Bioorganic & medicinal chemistry letters, 2000-08, Vol.10 (16), p.1867-1870
2000
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Details
- Autor(en) / Beteiligte
- Titel
- 1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2000-08, Vol.10 (16), p.1867-1870
- Ort / Verlag
- Oxford: Elsevier
- Erscheinungsjahr
- 2000
- Quelle
- Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)
- Beschreibungen/Notizen
- Bisarylmethoxyethers have been identified with nanomolar 5-HT2C affinity and selectivity over both 5-HT2A and 5-HT2B receptors. Compounds such as 1, 2, 8, 12, 14 and 18 have potent oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function and their therapeutic potential is currently under further investigation.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/S0960-894X(00)00365-6Titel-ID: cdi_proquest_miscellaneous_72224421
- Format
- –
- Schlagworte
- Aminopyridines - administration & dosage, Aminopyridines - chemical synthesis, Aminopyridines - chemistry, Aminopyridines - pharmacology, Animals, Biological and medical sciences, Drug Design, Indoles - administration & dosage, Indoles - chemical synthesis, Indoles - chemistry, Indoles - pharmacology, Kinetics, Medical sciences, Molecular Structure, Motor Activity - drug effects, Neuropharmacology, Neurotransmitters. Neurotransmission. Receptors, Pharmacology. Drug treatments, Rats, Receptor, Serotonin, 5-HT2C, Receptors, Serotonin - metabolism, Serotonin Antagonists - administration & dosage, Serotonin Antagonists - chemical synthesis, Serotonin Antagonists - chemistry, Serotonin Antagonists - pharmacology, Serotoninergic system, Structure-Activity Relationship