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检测方案
≥98% (HPLC)
形式
powder
颜色
white to tan
溶解性
DMSO: ≥10 mg/mL
创始人
Sanofi Aventis
储存温度
2-8°C
SMILES字符串
CCCN(CCC)C(=O)Cc1c(nc2ccc(Cl)cn12)-c3ccc(Cl)cc3
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
InChI key
JRTIDHTUMYMPRU-UHFFFAOYSA-N
基因信息
human ... TSPO(706)
生化/生理作用
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.
特点和优势
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.
[A new case of hepatitis after alpidem monotherapy].
Gastroenterologie clinique et biologique, 18(10), 903-904 (1994-01-01)
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
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
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
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
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