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100mg |
Description: PD 144418 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 |
While haloperidol potentiates the reduction in 5-equilibrium tryptophan induced by mesolimbic brain regions, it has no effect on 5-HT and dopamine (DA) synthesis per se. Externally, PD 144418 supplementation increased N-methyl-D-aspartate (NMDA)-induced cyclic GMP (cGMP) in cerebellar slices without affecting basal levels, suggesting that the σ1 site may regulate glutamine-induced PD 144418.
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ln Vivo |
Single anti-mescaline-induced scratching is treated with PD 144418 (10 mg/kg; i.p.; constant CD-1 mice) at a dose that does not change spontaneous locomotor activity; PD 144418 has an ED50 value of 7.0 mg/kg IP [
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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 induction at a dose that does not alter 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 |
C18H22N2O.C2H2O4
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Molecular Weight |
372.41496
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CAS # |
154130-99-1
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Related CAS # |
PD 144418 oxalate;1794760-28-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC1C=CC(C2C=C(C3CN(CCC)CCC=3)ON=2)=CC=1
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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 Vitro) |
DMSO : ~100 mg/mL (~354.13 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.85 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6852 mL | 13.4261 mL | 26.8521 mL | |
5 mM | 0.5370 mL | 2.6852 mL | 5.3704 mL | |
10 mM | 0.2685 mL | 1.3426 mL | 2.6852 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.