D-Amino Acid Homopiperazine Amides: Discovery of A-320436, a Potent and Selective Non-Imidazole Histamine H3-Receptor Antagonist
| Autor: | Gerard B. Fox, Youssef L. Bennani, Ramin Faghih, Kathy M. Krueger, Michael P. Curtis, Arthur A. Hancock, Jia Bao Pan, Marlon D. Cowart, Timothy A. Esbenshade, Wesley J. Dwight, Thomas G. Pagano, John K. Pratt |
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| Rok vydání: | 2004 |
| Předmět: |
Cerebral Cortex
Stereochemistry Histamine Antagonists Antagonist Pharmaceutical Science Chemical synthesis Piperazines Rats Mice Structure-Activity Relationship chemistry.chemical_compound chemistry In vivo Drug Discovery Animals Humans Receptors Histamine H3 Imidazole Structure–activity relationship Histamine H3 receptor Receptor Histamine |
| Zdroj: | Archiv der Pharmazie. 337:219-229 |
| ISSN: | 1521-4184 0365-6233 |
| Popis: | Structure-activity relationships of homopiperazine-containing alkoxybiaryl nitriles employing various D-amino acid moieties and their N-furanoyl analogues were undertaken. This led to A-320436, a potent and selective non-imidazole H(3)-receptor antagonist possessing balanced affinity for both rat and human H(3)-receptors. This compound was shown to demonstrate in vitro and in vivo functional antagonism and is non-neurotoxic at doses (i.p.) up to 163 mg/kg in a general observation test. |
| Databáze: | OpenAIRE |
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