Polypharmacology of dopamine receptor ligands.

Abstract:

:Most neurological diseases have a multifactorial nature and the number of molecular mechanisms discovered as underpinning these diseases is continuously evolving. The old concept of developing selective agents for a single target does not fit with the medical need of most neurological diseases. The development of designed multiple ligands holds great promises and appears as the next step in drug development for the treatment of these multifactorial diseases. Dopamine and its five receptor subtypes are intimately involved in numerous neurological disorders. Dopamine receptor ligands display a high degree of cross interactions with many other targets including G-protein coupled receptors, transporters, enzymes and ion channels. For brain disorders like Parkinsońs disease, schizophrenia and depression the dopaminergic system, being intertwined with many other signaling systems, plays a key role in pathogenesis and therapy. The concept of designed multiple ligands and polypharmacology, which perfectly meets the therapeutic needs for these brain disorders, is herein discussed as a general ligand-based concept while focusing on dopaminergic agents and receptor subtypes in particular.

journal_name

Prog Neurobiol

journal_title

Progress in neurobiology

authors

Butini S,Nikolic K,Kassel S,Brückmann H,Filipic S,Agbaba D,Gemma S,Brogi S,Brindisi M,Campiani G,Stark H

doi

10.1016/j.pneurobio.2016.03.011

subject

Has Abstract

pub_date

2016-07-01 00:00:00

pages

68-103

eissn

0301-0082

issn

1873-5118

pii

S0301-0082(16)30048-X

journal_volume

142

pub_type

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