Abstract
The synthesis and biological evaluation of novel antagonists of the rat H(3) receptor are described. These compounds differ from prototypical H(3) antagonists in that they do not contain an imidazole moiety, but rather a substituted aminopyrrolidine moiety. A systematic modification of the substituents on the aminopyrrolidine ring was performed using pre-formatted precursor sets, where applicable, to afford several compounds with high affinity and selectivity for the H(3) receptor.
MeSH terms
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Acylation
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Animals
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Cerebral Cortex / drug effects
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Cerebral Cortex / metabolism
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Drug Evaluation, Preclinical
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Histamine Antagonists / chemical synthesis*
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Histamine Antagonists / pharmacology*
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Humans
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In Vitro Techniques
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Ligands
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Pyrrolidines / chemical synthesis*
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Pyrrolidines / pharmacology*
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Rats
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Receptors, Histamine H1 / drug effects
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Receptors, Histamine H1 / metabolism
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Receptors, Histamine H2 / drug effects
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Receptors, Histamine H2 / metabolism
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Receptors, Histamine H3 / drug effects*
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Structure-Activity Relationship
Substances
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Histamine Antagonists
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Ligands
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Pyrrolidines
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Receptors, Histamine H1
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Receptors, Histamine H2
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Receptors, Histamine H3