Novel non-peptide ligands for the somatostatin sst3 receptor.
A series of imidazole derivatives has been prepared using high throughput parallel synthesis. Several compounds showed high affinity (Ki in 10(-6)-10(-8) M range) and selectivity at recombinant human somatostatin receptor subtype 3 (hsst3).
Moinet
C
C
Institut Henri Beaufour, Les Ulis, France. christophe.moinet@beaufour-ipsen.com
Contour-Galcéra
M O
MO
Poitout
L
L
Morgan
B
B
Gordon
T
T
Rouber
P
P
Thurieau
C
C
D000577:Amides / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D001665:Binding Sites / Q000502:physiology; D016466:CHO Cells; D005576:Colforsin / Q000494:pharmacology*; D006224:Cricetinae; D000242:Cyclic AMP / Q000819:agonists* / Q000032:analysis / Q000096:biosynthesis; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology; D008024:Ligands; D009578:Nitrobenzenes / Q000138:chemical synthesis / Q000494:pharmacology*; D011485:Protein Binding / Q000502:physiology; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013004:Somatostatin / Q000494:pharmacology*
D000577:Amides; D007093:Imidazoles; C429627:L796778; D008024:Ligands; D009578:Nitrobenzenes; D017481:Receptors, Somatostatin; D011994:Recombinant Proteins; C103631:somatostatin receptor 3; D005576:Colforsin; D013004:Somatostatin; D000242:Cyclic AMP