Autor: |
Madras BK; Department of Psychiatry, Harvard Medical School, New England Primate Research Center, 1 Pine Hill Drive, Southborough, MA 01772-9102, USA. bertha_madras@hms.harvard.edu, Fahey MA, Miller GM, De La Garza R, Goulet M, Spealman RD, Meltzer PC, George SR, O'Dowd BF, Bonab AA, Livni E, Fischman AJ |
Jazyk: |
angličtina |
Zdroj: |
European journal of pharmacology [Eur J Pharmacol] 2003 Oct 31; Vol. 479 (1-3), pp. 41-51. |
DOI: |
10.1016/j.ejphar.2003.08.055 |
Abstrakt: |
Without exception, therapeutic and addictive drugs that produce their primary effects by blocking monoamine transporters in brain contain an amine nitrogen in their structure. This fundamental canon of drug design was based on a prevailing premise that an amine nitrogen is required to mimic the structures of monoamine neurotransmitters and other natural products. Non-amines, a novel class of compounds that contain no amine nitrogen, block monoamine transporters in the nM range and display markedly high selectivity for monoamine transporters, but not for receptors. Non-amines retain the spectrum of biochemical and pharmacological properties characteristic of amine-bearing counterparts. These novel drugs compel a revision of current concepts of drug-monoamine transporter complex formation and open avenues for discovery of a new generation of therapeutic drugs. |
Databáze: |
MEDLINE |
Externí odkaz: |
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