A Pyridazine Series of α2/α3 Subtype Selective GABAA Agonists for the Treatment of Anxiety
| العنوان: | A Pyridazine Series of α2/α3 Subtype Selective GABAA Agonists for the Treatment of Anxiety |
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| المؤلفون: | Wayne F. A. Sheppard, David S. Reynolds, Alison J. Smith, John R. Atack, Joanna Stanley, David James Hallett, Richard Thomas Lewis, Keith A. Wafford, Rowan A. Wilson, Timothy Blackburn, George R. Marshall, Wesley Peter Blackaby, Andrew Pike, Spencer J. Tye, Andrew Stephen Robert Jennings, Susan M. Cook, Pushpinder Ferris, Bindi Sohal |
| المصدر: | Journal of Medicinal Chemistry. 49:2600-2610 |
| بيانات النشر: | American Chemical Society (ACS), 2006. |
| سنة النشر: | 2006 |
| مصطلحات موضوعية: | Agonist, medicine.drug_class, Anxiety, Pharmacology, Ligands, Pyridazine, Structure-Activity Relationship, chemistry.chemical_compound, Oral administration, In vivo, Drug Discovery, medicine, Animals, Humans, GABA-A Receptor Agonists, Receptor, GABA Agonists, Benzodiazepine, Binding Sites, Molecular Structure, GABAA receptor, Stereoisomerism, Recombinant Proteins, Rats, Pyridazines, Anti-Anxiety Agents, Biochemistry, chemistry, Sedative, Molecular Medicine |
| الوصف: | The development of a series of GABA(A) alpha2/alpha3 subtype selective pyridazine based benzodiazepine site agonists as anxiolytic agents with reduced sedative/ataxic potential is described, including the discovery of 16, a remarkably alpha3-selective compound ideal for in vivo study. These ligands are antagonists at the alpha1 subtype, with good CNS penetration and receptor occupancy, and excellent oral bioavailability. |
| تدمد: | 1520-4804 0022-2623 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3256a1392c1eb18c5f05fe4684c424b7 https://doi.org/10.1021/jm051144x |
| رقم الأكسشن: | edsair.doi.dedup.....3256a1392c1eb18c5f05fe4684c424b7 |
| قاعدة البيانات: | OpenAIRE |
Find this issue from the American Chemical Society | تدمد: | 15204804 00222623 |
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