Abstract
Employing the dopamine autoreceptor agonist (-)-3-PPP (3) as well as the cholinergic receptor ligands 4 and 5 as lead compounds the 3-pyrrolidinylisoxazoles 2a,b as well as its optical antipodes ent 2a,b were synthesized from (R)-aspartic acid (6) and (S)-aspartic acid (ent-6), respectively. Pharmacological properties of the target compounds were evaluated employing dopamine D2 receptor binding studies and functional experiments on muscarinic M2 receptors.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Binding, Competitive
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Cattle
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Guinea Pigs
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In Vitro Techniques
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Isoxazoles / chemical synthesis*
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Isoxazoles / chemistry
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Isoxazoles / metabolism
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Ligands
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Myocardium / metabolism
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Neostriatum / metabolism
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Pyrrolidines / chemical synthesis*
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Pyrrolidines / chemistry
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Pyrrolidines / metabolism
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Radioligand Assay
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Receptor, Muscarinic M2
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Receptors, Dopamine D2 / metabolism*
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Receptors, Muscarinic / metabolism*
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Stereoisomerism
Substances
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3-methyl-5-(1-methyl-3-pyrrolidinyl)isoxazole
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3-methyl-5-(1-propyl-3-pyrrolidinyl)isoxazole
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Isoxazoles
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Ligands
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Pyrrolidines
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Receptor, Muscarinic M2
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Receptors, Dopamine D2
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Receptors, Muscarinic