Non-amine-based dopamine transporter (reuptake) inhibitors retain properties of amine-based progenitors
| Autor: | Michele A. Fahey, Susan R. George, Ali A. Bonab, Bertha K. Madras, Eli Livni, Richard De La Garza, Martin Goulet, Peter C. Meltzer, Alan J. Fischman, Brian F. O'Dowd, Roger D. Spealman, Gregory M. Miller |
|---|---|
| Rok vydání: | 2003 |
| Předmět: |
Male
Biogenic Amines Dopamine Plasma Membrane Transport Proteins Nerve Tissue Proteins Pharmacology Structure-Activity Relationship Dopamine Uptake Inhibitors Dopamine Membrane Transport Modulators Reaction Time medicine Animals Rats Wistar Saimiri Serotonin transporter Dopamine transporter Membrane Glycoproteins Dose-Response Relationship Drug biology Chemistry Brain Membrane Transport Proteins Transporter Macaca mulatta Rats Monoamine neurotransmitter Biochemistry biology.protein Catecholamine Reuptake inhibitor medicine.drug |
| Zdroj: | European Journal of Pharmacology. 479:41-51 |
| ISSN: | 0014-2999 |
| DOI: | 10.1016/j.ejphar.2003.08.055 |
| Popis: | 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: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect