词条 | Imagabalin |
释义 |
| IUPAC_name = (3S,5R)-3-amino-5-methyloctanoic acid | image = Imagabalin.svg | CAS_number = 610300-07-7 | CAS_supplemental = 610300-00-0 (hydrochloride) | ATC_prefix = None | ATC_suffix = | KEGG = D09627 | C = 9 | H = 19 | N = 1 | O = 2 | molecular_weight = 173.253 g/mol | synonyms = PD-0332334; PD-332,334 | PubChem = 10236037 | ChemSpiderID = 8411525 | smiles = O=C(O)C[C@@H](N)C[C@@H](CCC)C | StdInChI = 1S/C9H19NO2/c1-3-4-7(2)5-8(10)6-9(11)12/h7-8H,3-6,10H2,1-2H3,(H,11,12)/t7-,8+/m1/s1 | StdInChIKey = JXEHXYFSIOYTAH-SFYZADRCSA-N | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | pregnancy_category = | legal_status = | routes_of_administration = }}Imagabalin (INN, USAN; PD-332,334) is a drug which acts as a ligand for the α2δ subunit of the voltage-dependent calcium channel,[1] with some selectivity for the α2δ1 subunit over α2δ2.[2] Under development by Pfizer as a pharmaceutical medication, it has demonstrated preclinical efficacy of anxiolytic, analgesic, hypnotic, and anticonvulsant-like activity and is currently in phase III clinical trials for the treatment of generalized anxiety disorder.[2][3] See also
References1. ^{{cite journal |vauthors=Quintero JE, Pomerleau F, Huettl P, Johnson KW, Offord J, Gerhardt GA | title = Methodology for rapid measures of glutamate release in rat brain slices using ceramic-based microelectrode arrays: basic characterization and drug pharmacology | journal = Brain Research | volume = 1401 | issue = | pages = 1–9 |date=July 2011 | pmid = 21664606 | doi = 10.1016/j.brainres.2011.05.025 | url = http://linkinghub.elsevier.com/retrieve/pii/S0006-8993(11)00910-3| pmc = 3197737 }} {{Anxiolytics}}{{Calcium channel blockers}}{{nervous-system-drug-stub}}2. ^1 {{cite press release | title = Therapies in the Pipeline for Sleep Disorders: Focus on Novel Mechanisms and Disease Models | author = Larry Ereshefsky | year = 2008 | page = 11 | url = http://www.cmellc.com/psychcongress/images/08pdf/43-5%20Ereshefsky.pdf | accessdate = 2012-04-22 | format = PDF}} 3. ^{{cite web | url = http://clinicaltrials.gov/ct2/show/NCT00542685 | title = A 10-Week Study Evaluating the Efficacy And Safety of PD 0332334 for the Treatment of Generalized Anxiety Disorder | accessdate = 2012-04-22}} 6 : Amino acids|Anxiolytics|Calcium channel blockers|GABA analogues|Pfizer products|Experimental drugs |
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