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关于此项目
经验公式(希尔记法):
C20H23ClFNO
化学文摘社编号:
分子量:
347.85
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI
1S/C20H23ClFNO/c21-18-5-3-17(4-6-18)20(24)14-23-11-9-16(10-12-23)13-15-1-7-19(22)8-2-15/h1-8,16,20,24H,9-14H2
SMILES string
OC(CN1CCC(CC1)Cc2ccc(F)cc2)c3ccc(Cl)cc3
InChI key
GGUSQTSTQSHJAH-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 5 mg/mL, clear, H2O: insoluble
originator
Sanofi Aventis
storage temp.
2-8°C
Quality Level
Gene Information
human ... GRIN2B(2904)
rat ... Adra1a(29412)
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Biochem/physiol Actions
NR2B selective NMDA glutamate receptor antagonist which appears to target the "polyamine site" on the NMDA receptor, setting it apart from other NR2B receptor antagonists. Possesses neuroprotective effects in models of ischemia, but prolongs the QT interval in patients; currently under investigation for acute and chronic pain.
NR2B selective NMDA glutamate receptor antagonist.
Features and Benefits
This compound was developed by Sanofi Aventis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves
法规信息
新产品
此项目有
O A Dravolina et al.
Pharmacology, biochemistry, and behavior, 65(4), 611-620 (2000-04-15)
Current perspectives on the clinical use of NMDA receptor antagonists infer repeated administration schedules for the management of different pathological states. The development of tolerance and cross-tolerance between different NMDA receptor antagonists may be an important factor contributing to the
N A Sharif et al.
The British journal of ophthalmology, 83(2), 236-240 (1999-07-09)
This study characterised the pharmacology of [3H]-ifenprodil binding to the polyamine binding sites (PBS) on the N-methyl-D-aspartate (NMDA) receptor channel complex on human retinas. These data were correlated with the known neuroprotective effects of ifenprodil and eliprodil. Specific binding of
P J Missel et al.
Pharmaceutical development and technology, 11(1), 87-91 (2006-03-21)
Measurement of drug release of a sparingly soluble drug by conventional methods proceeds very slowly without the aid of surfactants. Two preliminary automated methods were developed that increase sensitivity and accelerate such studies by working at very small reservoir volumes.
P Wlaź et al.
Neuropharmacology, 38(2), 243-251 (1999-04-28)
The discovery that glutamate's activity at the N-methyl-D-aspartate (NMDA) receptor is positively modulated by glycine and polyamines has led to a new pharmacological strategy that NMDA receptor-mediated events could be antagonized indirectly at the strychnine-insensitive glycine co-agonist site (glycine(B) receptor)
M Reyes et al.
Brain research, 782(1-2), 212-218 (1998-03-31)
The N-methyl-D-aspartate (NMDA) subtype of glutamate receptor is one pathway through which excessive influx of calcium has been suggested to trigger ischemia-induced delayed neuronal death. NMDA receptors are heterooligomeric complexes comprised of both NR1 and NR2A-D subunits, in various combinations.
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