Non-competitive inhibitors of metabotropic glutamate receptor 5 (mGluR5).
Based on a pharmacophore alignment on known non-competitive mGluR5 inhibitors applying 4SCan technology, a new lead series was identified and further structurally investigated. K(i)'s as low as around 100 nM were achieved.
Tasler
Stefan
S
4SC AG, Martinsried, Germany. stefan.tasler@4sc.com
Kraus
Jürgen
J
Pegoraro
Stefano
S
Aschenbrenner
Andrea
A
Poggesi
Elena
E
Testa
Rodolfo
R
Motta
Gianni
G
Leonardi
Amedeo
A
D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry / Q000494:pharmacology*; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D018691:Excitatory Amino Acid Antagonists; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate