Eliprodil

Modify Date: 2024-01-05 13:08:38

Eliprodil Structure
Eliprodil structure
Common Name Eliprodil
CAS Number 119431-25-3 Molecular Weight 347.85400
Density 1.205 g/cm3 Boiling Point 474.1ºC at 760 mmHg
Molecular Formula C20H23ClFNO Melting Point N/A
MSDS Chinese USA Flash Point 240.5ºC
Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning

 Use of Eliprodil


Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).IC50 value:Target: NR2B-NMDA antagonistHuman N-type Ca2+ channel currents were inhibited by ifenprodil and eliprodil with IC50 values of 50 microM and 10 microM respectively whereas P-type Ca2+ channel currents were inhibited reversibly by ifenprodil and eliprodil with approximate IC50 values of 60 microM and 9 microM respectively. eliprodil (1 microm) produced a moderate reverse rate-dependent prolongation of the action potential duration (7.4+/-1.5, 8.9+/-2.1 and 9.9+/-1.8% at cycle lengths of 300, 1000 and 5000 ms, respectively; n=9).

 Names

Name Eliprodil,α-(4-Chlorophenyl)-4-[(4-fluorophenyl)methyl]-1-piperidineethanol
Synonym More Synonyms

 Eliprodil Biological Activity

Description Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).IC50 value:Target: NR2B-NMDA antagonistHuman N-type Ca2+ channel currents were inhibited by ifenprodil and eliprodil with IC50 values of 50 microM and 10 microM respectively whereas P-type Ca2+ channel currents were inhibited reversibly by ifenprodil and eliprodil with approximate IC50 values of 60 microM and 9 microM respectively. eliprodil (1 microm) produced a moderate reverse rate-dependent prolongation of the action potential duration (7.4+/-1.5, 8.9+/-2.1 and 9.9+/-1.8% at cycle lengths of 300, 1000 and 5000 ms, respectively; n=9).
Related Catalog
References

[1]. Bath CP, et al. The effects of ifenprodil and eliprodil on voltage-dependent Ca2+ channels and in gerbil global cerebral ischaemia. Eur J Pharmacol. 1996 Mar 28;299(1-3):103-12.

[2]. Lengyel C, et al. Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: importance of the decreased repolarisation reserve in the development of proarrhythmic risk. Br J Pharmacol. 2004 Sep;143(1):152-8.

 Chemical & Physical Properties

Density 1.205 g/cm3
Boiling Point 474.1ºC at 760 mmHg
Molecular Formula C20H23ClFNO
Molecular Weight 347.85400
Flash Point 240.5ºC
Exact Mass 347.14500
PSA 23.47000
LogP 4.40510
Vapour Pressure 8.57E-10mmHg at 25°C
Index of Refraction 1.58
Storage condition 2-8°C

 Safety Information

Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning
Hazard Statements H319-H410
Precautionary Statements P273-P305 + P351 + P338-P501
Personal Protective Equipment Eyeshields;Gloves
Hazard Codes N: Dangerous for the environment;
Risk Phrases R50/53
Safety Phrases 60-61
RIDADR UN 3077 9/PG 3
HS Code 2933399090

 Customs

HS Code 2933399090
Summary 2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles24

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NMDA receptor antagonists do not block the development of sensitization of catalepsy, but make its expression state-dependent.

Behav. Pharmacol. 12(2) , 143-9, (2001)

Dopamine (DA) receptor blockade induces catalepsy in rats which increases in strength upon retesting. This increase in catalepsy represents a form of sensitization which has been shown to be completel...

Synthesis and resolution of racemic eliprodil and evaluation of the enantiomers of eliprodil as NMDA receptor antagonists.

Bioorg. Med. Chem. Lett. 10(12) , 1377-80, (2000)

A short synthesis of the NMDA receptor antagonist (rac)-Eliprodil (9) and its resolution into the enantiomers by chiral HPLC is described. The enantiomers (R)-9 and (S)-9 were found to exhibit markedl...

The sequential analysis of repeated binary responses: a score test for the case of three time points.

Stat. Med. 25(13) , 2196-214, (2006)

In this paper a robust method is developed for the analysis of data consisting of repeated binary observations taken at up to three fixed time points on each subject. The primary objective is to compa...

 Synonyms

eliprodil
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