Neurochemical and Behavioral Evidence for a Selective Presynaptic Dopamine Receptor Agonist

A new dopamine analog, 6,7-dihydroxy-2-dimethylaminotetralin (TL-99), was compared to apomorphine in three tests of dopaminergic function in the central nervous system. The tests, performed on rats, included production of changes in locomotor activity (involving both presynaptic and postsynaptic rec...

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Bibliographic Details
Published in:Science (American Association for the Advancement of Science) 1980-12, Vol.210 (4474), p.1141-1143
Main Authors: Goodale, David B., Rusterholz, David B., Long, John P., Flynn, Jan R., Walsh, Brian, Cannon, Joseph G., Lee, Teresa
Format: Article
Language:English
Subjects:
Animals
Apomorphine - pharmacology
Behavior, Animal - drug effects
Brain - drug effects
Central nervous system
Dopamine agonists
Dopamine receptors
Dosage
Levodopa - metabolism
Locomotion
Motor Activity - drug effects
Naphthols
Nervous system diseases
Pharmacology
Presynaptic receptors
Rats
Receptors
Receptors, Dopamine - drug effects
Rotation
Synaptic Membranes - drug effects
Tetrahydronaphthalenes
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Summary:A new dopamine analog, 6,7-dihydroxy-2-dimethylaminotetralin (TL-99), was compared to apomorphine in three tests of dopaminergic function in the central nervous system. The tests, performed on rats, included production of changes in locomotor activity (involving both presynaptic and postsynaptic receptors), inhibition of dopa accumulation (quantifying presynaptic receptor activity), and the rotation model (quantifying postsynaptic receptor activation). Apomorphine was efficacious at both presynaptic and postsynaptic receptors, whereas TL-99 was much more efficacious at the presynaptic receptor. This result indicates not only that differences exist between presynaptic and postsynaptic dopamine receptors, but also that these differences may be exploited in the design of selective dopamine agonists.
ISSN:0036-8075
1095-9203
DOI:10.1126/science.7444443