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Ifenprodil Tartrate

NMDA receptor antagonist CAS# 23210-58-4

Ifenprodil Tartrate

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Chemical structure

Ifenprodil Tartrate

3D structure

Chemical Properties of Ifenprodil Tartrate

Cas No. 23210-58-4 SDF Download SDF
PubChem ID 656586 Appearance Powder
Formula C46H60N2O10 M.Wt 801.0
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO > 10 mM
Chemical Name 4-[2-(4-benzylpiperidin-1-yl)-1-hydroxypropyl]phenol;(2R,3R)-2,3-dihydroxybutanedioic acid
SMILES CC(C(C1=CC=C(C=C1)O)O)N2CCC(CC2)CC3=CC=CC=C3.CC(C(C1=CC=C(C=C1)O)O)N2CCC(CC2)CC3=CC=CC=C3.C(C(C(=O)O)O)(C(=O)O)O
Standard InChIKey DMPRDSPPYMZQBT-CEAXSRTFSA-N
Standard InChI InChI=1S/2C21H27NO2.C4H6O6/c2*1-16(21(24)19-7-9-20(23)10-8-19)22-13-11-18(12-14-22)15-17-5-3-2-4-6-17;5-1(3(7)8)2(6)4(9)10/h2*2-10,16,18,21,23-24H,11-15H2,1H3;1-2,5-6H,(H,7,8)(H,9,10)/t;;1-,2-/m..1/s1
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 Ifenprodil Tartrate

DescriptionIfenprodil tartrate is a novel N-methyl-D-aspartate (NMDA) receptor antagonist that selectively inhibits receptors containing the NR2B subunit.

References:
[1]. Gotti B, et al. Ifenprodil and SL 82.0715 as cerebral anti-ischemic agents. I. Evidence for efficacy in models of focal cerebral ischemia. J Pharmacol Exp Ther. 1988 Dec;247(3):1211-21. [2]. Reynolds IJ, et al. Ifenprodil is a novel type of N-methyl-D-aspartate receptor antagonist: interaction with polyamines. Mol Pharmacol. 1989 Nov;36(5):758-65. [3]. Schoemaker H, et al. Binding of [3H]ifenprodil, a novel NMDA antagonist, to a polyamine-sensitive site in the rat cerebral cortex. Eur J Pharmacol. 1990 Feb 6;176(2):249-50. [4]. Shalaby IA, et al. Neuroprotective effects of the N-methyl-D-aspartate receptor antagonists ifenprodil and SL-82,0715 on hippocampal cells in culture. J Pharmacol Exp Ther. 1992 Feb;260(2):925-32.

Ifenprodil Tartrate Dilution Calculator

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Preparing Stock Solutions of Ifenprodil Tartrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.2484 mL 6.2422 mL 12.4844 mL 24.9688 mL 31.211 mL
5 mM 0.2497 mL 1.2484 mL 2.4969 mL 4.9938 mL 6.2422 mL
10 mM 0.1248 mL 0.6242 mL 1.2484 mL 2.4969 mL 3.1211 mL
50 mM 0.025 mL 0.1248 mL 0.2497 mL 0.4994 mL 0.6242 mL
100 mM 0.0125 mL 0.0624 mL 0.1248 mL 0.2497 mL 0.3121 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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Background on Ifenprodil Tartrate

Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM.

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References on Ifenprodil Tartrate

[Double-blind randomized controlled trial of ifenprodil tartrate versus placebo in chronic arterial occlusive disease of the legs at stage II of the Leriche and Fontaine classification].[Pubmed:7745355]

J Mal Vasc. 1995;20(1):21-7.

Authors report results on a comparative multicenter double blind trial carried out to assess the efficacy of Ifenprodil Tartrate (*) (60 mg a.d.) versus placebo in symptomatic treatment of stable peripheral arterial occlusive disease (Fontaine stage II). Ninety four patients were included in this six months, two parallel group study (2 homogeneous groups) which shows a statistically significant functional improvement in the treatment group versus the placebo group. After six months of treatment, the maximum walking distance (MWD)--main assessment criteria--was 126.0 +/- 18.5 meters in the Ifenprodil group versus 46.4 +/- 20.2 meters in the placebo group (p = 0.005). This represents an improvement of 62.1% in the Ifenprodil group versus 21.0% in the placebo group. An improvement of at least 50% in MWD was observed in 41.3% of patients treated by Ifenprodil and in only 12.5% of patients receiving placebo (p = 0.002). The evolution of ankle/brachial systolic post exercise index from JO to J180 was not significantly different in the two groups. Clinical and biological tolerance of Ifenprodil Tartrate was excellent.

[Quality of life of patient with peripheral arterial obliterative disease treated with ifenprodil tartrate. Results of an ARTEMIS study].[Pubmed:9844701]

Drugs. 1998;56 Suppl 3:37-48.

A clinical trial was performed to assess the effects on quality of life of a treatment (Ifenprodil Tartrate 20 mg, 3 times daily for one year) in patients suffering from peripheral arterial obliterative disease of the lower extremities with intermittent claudication. A specific questionnaire--ARTEMIS--was used to evaluate quality of life. The study enabled the responsiveness over time of the ARTEMIS questionnaire to be checked. During this open, prospective, multicentre study, patients requiring treatment for peripheral arterial disease of the lower extremities and recruited by angiologists and general practitioners filled in the complete or short form of the ARTEMIS questionnaire, respectively, at baseline, and at 3, 6, 9 and 12 months. 4821 patients were recruited. 4494 questionnaires were analysed (169 from the angiologist group and 4325 from the general practitioner group). The majority of the patients (mean age 67 years) were men (70%), either former or current smokers (68%), with high blood pressure (54%), hyperlipidaemia (48%) and type 2 (non-insulin-dependent) diabetes mellitus (16%), and with a 3-year history of intermittent claudication (+/- 3.5) on average. Quality-of-life scores improved (as from month 3) between baseline and month 12. This progression was significant for all dimensions of the reduced questionnaire (p < or = 0.0001) and for 12 of the 15 dimensions of the complete version. These quality-of-life results should be measured against the global clinical improvement, which was rated as good by the investigators (70% of cases). Treatment tolerability was assessed for the 4821 patients recruited and was judged satisfactory. The number and type of serious events and recorded deaths corresponded to events commonly observed in this elderly population. These results show how the ARTEMIS quality-of-life scales can be used in community practice during symptomatic treatment with a vasoactive agent such as ifenprodil, to assess quality-of-life improvements in patients suffering from stage II peripheral arterial disease of the lower extremities.

Description

Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM.

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