Abstract
The potencies of a series of 2 beta-substituted cocaine analogues to displace [3H]-3 beta-(p-fluorophenyl)tropane-2 beta-carboxylic acid methyl ester binding in rat striatal membranes demonstrate the requirement for a 2 beta-substituent with two hydrogen-bond acceptors. The insensitivity of the ester moiety to steric and electronic factors suggests its modification to provide site-specific irreversible ligands.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Analgesics / chemical synthesis*
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Analgesics / chemistry
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Analgesics / pharmacology
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Animals
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Binding Sites
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Carrier Proteins*
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Cocaine / analogs & derivatives*
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Cocaine / chemistry
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Cocaine / pharmacology
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Corpus Striatum / drug effects
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Corpus Striatum / metabolism
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Male
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Rats
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Rats, Inbred Strains
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Receptors, Drug / drug effects*
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Receptors, Drug / metabolism
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Structure-Activity Relationship
Substances
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Analgesics
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Carrier Proteins
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Receptors, Drug
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cocaine receptor
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Cocaine