Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5).
Studies of structure-activity relationships for the linker in a new series of metabotropic glutamate receptor 5 antagonists are presented together with in vitro and in vivo pharmacokinetic data.
Bach
Peter
P
Department of Medicinal Chemistry, AstraZeneca R&D Mölndal, Pepparedsleden 1, S-431 83 Mölndal, Sweden. Peter.Bach@astrazeneca.com
Nilsson
Karolina
K
Svensson
Tor
T
Bauer
Udo
U
Hammerland
Lance G
LG
Peterson
Alecia
A
Wållberg
Andreas
A
Osterlund
Krister
K
Karis
David
D
Boije
Maria
M
Wensbo
David
D
D000480:Alkynes / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D003432:Cross-Linking Reagents / Q000737:chemistry*; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D015394:Molecular Structure; D011725:Pyridines / Q000737:chemistry*; D051381:Rats; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000480:Alkynes; D003432:Cross-Linking Reagents; C578937:Grm5 protein, rat; D011725:Pyridines; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate; C023666:pyridine