PD 144418 oxalate
PD 144418 oxalate is a highly potent and selective ligand of the sigma-1 (σ1) receptor, with Ki values being 0.08 and 1377 nM for σ1 and σ2 receptors, respectively. The σ1 receptor, one of two σ receptor subtypes, is a transmembrane protein widely expressed in a variety of tissues, and it is relatively concentrated in certain regions of the central nervous system. The σ receptor has been implicated in many neuronal processes, as well as in the pathophysiology of certain psychiatric disorders, including depression, schizophrenia, motor disturbances, pain, drug addiction, attention deficit disorders, and probably cancer.
References:
1. Akunne HC, Whetzel SZ, Wiley JN, et al. The pharmacology of the novel and selective sigma ligand, PD 144418. Neuropharmacology, 1997, 36(1): 51-62.
2. Guitart X, Codony X, Monroy X. Sigma receptors: biology and therapeutic potential. Psychopharmacology (Berl), 2004, 174(3): 301-319.
| Physical Appearance | Off-white solid |
| Storage | Desiccate at RT |
| M.Wt | 372.42 |
| Cas No. | 154130-99-1 |
| Formula | C18H22N2O·C2H2O4 |
| Solubility | <18.62mg/ml in DMSO |
| Chemical Name | 5-(1-propyl-1,2,5,6-tetrahydropyridin-3-yl)-3-(p-tolyl)isoxazole oxalate |
| SDF | Download SDF |
| Canonical SMILES | CCCN1CCC=C(C2=CC(C3=CC=C(C)C=C3)=NO2)C1.OC(C(O)=O)=O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Animal experiment:[1] | |
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Animal models |
Male CD-1 mice |
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Dosage form |
3, 10 and 30 mg/kg Administered intraperitoneally 60 min before oral administration of mescaline HCl |
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Applications |
Similar to other σ ligands such as haloperidol and clozapine, PD 144418 was able to antagonize mescaline-induced scratching at doses that did not alter spontaneous motor activity, with an ED50 value of 7.0 mg/kg. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Akunne HC, Whetzel SZ, Wiley JN, et al. The pharmacology of the novel and selective sigma ligand, PD 144418. Neuropharmacology, 1997, 36(1): 51-62. 2. Guitart X, Codony X, Monroy X. Sigma receptors: biology and therapeutic potential. Psychopharmacology (Berl), 2004, 174(3): 301-319. |
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Quality Control & MSDS
- View current batch:
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
