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关于此项目
经验公式(希尔记法):
C21H23Cl2N3O
化学文摘社编号:
分子量:
404.33
UNSPSC Code:
12352200
PubChem Substance ID:
MDL number:
InChI
1S/C21H23Cl2N3O/c1-3-11-25(12-4-2)20(27)13-18-21(15-5-7-16(22)8-6-15)24-19-10-9-17(23)14-26(18)19/h5-10,14H,3-4,11-13H2,1-2H3
SMILES string
CCCN(CCC)C(=O)Cc1c(nc2ccc(Cl)cn12)-c3ccc(Cl)cc3
InChI key
JRTIDHTUMYMPRU-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to tan
solubility
DMSO: ≥10 mg/mL
originator
Sanofi Aventis
storage temp.
2-8°C
Gene Information
human ... TSPO(706)
Biochem/physiol Actions
Alpidem is a potent antagonist of peripheral benzodiazepine receptor (PBR) that is located on the outer mitochondrial membrane and interacts with the mitochondrial permeability transition (MPT) pore. Alpidem is an anxiolytic drug from the imidazopyridine family. Alpidem acts selectively on the α3 receptor subtype and to a lesser extent at the α1 subtype (Kd of 0.33nM and 1.67nM respectively), of the benzodiazepine receptor.
Alpidem is a potent peripheral benzodiazepine receptor (PBR) antagonist.
Features and Benefits
This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the GABAA Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Sanofi Aventis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
D J Sanger et al.
Psychopharmacology, 113(3-4), 395-403 (1994-01-01)
Alpidem in an imidazopyridine derivative which binds selectively to the omega 1 (BZ1) receptor subtype. It is active in some, but not all, behavioural tests sensitive to benzodiazepine anxiolytics and has clinical anti-anxiety effects. However, in a previous study, it
A Chodera et al.
Polish journal of pharmacology, 46(5), 479-481 (1994-09-01)
The development of tolerance to the pharmacodynamic effects of azopirone (buspirone) and imidazopyridines (alpidem and zolpidem) was investigated. It was found that tolerance to the anxiolytic effect of buspirone develops only after 42 days of administration (twice daily). Of the
J F O'Hanlon et al.
Neuropsychobiology, 31(2), 81-88 (1995-01-01)
Effects of benzodiazepine (diazepam, lorazepam) and benzodiazepine-like anxiolytics (alpidem, suriclone) and a 5-HT-3 antagonist (ondansetron) on actual driving performance were measured in three double-blind, placebo-controlled studies. Subjects were healthy volunteers in two and anxious patients in the third. Treatments lasted
M Anzini et al.
Journal of medicinal chemistry, 39(21), 4275-4284 (1996-10-11)
Alpidem (1), the anxiolytic imidazopyridine, has nanomolar binding affinity for both the central benzodiazepine receptor (CBR) and the peripheral benzodiazepine receptor (PBR). A novel class of PBR ligands related to alpidem has been designed by comparing the interaction models of
[Subfulminant hepatitis caused by alpidem and treated by liver transplantation].
P Ausset et al.
Gastroenterologie clinique et biologique, 19(2), 222-223 (1995-02-01)
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