1606979-88-7Relevant articles and documents
Discovery of N-sulfonyl-7-azaindoline derivatives as potent, orally available and selective M4 muscarinic acetylcholine receptor agonists
Suwa, Atsushi,Konishi, Yasuko,Uruno, Yoshiharu,Takai, Kentaro,Nakako, Tomokazu,Sakai, Mutsuko,Enomoto, Takeshi,Ochi, Yoshiaki,Matsuda, Harumi,Kitamura, Atsushi,Uematsu, Yasuaki,Kiyoshi, Akihiko,Sumiyoshi, Takaaki
, p. 2909 - 2912 (2014)
We designed and synthesized novel N-sulfonyl-7-azaindoline derivatives as selective M4 muscarinic acetylcholine receptor agonists. Modification of the N-carbethoxy piperidine moiety of compound 2, an M4 muscarinic acetylcholine receptor (mAChR)-preferring agonist, led to compound 1, a selective M4 mAChR agonist. Compound 1 showed a highly selective M4 mAChR agonistic activity with weak hERG inhibition in vitro. A pharmacokinetic study of compound 1 in vivo revealed good bioavailability and brain penetration in rats. Compound 1 reversed methamphetamine-induced locomotor hyperactivity in rats (1-10 mg/kg, po).