Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.
Imidazo[1,2-a]pyrimidines are GABA(A) receptor benzodiazepine binding site ligands which can exhibit functional selectivity for the alpha(3) subtype over the alpha(1) subtype. SAR studies to optimize this functional selectivity are described.
Blackaby
Wesley P
WP
Neuroscience Research Centre, Merck Sharp and Dohme Research Laboratories, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. Wesley_Blackaby@merck.com
Atack
John R
JR
Bromidge
Frances
F
Castro
José L
JL
Goodacre
Simon C
SC
Hallett
David J
DJ
Lewis
Richard T
RT
Marshall
George R
GR
Pike
Andrew
A
Smith
Alison J
AJ
Street
Leslie J
LJ
Tattersall
David F D
DF
Wafford
Keith A
KA
D007093:Imidazoles / Q000737:chemistry* / Q000378:metabolism*; D008024:Ligands; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D011963:Receptors, GABA-A / Q000378:metabolism*; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D007093:Imidazoles; D008024:Ligands; D011743:Pyrimidines; D011963:Receptors, GABA-A; C029899:imidazole