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PD 144418 oxalate

CAS# 154130-99-1

PD 144418 oxalate

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Chemical structure

PD 144418 oxalate

3D structure

Chemical Properties of PD 144418 oxalate

Cas No. 154130-99-1 SDF Download SDF
PubChem ID 53447361 Appearance Powder
Formula C20H24N2O5 M.Wt 372.42
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in DMSO
Chemical Name 3-(4-methylphenyl)-5-(1-propyl-3,6-dihydro-2H-pyridin-5-yl)-1,2-oxazole;oxalic acid
SMILES CCCN1CCC=C(C1)C2=CC(=NO2)C3=CC=C(C=C3)C.C(=O)(C(=O)O)O
Standard InChIKey IWSFHSVGBKPYFN-UHFFFAOYSA-N
Standard InChI 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)7-9-15;3-1(4)2(5)6/h5-9,12H,3-4,10-11,13H2,1-2H3;(H,3,4)(H,5,6)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PD 144418 oxalate

DescriptionHigh affinity, selective σ1 ligand (Ki values are 0.08 and 1377 nM for σ1 and σ2 respectively). Displays no significant activity at a wide range of other receptors, ion channels and enzymes. Antagonizes mescaline-induced scratching in mice following i.p. administration. Also attenuates cocaine-induced hyperactivity in mice.

PD 144418 oxalate Dilution Calculator

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PD 144418 oxalate Molarity Calculator

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Preparing Stock Solutions of PD 144418 oxalate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6851 mL 13.4257 mL 26.8514 mL 53.7028 mL 67.1285 mL
5 mM 0.537 mL 2.6851 mL 5.3703 mL 10.7406 mL 13.4257 mL
10 mM 0.2685 mL 1.3426 mL 2.6851 mL 5.3703 mL 6.7129 mL
50 mM 0.0537 mL 0.2685 mL 0.537 mL 1.0741 mL 1.3426 mL
100 mM 0.0269 mL 0.1343 mL 0.2685 mL 0.537 mL 0.6713 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on PD 144418 oxalate

Relationship between cerebral sigma-1 receptor occupancy and attenuation of cocaine's motor stimulatory effects in mice by PD144418.[Pubmed:25100754]

J Pharmacol Exp Ther. 2014 Oct;351(1):153-63.

Psychostimulant effects of cocaine are mediated partly by agonist actions at sigma-1 (sigma1) receptors. Selective sigma1 receptor antagonists attenuate these effects and provide a potential avenue for pharmacotherapy. However, the selective and high affinity sigma1 antagonist PD144418 (1,2,3,6-tetrahydro-5-[3-(4-methylphenyl)-5-isoxazolyl]-1-propylpyridine) has been reported not to inhibit cocaine-induced hyperactivity. To address this apparent paradox, we evaluated aspects of PD144418 binding in vitro, investigated sigma1 receptor and dopamine transporter (DAT) occupancy in vivo, and re-examined effects on locomotor activity. PD144418 displayed high affinity for sigma1 sites (Ki 0.46 nM) and 3596-fold selectivity over sigma2 sites (Ki 1654 nM) in guinea pig brain membranes. No appreciable affinity was noted for serotonin and norepinephrine transporters (Ki >100 muM), and the DAT interaction was weak (Ki 9.0 muM). In vivo, PD144418 bound to central and peripheral sigma1 sites in mouse, with an ED50 of 0.22 mumol/kg in whole brain. No DAT occupancy by PD144418 (10.0 mumol/kg) or possible metabolites were observed. At doses that did not affect basal locomotor activity, PD144418 (1, 3.16, and 10 mumol/kg) attenuated cocaine-induced hyperactivity in a dose-dependent manner in mice. There was good correlation (r(2) = 0.88) of hyperactivity reduction with increasing cerebral sigma1 receptor occupancy. The behavioral ED50 of 0.79 mumol/kg corresponded to 80% occupancy. Significant sigma1 receptor occupancy and the ability to mitigate cocaine's motor stimulatory effects were observed for 16 hours after a single 10.0 mumol/kg dose of PD144418.

The pharmacology of the novel and selective sigma ligand, PD 144418.[Pubmed:9144641]

Neuropharmacology. 1997 Jan;36(1):51-62.

The pharmacology of PD 144418 (1-propyl-5-(3-p-tolyl-isoxazol-5-yl)-1,2,3,6-tetrahydropyridine) was characterized using neurochemical, biochemical and behavioral techniques. For sigma (sigma 1 and sigma 2 respectively) sites, PD 144418 affinities were determined using whole guinea pig brain membranes with [3H](+)-pentazocine and neuroblastoma x glioma cell membranes using [3H]1,3,di-O-tolylguanidine (DTG) in the presence of 200 nM (+)-pentazocine. PD 144418 exhibited an affinity for sigma 1 of 0.08 nM (Ki) versus a K1 of 1377 nM for sigma 2 site. Additional receptor binding studies indicated that PD 144418 lacked affinity for dopaminergic, adrenergic, muscarinic and a variety of other receptors. In vitro studies indicated that PD 144418 reversed the N-methyl-D-aspartate (NMDA)-induced increase in cyclic GMP (cGMP) in rat cerebellar slices without affecting the basal levels, suggesting that sigma 1 sites may be important in the regulation of glutamine-induced actions. PD 144418 potentiated the decrease in 5-hydroxytryptophan caused by haloperidol in the mesolimbic region, but by itself had no effect in 5-hydroxytrypamine (5-HT) and dopamine (DA) synthesis. Behaviorally, similar to other sigma ligands, PD 144418 antagonized mescaline-induced scratching at doses that did not alter spontaneous motor activity. This action is suggestive of potential antipsychotic property. It exhibited no anxiolytic and antidepressant properties in the models used. These results show that PD 144418 is a very selective sigma 1 agent, devoid of any significant affinity for other receptors and that sigma 1 site may modulate actions in the CNS.

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.

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