrates lesser affinity (mean pKi of 8.80 in membranes and 8.00 in whole cells, as determined by radioligand binding) and potency as an inverse agonist (mean pIC50 7.1 in R-SAT) at human 5-HT 2C receptors, and lacks affinity and functional activity at 5-HT 2B receptors, dopamine D2 receptors, and other human monoaminergic receptors. In Vivo Pimavanserin hemitartrate attenuates head-twitch behavior (3 mg/kg p.o.), and prepulse inhibition deficits (1-10 mg/kg s.c.) induced by the 5-HT2A receptor agonist in rats and reduces the hyperactivity induced in mice by the N-methyl-D-aspartate receptor noncompetitive antagonist, consistent with a 5-HT 2A receptor mechanism of action in vivo and antipsychotic-like efficacy. Pimavanserin hemitartrate demonstrates 42.6% oral bioavailability in rats.

Identifiers

SMILES: [C@@H]([C@H](C(O)=O)O)(C(O)=O)O.N(CC1=CC=C(F)C=C1)(C(NCC2=CC=C(OCC(C)C)C=C2)=O)C3CCN(C)CC3
InChIKey: XTTVNKCYECPJOF-LREBCSMRSA-N

Specifications

MW (average): 577.6416
Formula: C₂₉H₄₀FN₃O₈
CAS No.: 706782-28-7
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: 4°C, sealed storage, away from moisture

Solubility

Soluble in DMSO : 100 mg/mL H2O : 50 mg/mL

Documents

References

[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.

[2].Ezzeldin E, et al. A rapid, simple and highly sensitive UPLC-MS/MS method for quantitation of pimavanserin in plasma and tissues: Application to pharmacokinetics and brain uptake studies in mice. J Chromatogr B Analyt Technol Biomed Life Sci. 2020 Apr 15;1143:122015.

Same target

Search 5-HT Receptor

Same research area

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