
Bioorganic and Medicinal Chemistry p. 1293 - 1299 (1997)
Update date:2022-08-04
Topics:
Swahn, Britt-Marie
Edvinsson, Karin M.
Kallin, Elisabet
Larsson, Ulf
Berge, Odd-Geir
Molin, Hakan
Pelcman, Benjamin
Claesson, Alf
(2R,3S,1'R)-3-(1-Hydroxy-2-phosphonoethyl)-2-piperidinecarboxylic acid 1 has been synthesized by two different methods. The NMDA receptor binding affinities (K(i) values) are 74 nM for compound 1, and 64 nM for the corresponding ketone 2. The analgesic effects were evaluated using the mouse hot-plate test and the mouse formalin model. The ED50 values for the racemates of compounds 1 and 2, using the mouse hotplate and intrathecal injection, were 0.53 and 0.51 nmol, respectively.
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(1997)Doi:10.1021/jo01050a518
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(1997)