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.
Pharmacology, biochemistry, and behavior, 56(2), 317-324 (1997-02-01)
A comparative study between two drugs acting on the GABAA receptor, alprazolam and alpidem was undertaken, using simple tests such as measurement of spontaneous locomotor activity, four plates test and rotarod in mice. Additional conflict test was further performed using
We have recently shown that compounds with high affinity for peripheral-type benzodiazepine receptors inhibited glucose-induced insulin secretion in vitro. We therefore performed an oral glucose tolerance test in anxious inpatients treated with the imidazopyridine derivative alpidem, which has been shown
European journal of pharmacology, 280(2), 167-173 (1995-07-04)
An alpidem-insensitive benzodiazepine binding site in the rat spinal cord has recently been identified in our laboratory. We report here the binding of 23 1,4-benzodiazepines to this site using [3H]Ro15-4513 (ethyl-8-azido-6-dihydro-5-methyl-4H-imidazo[1,2- a][1,4]benzodiazepine-3-carboxylate) in the presence of 65 microM alpidem (6-chloro-2-(4-chlorophenyl)-N,N-
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 18(3-4), 231-240 (2003-03-28)
Alpidem analogues containing a GABA (1-3) or glycine (4-6) moiety were synthesized and their interaction with the GABA/benzodiazepine receptor complex at central (CBR) and peripheral (PBR) level was evaluated. In particular, their ability to modulate the specific binding of [3H]-GABA
Journal of chromatography. A, 668(2), 403-411 (1994-05-13)
Alpidem, 6-chloro-2-(4-chlorophenyl)-N,N-dipropylimidazo[1,2-a]pyridine- 3-acetamide, is an anxiolytic imidazopyridine that undergoes a first-pass elimination after oral administration to humans; it is actively metabolized and three circulating metabolites have been identified in plasma due to N-dealkylation, oxidation or a combination of both processes.
DISCOVER Bioactive Small Molecules for Neuroscience
Questions
Reviews
★★★★★ No rating value
Active Filters
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
![(Tyr[SO3H]27)Cholecystokinin fragment 26-33 Amide ≥97% (HPLC), powder](/deepweb/assets/sigmaaldrich/product/structures/125/021/32eb71ec-73e5-4cfc-94d0-ebcf5e784e39/640/32eb71ec-73e5-4cfc-94d0-ebcf5e784e39.png)
