[CAS NO. 706782-28-7] Pimavanserinhemitartrate

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PRODUCTS SPECIFICATIONS [706782-28-7]

Catalog

HY-14557A

Brand

MCE

CAS

706782-28-7

DESCRIPTION [706782-28-7]

Overview

MDL	-
Molecular Weight	502.59
Molecular Formula	C25H34FN3O2.1/2C4H6O6
SMILES	O=C(O)[C@H](O)[C@@H](O)C(O)=O.O=C(NCC1=CC=C(OCC(C)C)C=C1)N(CC2=CC=C(F)C=C2)C3CCN(C)CC3.[1/2]

For research use only. We do not sell to patients.

7 Publications Citing Use of MCE

Summary

Pimavanserin (ACP-103) hemitartrate is a potent 5-HT 2A receptor inverse agonist with pIC ₅₀ and pK _i of 8.73 and 9.3, respectively.

IC50 & Target

5-HT _2A Receptor

8.73 (pIC ₅₀ )

5-HT _2A Receptor

9.3 (pKi)

In Vitro

Pimavanserin hemitartrate competitively antagonizes the binding of [ ³ H]ketanserin to heterologously expressed human 5-HT 2A receptors with a mean pK _i 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 pIC ₅₀ of 8.7. Pimavanserin hemitartrate demonstrates lesser affinity (mean pK _i of 8.80 in membranes and 8.00 in whole cells, as determined by radioligand binding) and potency as an inverse agonist (mean pIC ₅₀ 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 ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT05555615	ACADIA Pharmaceuticals Inc.	Irritability Associated With Autism Spectrum Disorder	November 2, 2022	Phase 2\|Phase 3
NCT04809116	Baylor College of Medicine\|ACADIA Pharmaceuticals Inc.	Insomnia Chronic\|Posttraumatic Stress Disorder	December 15, 2022	Phase 4
NCT02035553	ACADIA Pharmaceuticals Inc.	Alzheimer´s Disease Psychosis	November 2013	Phase 2
NCT00361166	ACADIA Pharmaceuticals Inc.	Schizophrenia	August 2005	Phase 2
NCT03018340	ACADIA Pharmaceuticals Inc.	Adjunctive Treatment of Major Depressive Disorder	December 2016	Phase 2
NCT02970292	ACADIA Pharmaceuticals Inc.	Schizophrenia	October 26, 2016	Phase 3
NCT03118947	ACADIA Pharmaceuticals Inc.	Agitation and Aggression in Alzheimer´s Disease	February 23, 2017	Phase 2
NCT00087542	ACADIA Pharmaceuticals Inc.	Hallucinations\|Psychoses\|Parkinson´s Disease	March 2004	Phase 2
NCT03994965	Bjorn H. Ebdrup\|Rigshospitalet, Denmark\|GCP unit, Copenhagen University Hospital\|ACADIA Pharmaceuticals Inc.\|University of Copenhagen	Schizophrenia\|Psychosis	January 2020	Phase 2
NCT04794413	Joseph Jankovic\|Andrew Billnitzer, MD\|Baylor College of Medicine	Tourette Syndrome\|Tardive Dyskinesia	November 12, 2018	Early Phase 1
NCT03325556	ACADIA Pharmaceuticals Inc.	Dementia-related Psychosis	September 27, 2017	Phase 3
NCT01174004	ACADIA Pharmaceuticals Inc.	Parkinson´s Disease Psychosis	July 2010	Phase 3
NCT04373317	VA Office of Research and Development	Parkinson´s Disease Psychosis	October 24, 2022	Phase 4
NCT05590637	The University of Texas Health Science Center at San Antonio\|Alzheimer´s Association	Parkinson´s Disease Psychosis\|Dementia With Lewy Bodies	April 22, 2022	Phase 4
NCT03968159	ACADIA Pharmaceuticals Inc.	Adjunctive Treatment of Major Depressive Disorder	April 25, 2019	Phase 3
NCT01518309	ACADIA Pharmaceuticals Inc.	Parkinson´s Disease Psychosis	November 17, 2004	Phase 2
NCT03575052	ACADIA Pharmaceuticals Inc.	Neuropsychiatric Symptoms Related to Neurodegenerative Disease	May 21, 2018	Phase 3
NCT05523895	ACADIA Pharmaceuticals Inc.	Irritability Associated With Autism Spectrum Disorder	August 9, 2022	Phase 2\|Phase 3
NCT03947216	University Hospital, Strasbourg, France\|NS-PARK\|EUCLID Clinical Trial Platform\|F-CRIN	Parkinson Disease	October 23, 2020	Phase 2
NCT03482882	ACADIA Pharmaceuticals Inc.	Treatment of Depression in Adults With Parkinson´s Disease (PD)	March 9, 2018	Phase 2
NCT00086294	National Institute of Neurological Disorders and Stroke (NINDS)\|National Institutes of Health Clinical Center (CC)	Parkinson´s Disease\|Dyskinesias	June 25, 2004	Phase 2
NCT05441280	VA Office of Research and Development\|ACADIA Pharmaceuticals Inc.	Post-traumatic Stress Disorder\|Insomnia	January 9, 2023	Phase 2
NCT04531982	ACADIA Pharmaceuticals Inc.	Schizophrenia	August 5, 2020	Phase 3
NCT04292223	ACADIA Pharmaceuticals Inc.	Parkinson Disease Psychosis	February 10, 2020	Phase 4
NCT04188392	Baylor College of Medicine	Post-traumatic Stress Disorder\|Insomnia	January 6, 2020	Phase 4
NCT03623321	ACADIA Pharmaceuticals Inc.	Neuropsychiatric Symptoms Related to Neurodegenerative Disease	July 17, 2018	Phase 3
NCT00550238	ACADIA Pharmaceuticals Inc.	Parkinson´s Disease Psychosis	July 2007	Phase 3
NCT04164758	ACADIA Pharmaceuticals Inc.	Parkinson´s Disease	October 23, 2019	Phase 2
NCT02992132	ACADIA Pharmaceuticals Inc.	Agitation and Aggression in Alzheimer´s Disease	November 2016	Phase 2
NCT00658567	ACADIA Pharmaceuticals Inc.	Parkinson´s Disease Psychosis	March 2008	Phase 3
NCT02970305	ACADIA Pharmaceuticals Inc.	Schizophrenia	November 4, 2016	Phase 2
NCT04000009	ACADIA Pharmaceuticals Inc.	Adjunctive Treatment of Major Depressive Disorder	June 6, 2019	Phase 3
NCT05357612	Vanderbilt University Medical Center\|ACADIA Pharmaceuticals Inc.	Neurodegenerative Diseases\|Parkinson Disease\|Parkinson Disease Psychosis	November 2022	Phase 4
NCT02762591	ACADIA Pharmaceuticals Inc.	Parkinson´s Disease Psychosis
NCT03121586	ACADIA Pharmaceuticals Inc.	Schizophrenia	January 2017	Phase 3
NCT00477672	ACADIA Pharmaceuticals Inc.	Parkinson´s Disease Psychosis	June 2007	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 75 mg/mL ( 149.23 mM )

H ₂ O : 50 mg/mL ( 99.48 mM ; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9897 mL	9.9485 mL	19.8969 mL
5 mM	0.3979 mL	1.9897 mL	3.9794 mL
10 mM	0.1990 mL	0.9948 mL	1.9897 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.14 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.14 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.14 mM); Clear solution

* All of the co-solvents are available by MCE.

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 inve

Synonyms

Urea, N-[(4-fluorophenyl)methyl]-N-(1-methyl-4-piperidinyl)-N′-[[4-(2-methylpropoxy)phenyl]methyl]-, (2R,3R)-2,3-dihydroxybutanedioate (2:1)

Pimavanserin tartrate

ACP 103