دورية أكاديمية
Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity.
| العنوان: | Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity. |
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| المؤلفون: | Acker BA; Neuroscience Research, Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA., Jacobsen EJ, Rogers BN, Wishka DG, Reitz SC, Piotrowski DW, Myers JK, Wolfe ML, Groppi VE, Thornburgh BA, Tinholt PM, Walters RR, Olson BA, Fitzgerald L, Staton BA, Raub TJ, Krause M, Li KS, Hoffmann WE, Hajos M, Hurst RS, Walker DP |
| المصدر: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jun 15; Vol. 18 (12), pp. 3611-5. Date of Electronic Publication: 2008 May 01. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Ltd Original Publication: Oxford ; New York : Pergamon Press, c1991- |
| مواضيع طبية MeSH: | Azabicyclo Compounds/*pharmacology , Nicotinic Agonists/*pharmacology , Pyridines/*pharmacology , Receptors, Nicotinic/*drug effects, Animals ; Azabicyclo Compounds/chemical synthesis ; Azabicyclo Compounds/chemistry ; Benzamides/pharmacology ; Blood Proteins/drug effects ; Bridged Bicyclo Compounds/pharmacology ; Bridged Bicyclo Compounds, Heterocyclic/pharmacology ; Dogs ; Dose-Response Relationship, Drug ; Humans ; Mice ; Microsomes, Liver/drug effects ; Molecular Conformation ; Nicotinic Agonists/chemical synthesis ; Nicotinic Agonists/chemistry ; Pyridines/chemical synthesis ; Pyridines/chemistry ; Quinuclidines/pharmacology ; Rats ; Receptors, Muscarinic/drug effects ; Stereoisomerism ; Structure-Activity Relationship ; alpha7 Nicotinic Acetylcholine Receptor |
| مستخلص: | A novel alpha7 nAChR agonist, N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (3a, PHA-709829), has been identified for the potential treatment of cognitive deficits in schizophrenia. The compound shows potent and selective alpha7 in vitro activity, excellent brain penetration, good rat oral bioavailability and robust in vivo efficacy in a rat auditory sensory gating model. |
| المشرفين على المادة: | 0 (Azabicyclo Compounds) 0 (Benzamides) 0 (Blood Proteins) 0 (Bridged Bicyclo Compounds) 0 (Bridged Bicyclo Compounds, Heterocyclic) 0 (Chrna7 protein, human) 0 (Chrna7 protein, mouse) 0 (Chrna7 protein, rat) 0 (N-(1-azabicyclo(2.2.2)oct-3-yl)furo(2,3-c)pyridine-5-carboxamide) 0 (N-(1-azabicyclo(3.2.1)oct-3-yl)furo(2,3-c)pyridine-5-carboxamide) 0 (Nicotinic Agonists) 0 (PNU-282987) 0 (Pyridines) 0 (Quinuclidines) 0 (Receptors, Muscarinic) 0 (Receptors, Nicotinic) 0 (alpha7 Nicotinic Acetylcholine Receptor) |
| تواريخ الأحداث: | Date Created: 20080521 Date Completed: 20080825 Latest Revision: 20161124 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1016/j.bmcl.2008.04.070 |
| PMID: | 18490160 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3405 |
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| DOI: | 10.1016/j.bmcl.2008.04.070 |