Ro 8-4304 hydrochloride

CAS# 1312991-77-7

Ro 8-4304 hydrochloride

Catalog No. BCC7655----Order now to get a substantial discount!

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Chemical structure

Ro 8-4304 hydrochloride

3D structure

Chemical Properties of Ro 8-4304 hydrochloride

Cas No. 1312991-77-7 SDF Download SDF
PubChem ID 11957680 Appearance Powder
Formula C21H24ClFN2O3 M.Wt 406.88
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mM in water and to 100 mM in DMSO
Chemical Name 4-[3-[4-(4-fluorophenyl)-3,6-dihydro-2H-pyridin-1-yl]-2-hydroxypropoxy]benzamide;hydrochloride
SMILES C1CN(CC=C1C2=CC=C(C=C2)F)CC(COC3=CC=C(C=C3)C(=O)N)O.Cl
Standard InChIKey MQOXWHKUQOFFJW-UHFFFAOYSA-N
Standard InChI InChI=1S/C21H23FN2O3.ClH/c22-18-5-1-15(2-6-18)16-9-11-24(12-10-16)13-19(25)14-27-20-7-3-17(4-8-20)21(23)26;/h1-9,19,25H,10-14H2,(H2,23,26);1H
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 Ro 8-4304 hydrochloride

DescriptionNMDA receptor antagonist (IC50 = 0.4 μM) that displays > 100 fold selectivity for NR2B-containing receptors over NR2A-containing receptors. Exhibits an activity-dependent mechanism of NMDA antagonism and is competitive with respect to spermine .

Ro 8-4304 hydrochloride Dilution Calculator

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Preparing Stock Solutions of Ro 8-4304 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.4577 mL 12.2886 mL 24.5773 mL 49.1545 mL 61.4432 mL
5 mM 0.4915 mL 2.4577 mL 4.9155 mL 9.8309 mL 12.2886 mL
10 mM 0.2458 mL 1.2289 mL 2.4577 mL 4.9155 mL 6.1443 mL
50 mM 0.0492 mL 0.2458 mL 0.4915 mL 0.9831 mL 1.2289 mL
100 mM 0.0246 mL 0.1229 mL 0.2458 mL 0.4915 mL 0.6144 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 Ro 8-4304 hydrochloride

State-dependent NMDA receptor antagonism by Ro 8-4304, a novel NR2B selective, non-competitive, voltage-independent antagonist.[Pubmed:9504387]

Br J Pharmacol. 1998 Feb;123(3):463-72.

1. Subunit-selective blockade of N-methyl-D-aspartate (NMDA) receptors provides a potentially attractive strategy for neuroprotection in the absence of undesirable side effects. Here, we describe a novel NR2B-selective NMDA antagonist, 4- inverted question mark3-[4-(4-fluoro-phenyl)-3,6-dihydro-2H-pyridin-1-yl]-2-hydroxy-propoxy inverted question mark-benzamide (Ro 8-4304), which exhibits >100 fold higher affinity for recombinant NR1(001)/NR2B than NR1(001)/NR2A receptors. 2. Ro 8-4304 is a voltage-independent, non-competitive antagonist of NMDA receptors in rat cultured cortical neurones and exhibits a state-dependent mode of action similar to that described for ifenprodil. 3. The apparent affinity of Ro 8-4304 for the NMDA receptor increased in an NMDA concentration-dependent manner so that Ro 8-4304 inhibited 10 and 100 microM NMDA responses with IC50s of 2.3 and 0.36 microM, respectively. Currents elicited by 1 microM NMDA were slightly potentiated in the presence of 10 microM Ro 8-4304, and Ro 8-4304 binding slowed the rate of glutamate dissociation from NMDA receptors. 4. These results were predicted by a reaction scheme in which Ro 8-4304 exhibits a 14 and 23 fold higher affinity for the activated and desensitized states of the NMDA receptor, respectively, relative to the agonist-unbound resting state. Additionally, Ro 8-4304 binding resulted in a 3 4 fold increase in receptor affinity for glutamate site agonists. 5. Surprisingly, whilst exhibiting a similar affinity for NR2B-containing NMDA receptors as ifenprodil, Ro 8-4304 exhibited markedly faster kinetics of binding and unbinding to the NMDA receptor. This spectrum of kinetic behaviour reveals a further important feature of this emerging class of NR2B-selective compounds.

An allosteric interaction between the NMDA receptor polyamine and ifenprodil sites in rat cultured cortical neurones.[Pubmed:9729614]

J Physiol. 1998 Oct 1;512 ( Pt 1):17-28.

1. The atypical NR2B subunit-selective NMDA receptor antagonist ifenprodil was originally believed to act as a competitive antagonist at the polyamine binding site of the NMDA receptor. However, a number of studies have suggested that ifenprodil might bind to a distinct site. 2. Using whole-cell voltage clamp recordings, we have studied the interaction of spermine with both ifenprodil and the related NR2B selective antagonist Ro 8-4304 at the NMDA receptor in rat cultured cortical neurones in the presence of saturating concentrations of glycine. 3. Ifenprodil and Ro 8-4304 inhibited steady-state currents evoked by 100 microM NMDA in the absence of spermine with IC50 values of 0.3 and 0.6 microM, respectively. In the presence of 1 and 3 mM spermine, IC50 values for ifenprodil were 1.4 and 1.8 microM and for Ro 8-4304 they were 3. 0 and 7.5 microM, respectively. 4. In the presence of spermine, the on-time constant of receptor blockade by both antagonists was significantly slower than control and the off-time constant of recovery from receptor blockade following removal of Ro 8-4304 was significantly faster. 5. Fast application of spermine during an NMDA steady-state current in the continuous presence of a subsaturating concentration of either antagonist resulted in a biphasic increase in the current, consistent with a fast increase upon spermine binding and a slow increase resultant from dissociation of antagonist due to spermine binding-induced allosteric reduction in receptor antagonist affinity. In agreement with this, at higher, saturating concentrations of antagonist, the slow increase in current amplitude was markedly reduced or absent. 6. These observations are consistent with a non-competitive, allosteric interaction between spermine and the antagonists, such that spermine binding to the NMDA receptor results in a reduction in receptor affinity for the antagonists and vice versa. 7. The effects of Mg2+ on the NMDA-evoked currents and its interaction with ifenprodil were similar to those of spermine, supporting the suggestion that Mg2+ might be the physiological ligand acting at the spermine site mediating glycine-independent stimulation.

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