5-Alkyltryptamine derivatives as highly selective and potent 5-HT1D receptor agonists
| Autor: | Anne O'Brien, Rajender Kamboj, Cora Chen, David H. Lee, Charles Q. Meng, Tao Xin, Donna Hynd, Abdelmalik Slassi, Neil MacLean, Hong Wang, Louise Edwards, Caroline Seto, Suman Rakhit |
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| Rok vydání: | 2000 |
| Předmět: |
Agonist
Tertiary amine Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science In Vitro Techniques Biochemistry Chemical synthesis chemistry.chemical_compound Drug Discovery medicine Animals Saphenous Vein Molecular Biology Indole test Bicyclic molecule Organic Chemistry Tryptamines In vitro Serotonin Receptor Agonists chemistry Receptor Serotonin 5-HT1D Receptors Serotonin Molecular Medicine Rabbits 5-HT1D receptor Ethylamine Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 10:1707-1709 |
| ISSN: | 0960-894X |
| Popis: | A series of 5-alkyltryptamines (6) and the corresponding conformationally constrained analogues (8) have been synthesized. The structure activity relationships (SAR) at the 5-position of the indole skeleton and the ethylamine side chain have been studied. Functional activities were assessed using isolated rabbit saphenous vein. Potent, selective ligands were found (6e, Ki 2.5 nM, 5-HT1B/5-HT1D 125-fold) that have potential for treating acute migraine. |
| Databáze: | OpenAIRE |
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