1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor

Pimavanserin tartrate (Synonyms: ACP-103 tartrate)

Cat. No.: HY-14557A Purity: 99.50%
Handling Instructions

Pimavanserin tartrate (ACP-103) is a potent 5-HT 2A receptor inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively.

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

Pimavanserin tartrate Chemical Structure

Pimavanserin tartrate Chemical Structure

CAS No. : 706782-28-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 93 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 168 In-stock
Estimated Time of Arrival: December 31
100 mg USD 228 In-stock
Estimated Time of Arrival: December 31
200 mg USD 348 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
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Other Forms of Pimavanserin tartrate:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Pimavanserin tartrate (ACP-103) is a potent 5-HT 2A receptor inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively.

IC50 & Target

pIC50: 8.73 (5-HT 2A)[1]

pKi: 9.3 (5-HT 2A)[1]

In Vitro

Pimavanserin tartrate 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. ACP- 103 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 tartrate 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[1].

In Vivo

Pimavanserin tartrate 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 tartrate demonstrates 42.6% oral bioavailability in rats[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 75 mg/mL (74.61 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9948 mL 4.9741 mL 9.9483 mL
5 mM 0.1990 mL 0.9948 mL 1.9897 mL
10 mM 0.0995 mL 0.4974 mL 0.9948 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats: Thirty minutes before being placed in the startle apparatus, rats are treated with saline (s.c.), MDL-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 after the pretreatment, rats are administered either DOI HCl (0.5 mg/kg s.c.) or 0.9% saline (s.c.). The acoustic startle session lasted approximately 37 min. After 1 week, rats are tested again in the same acoustic/tactile startle session in the exact order and at the same time as the previous week. The same pretreatment drug or vehicle is administered, and rats are crossed over to receive the treatment opposite to that they received the previous 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 spontaneous activity, ACP-103 is administered alone (s.c. 60 min before session start or p.o. 60 min before session start). For hyperactivity experiments, mice are treated with 0.3 mg/kg MK-801 (i.p.) 15 min presession (the peak dose for producing hyperactivity in an inverted-U dose-effect curve as determined in pilot experiments) in combination with vehicle or ACP-103. Motor activity data are collected during a 15-min session in a lit room[1]

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

References
Molecular Weight

1005.20

Formula

C₅₄H₇₄F₂N₆O₁₀

CAS No.

706782-28-7

SMILES

O=C(NCC1=CC=C(OCC(C)C)C=C1)N(CC2=CC=C(F)C=C2)C3CCN(C)CC3.O=C(O)[[email protected]](O)[[email protected]@H](O)C(O)=O.O=C(NCC4=CC=C(OCC(C)C)C=C4)N(CC5=CC=C(F)C=C5)C6CCN(C)CC6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Pimavanserin tartrate
Cat. No.:
HY-14557A
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Pimavanserin tartrate

Cat. No.: HY-14557A