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VOLUME 21, ISSUE 5, P187-193, MAY 01, 2000
Abstract
Recent evidence suggests that agmatine, which is an intermediate in polyamine biosynthesis,
might be an important neurotransmitter in mammals. Agmatine is synthesized in the
brain, stored
in synaptic vesicles in regionally selective neurons, accumulated by
uptake, released by
depolarization, and inactivated by agmatinase. Agmatine binds
to α2-adrenoceptors and
imidazoline binding sites, and blocks NMDA receptor channels and
other ligand-gated cationic
channels. Furthermore, agmatine inhibits nitric oxide
synthase, and induces the release of some
peptide hormones. As a result of its ability
to inhibit both hyperalgesia and tolerance to, and
withdrawal from, morphine, and
its neuroprotective activity, agmatine has potential as a
treatment of chronic pain,
addictive states and brain injury.
Keywords
Pharmacology • Neuroscience • Physiology
Keywords
Agmatine • NMDA • Arginine decarboxylase • Agmatinase • Imidazoline receptor
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Glossary
Chemical name
UK14304:
5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-6-quinoxalinamine
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Article Info
Identification
DOI: https://doi.org/10.1016/S0165-6147(00)01460-7
Copyright
© 2000 Elsevier Science Ltd. Published by Elsevier Inc. All rights reserved.
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