Synthesis of diaminobutane derivatives as potent Ca(2+)-permeable AMPA receptor antagonists.
We synthesized diaminobutane derivatives as potent Ca(2+)-permeable AMPA receptor antagonists with non-hypotensive activity. Compound 10c showed selective Ca(2+)-permeable AMPA receptor antagonist activity and neuroprotective effects in transient global ischemia models in gerbils.
Yoneda
Y
Y
Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd., 16-13, Kitakasai 1-Chome, Edogawa-ku, Tokyo 134-8630, Japan. yoned10z@diichipharm.co.jp
Kawajiri
S
S
Sugimura
M
M
Osanai
K
K
Kito
F
F
Ota
E
E
Mimura
T
T
D000818:Animals; D002118:Calcium / Q000378:metabolism*; D004195:Disease Models, Animal; D005849:Gerbillinae; D007511:Ischemia / Q000517:prevention & control; D018696:Neuroprotective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D011700:Putrescine / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors* / Q000378:metabolism
D018696:Neuroprotective Agents; D018091:Receptors, AMPA; D002118:Calcium; D011700:Putrescine