Website:www.dcchemicals.

com
Email: info@dcchemicals.com Phone:+86-21-58447131
Marketing Center: Room 610,Building 15, Jinxiang Rd 201, Shanghai,
China

Datasheet of Pimavanserin

Description:
Pimavanserin(ACP-103) is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based
functional assay. in vitro: ACP-103 competitively antagonized 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. ACP-103 displayed 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. ACP-103 demonstrated 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 lacked
affinity and functional activity at 5-HT(2B) receptors, dopamine D(2) receptors, and other human monoaminergic receptors [1].
in vivo: ACP-103 attenuated head-twitch behavior (3 mg/kg p.o.), and prepulse inhibition deficits (1-10 mg/kg s.c.) induced by
the 5-HT(2A) receptor agonist (+/-)-2,5-dimethoxy-4-iodoamphetamine hydrochloride in rats and reduced the hyperactivity
induced in mice by the N-methyl-d-aspartate receptor noncompetitive antagonist 5H-dibenzo[a,d]cyclohepten-5,10-imine
(dizocilpine maleate; MK-801) (0.1 and 0.3 mg/kg s.c.; 3 mg/kg p.o.), consistent with a 5-HT(2A) receptor mechanism of action
in vivo and antipsychotic-like efficacy. Single doses of ACP-103 (20-300 mg) resulted in dose-proportionate mean C(max)
values (9-152 ng/mL) and AUC(0-infinity) (706-10 798 h x ng/mL), and multiple doses (50-150 mg) resulted in
dose-proportionate mean C(max,ss) (93-248 ng/mL) and AUC(0-infinity,ss) (1839-4680 h x ng/mL). The half-life of ACP-103
was approximately 55 hours, with a t(max) at 6 hours. ACP-103 reduced tacrine-induced tremulous jaw movements in rats. In
addition, ACP-103 administered in combination with levodopa caused a dose-related reduction in dyskinesias in monkeys.

Chemical Information
Catalog

DC8795

Purity of current batch:

>98%

Molecular Weight (MW)

427.55

Molecular Formula

C25H34FN3O2

CAS No.

706779-91-1

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.

Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.