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alpidem : ウィキペディア英語版
alpidem

Alpidem (Ananxyl) is an anxiolytic drug from the imidazopyridine family, related to the more well known sleeping medication zolpidem. Unlike zolpidem however, alpidem does not produce sedative effects at normal doses, and is instead used specifically for the treatment of anxiety.〔Zivkovic B, Morel E, Joly D, Perrault G, Sanger DJ, Lloyd KG. Pharmacological and behavioral profile of alpidem as an anxiolytic. ''Synthelabo Recherche'', L.E.R.S., Bagneux, France. 1990 May;23 Suppl 3:108-13. PMID 1974069〕〔Sanger DJ, Zivkovic B. Discriminative stimulus effects of alpidem, a new imidazopyridine anxiolytic. ''Synthelabo Recherche'', Bagneux, France. 1994 Jan;113(3-4):395-403. PMID 7862851〕
Alipidem was developed by Synthélabo (now part of Sanofi-Aventis). It was approved for marketing in France in 1991. Clinical trial to obtain US FDA approval were halted in 1992 and the drug never received FDA approval. It was withdrawn from the French market by 1994 and is not approved for marketing anywhere in the world.〔( WHO Drug Information Vol. 8, No. 2, 1994, page 64 )〕
Alpidem has nanomolar binding affinity for both the central benzodiazepine receptor (CBR) and the peripheral benzodiazepine receptor (PBR) (translocator protein 18 kDa) (PBR (Ki ) 0.5-7 nM) and CBR (Ki ) 1-28 nM, respectively).〔 (a) Bourguignon, J. J. Endogenous and Synthetic Ligand of Mitochondrial Benzodiazepine Receptors: Structure-Affinity Relationships. In Peripheral Benzodiazepine Receptors; Giesen-Crouse, E., Ed.; Academic Press: London, 1993; pp 59-85. (b) Costa, E.; Romeo, E.; Auta, J.; Papadopoulos, V.; Kozikowski, A. P.; Guidotti, A. Is There a Pharmacology of Brain Steroidogenesis? In Neurosteroid and Brain Function, Fidia ResearchFundation Symposium Series; Costa, E., Paul, S. M., Eds.; Thieme Medical Publisher, Inc.: New York, 1991; pp 171-176. (c) Romeo, E.; Auta, J.; Kozikowski, A. P.; Ma, D.; Papadopoulos, V.; Puia, G.; Costa, E.; Guidotti, A. 2-Aryl-3-Indoleacetamides (FGIN-1): A New Class of Potent and Specific Ligands for the Mitochondrial DBI Receptor (MDR). J. Pharmacol. Exp. Ther. 1992, 262, 971-978. (d) Kozikowski, A. P.; Ma, D.; Romeo, E.; Auta, J.; Papadopoulos, V.; Puia, G.; Costa, E.; Guidotti, A.
Synthesis of (2-Arylindol-3-yl)acetamides as Probes of Mitochondrial Steroidogenesis - A New Mechanism for GABAA Receptor
Modulation. Angew. Chem., Int. Ed. Engl. 1992, 31, 1060-1062.〕 However the chemical structure of alpidem is not related to that of the benzodiazepines, and alpidem is thus sometimes referred to as a nonbenzodiazepine.〔Diamond BI, Nguyen H, O'Neal E, Ochs R, Kaffeman M, Borison RL. A comparative study of alpidem, a nonbenzodiazepine, and lorazepam in patients with nonpsychotic anxiety. ''Psychopharmacology Bulletin''. 1991;27(1):67-71.〕
==Indications==

Alpidem is not approved for any indication.

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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