Abstract
Three series of bicyclic, semirigid congeners of beta-phenethylamine have been prepared for evaluation of the effect of ring size (and of concomitant conformational variation) on biological activity in a variety of assays for adrenergic and dopaminergic actions. Pharmacologic activity was associated with 2-aminotetralin and 2-aminoindan derivateves, but was not found with 6-aminobenzocycloheptene derivatives. Noteworthy is the ability of several aminotetralins and aminoindans to increase the hot-plate reaction time without eliciting dopaminergic effects. This action was not blocked by pretreatment with naloxone.
Publication types
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Comparative Study
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amines / chemical synthesis
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Amines / pharmacology
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Analgesics / chemical synthesis
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Animals
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Benzocycloheptenes / chemical synthesis*
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Benzocycloheptenes / pharmacology
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Blood Pressure / drug effects
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Cats
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Dogs
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Exploratory Behavior / drug effects
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Humans
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Indans / chemical synthesis*
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Indans / pharmacology
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Indenes / chemical synthesis*
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Male
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Mice
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Naphthalenes / chemical synthesis*
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Phenethylamines / chemical synthesis
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Phenethylamines / pharmacology*
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Rats
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Reflex / drug effects
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Stereotyped Behavior / drug effects
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Structure-Activity Relationship
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Tetrahydronaphthalenes / chemical synthesis*
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Tetrahydronaphthalenes / pharmacology
Substances
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Amines
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Analgesics
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Benzocycloheptenes
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Indans
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Indenes
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Naphthalenes
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Phenethylamines
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Tetrahydronaphthalenes