Abstract
The synthesis and biological evaluation of novel tetrahydroisoquinoline, tetrahydroquinoline, and tetrahydroazepine antagonists of the human and rat H(3) receptors are described. The substitution around these rings as well as the nature of the substituent on nitrogen is explored. Several compounds with high affinity and selectivity for the human and rat H(3) receptors are reported.
MeSH terms
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Animals
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Azepines* / chemical synthesis
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Azepines* / chemistry
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Azepines* / pharmacology
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Drug Evaluation, Preclinical
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Humans
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Molecular Structure
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Rats
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Receptors, Histamine H3 / drug effects*
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Structure-Activity Relationship
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Tetrahydroisoquinolines / chemical synthesis*
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Tetrahydroisoquinolines / chemistry
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Tetrahydroisoquinolines / pharmacology
Substances
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Azepines
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Receptors, Histamine H3
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Tetrahydroisoquinolines
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3,4,5,6-tetrahydro-2H-azepine