1. GPCR/G Protein
    Neuronal Signaling
  2. Sigma Receptor
  3. PD 144418

PD 144418 

Cat. No.: HY-108512
Handling Instructions

PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively), devoid of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity.

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

PD 144418 Chemical Structure

PD 144418 Chemical Structure

CAS No. : 154130-99-1

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2 mg USD 180 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively), devoid of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity[1][2].

IC50 & Target

Ki: 0.08 nM (σ1receptor) and 1377 nM (σ2 receptor)[1]

In Vitro

In vitro, PD 144418 reverses the N-methyl-D-aspartate (NMDA)-induced increase in cyclic GMP (cGMP) in rat cerebellar slices without affecting the basal levels, suggesting that σ1 sites may be important in the regulation of glutamine-induced actions. PD 144418 potentiates the decrease in 5-hydroxytryptophan caused by Haloperidol in the mesolimbic region, but by itself has no effect in 5-HT and dopamine (DA) synthesis[1].

In Vivo

PD 144418 (10 mg/kg; intraperitoneal injection; male CD-1 mice) treatment antagonizes Mescaline-induced scratching at doses that did not alter spontaneous motor activity, with PD 144418 showing ED50 values of 7.0 mg/kg i.p.[1].

Animal Model: Male CD-1 mice induced with Mescaline[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection
Result: Antagonized mescaline-induced scratching at doses that did not alter spontaneous motor activity.
Molecular Weight

282.38

Formula

C₁₈H₂₂N₂O

CAS No.

154130-99-1

SMILES

CCCN1CC(C2=CC(C3=CC=C(C)C=C3)=NO2)=CCC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PD 144418PD144418PD-144418Sigma Receptorσ1cGMP5-hydroxytryptophanantipsychotichyperactivityInhibitorinhibitorinhibit

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PD 144418
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