The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure.
The identification of a highly selective D(2) partial agonist, D(3) antagonist tool molecule which demonstrates high levels of brain exposure and selectivity against an extensive range of dopamine, serotonin, adrenergic, histamine, and muscarinic receptors is described.
Holmes
Ian P
IP
GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK.
Blunt
Richard J
RJ
Lorthioir
Olivier E
OE
Blowers
Stephen M
SM
Gribble
Andy
A
Payne
Andrew H
AH
Stansfield
Ian G
IG
Wood
Martyn
M
Woollard
Patrick M
PM
Reavill
Charlie
C
Howes
Claire M
CM
Micheli
Fabrizio
F
Di Fabio
Romano
R
Donati
Daniele
D
Terreni
Silvia
S
Hamprecht
Dieter
D
Arista
Luca
L
Worby
Angela
A
Watson
Steve P
SP
D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D018491:Dopamine Agonists / Q000494:pharmacology*; D018492:Dopamine Antagonists / Q000494:pharmacology*; D017448:Receptors, Dopamine D2 / Q000819:agonists*; D050637:Receptors, Dopamine D3 / Q000037:antagonists & inhibitors*
D018491:Dopamine Agonists; D018492:Dopamine Antagonists; D017448:Receptors, Dopamine D2; D050637:Receptors, Dopamine D3