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| 5mg |
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PD 144418 oxalate is a novel, high affinity, highly potent and specific sigma 1 (σ1) receptor ligand with Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively. PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows highly potential antipsychotic activity.
| ln Vitro |
N-methyl-D-aspartate (NMDA)-induced increases in cyclic GMP (cGMP) in rat cerebellar slices were reversed in vitro by PD 144418, without changing basal levels. This suggests that glutamine, specifically the σ1 site, may play a significant role in the control of induced cyclic GMP (cGMP). take action. PD 144418 has no effect on the synthesis of 5-HT or dopamine (DA) per se, but it amplifies the haloperidol-induced drop in 5-hydroxytryptophan in the mesolimbic region [1].
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| ln Vivo |
Male CD-1 mice treated with 10 mg/kg i.p. with PD 144418 were able to suppress mescaline-induced scratching, but the dose had no effect on spontaneous locomotor activity. The ED50 of PD 144418 is 7.0 mg/kg ip [1].
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| Animal Protocol |
Animal/Disease Models: Male CD-1 mice, induced with mescaline [1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; Experimental Results:Antagonizes mescaline-induced effects at a dose that does not change spontaneous locomotor activity Scratching. |
| References |
[1]. Akunne HC, et al. The pharmacology of the novel and selective sigma ligand, PD 144418. Neuropharmacology. 1997 Jan;36(1):51-62.
[2]. Lever JR, et al. Relationship between cerebral sigma-1 receptor occupancy and attenuation of cocaine's motor stimulatory effects in mice by PD144418. J Pharmacol Exp Ther. 2014 Oct;351(1):153-63. |
| Molecular Formula |
C₂₀H₂₄N₂O₅
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|---|---|
| Molecular Weight |
372.4150
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| CAS # |
1794760-28-3
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| Related CAS # |
PD 144418;154130-99-1
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| SMILES |
CCCN1CC(C2=CC(C3=CC=C(C)C=C3)=NO2)=CCC1.O=C(O)C(O)=O
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| InChi Key |
IWSFHSVGBKPYFN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22N2O.C2H2O4/c1-3-10-20-11-4-5-16(13-20)18-12-17(19-21-18)15-8-6-14(2)7-9-153-1(4)2(5)6/h5-9,12H,3-4,10-11,13H2,1-2H3(H,3,4)(H,5,6)
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| Chemical Name |
3-(4-Methylphenyl)-5-(1-propyl-3,6-dihydro-2H-pyridin-5-yl)-1,2-oxazole Oxalate
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| Synonyms |
PD-144418 Oxalate PD-144418 PD144418 PD 144418
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6851 mL | 13.4257 mL | 26.8514 mL | |
| 5 mM | 0.5370 mL | 2.6851 mL | 5.3703 mL | |
| 10 mM | 0.2685 mL | 1.3426 mL | 2.6851 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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