Synthesis of polyamine derivatives having non-hypotensive Ca2 +-permeable AMPA receptor antagonist activity.
In order to obtain non-hypotensive and Ca2+-permeable AMPA receptor antagonists, we have synthesized a series of 1,4-bis(4-piperidinylmethyl)diaminobutanes. Compounds 13b, c, f had desirable properties.
Yoneda
Y
Y
Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co, Ltd, Tokyo, Japan. yonedL0z@daiichipharm.co.jp
Kawajiri
S
S
Hasegawa
A
A
Kito
F
F
Katano
S
S
Takano
E
E
Mimura
T
T
D000818:Animals; D015317:Biogenic Polyamines / Q000138:chemical synthesis / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D015220:Calcium Channels / Q000187:drug effects*; D003959:Diamines / Q000138:chemical synthesis / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007275:Injections, Intravenous; D018696:Neuroprotective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D018408:Patch-Clamp Techniques; D011073:Polyamines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014981:Xenopus
D015317:Biogenic Polyamines; D015220:Calcium Channels; D003959:Diamines; D018696:Neuroprotective Agents; D011073:Polyamines; D018091:Receptors, AMPA