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.
GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discovery, New Frontiers Science Park, Harlow, UK.
Ian P
IP
Holmes
Richard J
RJ
Blunt
Olivier E
OE
Lorthioir
Stephen M
SM
Blowers
Andy
A
Gribble
Andrew H
AH
Payne
Ian G
IG
Stansfield
Martyn
M
Wood
Patrick M
PM
Woollard
Charlie
C
Reavill
Claire M
CM
Howes
Fabrizio
F
Micheli
Romano
R
Di Fabio
Daniele
D
Donati
Silvia
S
Terreni
Dieter
D
Hamprecht
Luca
L
Arista
Angela
A
Worby
Steve P
SP
Watson
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