82626-01-5
82626-01-5
Chemical Structure
Alpidem
- CAS No.: 82626-01-5
- Formula:C21H23Cl2N3O
- Molecular Weight:404.34
IUPAC Name: 2-(6-chloro-2-(4-chlorophenyl)imidazo[1,2-a]pyridin-3-yl)-N,N-dipropylacetamide
InChIKey: JRTIDHTUMYMPRU-UHFFFAOYSA-N
SMILES: O=C(N(CCC)CCC)CC1=C(C2=CC=C(Cl)C=C2)N=C3C=CC(Cl)=CN31
Biological Activity: Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions[1][2][3][4][5][6][7][8][9][10][11].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Alpidem | 99.70% | Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions. | ||||||||||||||||||||
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Alpidem (Standard) | ≥98% | Alpidem (Standard) is the analytical standard of Alpidem (HY-W013150). This product is intended for research and analytical applications. Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions. | ||||||||||||||||||||
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Alpidem-d14 | Alpidem-d14 is the deuterium labeled Alpidem (HY-W013150). Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions. | |||||||||||||||||||||
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References
- [1]. Faure-Halley C, et al. Expression and properties of recombinant alpha 1 beta 2 gamma 2 and alpha 5 beta 2 gamma 2 forms of the rat GABAA receptor. Eur J Pharmacol. 1993 Aug 15;246(3):283-7. [Content Brief]
- [2]. Zivkovic B, et al. Pharmacological and behavioral profile of alpidem as an anxiolytic. Pharmacopsychiatry. 1990;23 Suppl 3:108-113. [Content Brief]
- [3]. Lucie Guetzoyan, et al. Flow chemistry synthesis of zolpidem, alpidem and other GABAA agonists and their biological evaluation through the use of in-line frontal affinity chromatography. Chem. Sci., 2013,4, 764-769.
- [4]. Berson A, et al. Toxicity of alpidem, a peripheral benzodiazepine receptor ligand, but not zolpidem, in rat hepatocytes: role of mitochondrial permeability transition and metabolic activation. J Pharmacol Exp Ther. 2001;299(2):793-800. [Content Brief]
- [5]. Anzini M, et al. Molecular basis of peripheral vs central benzodiazepine receptor selectivity in a new class of peripheral benzodiazepine receptor ligands related to alpidem. J Med Chem. 1996;39(21):4275-4284. [Content Brief]
- [6]. A. Durand, et al. Comparative Pharmacokinetic Profile of Two Imidazopyridine Drugs: Zolpidem and Alpidem. DRUG METABOLiSM REVIEWS. 24(2). 239-266 (1992).
- [7]. Garrigou-Gadenne D, et al. The disposition and pharmacokinetics of alpidem, a new anxiolytic, in the rat. Drug Metab Dispos. 1991 May-Jun;19(3):574-9. [Content Brief]
- [8]. Sanger DJ, et al. Discriminative stimulus effects of alpidem, a new imidazopyridine anxiolytic. Psychopharmacology (Berl). 1994;113(3-4):395-403. [Content Brief]
- [9]. Benavides J, et al. Comparative autoradiographic distribution of central omega (benzodiazepine) modulatory site subtypes with high, intermediate and low affinity for zolpidem and alpidem. Brain Res. 1993;604(1-2):240-250. [Content Brief]
- [10]. Trapani G, et al. Alpidem analogues containing a GABA or glycine moiety as new anticonvulsant agents. Eur J Pharm Sci. 2003;18(3-4):231-240. [Content Brief]
- [11]. Hascoët M, et al. Anticonflict effect of alpidem as compared with the benzodiazepine alprazolam in rats. Pharmacol Biochem Behav. 1997;56(2):317-324. [Content Brief]
Keywords
