Abstract
In vitro assays on a series of cis- and trans-octahydrobenzo[g]quinolines indicated an unusual trend of affinities at the dopaminergic receptors and alpha adrenoceptors. The trans N-benzyl analogues exhibited affinity at the alpha2 as well as the D1-like receptors whereas their N-unsubstituted congeners showed a distinct preference for the alpha2 adrenoceptor. Enhanced activity for the alpha2 receptors was also exhibited by the cis N-benzylated isomers. These observations are interpreted by theoretical calculations.
MeSH terms
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Animals
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Cell Membrane / metabolism
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Dopamine Agents / chemical synthesis
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Dopamine Agents / pharmacology*
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Models, Theoretical
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Prazosin / metabolism
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Quinolines / chemistry*
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Quinolines / pharmacology*
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Rats
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Receptors, Adrenergic, alpha / chemistry
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Receptors, Adrenergic, alpha / drug effects*
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Receptors, Adrenergic, alpha-2 / chemistry
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Receptors, Adrenergic, alpha-2 / drug effects*
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Spiperone / metabolism
Substances
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Dopamine Agents
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Quinolines
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Receptors, Adrenergic, alpha
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Receptors, Adrenergic, alpha-2
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Spiperone
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Prazosin