Matches in SemOpenAlex for { <https://semopenalex.org/work/W2042742187> ?p ?o ?g. }
- W2042742187 endingPage "5521" @default.
- W2042742187 startingPage "5506" @default.
- W2042742187 abstract "Enantiomeric propanolamines have been identified as a new class of NR2B-selective NMDA receptor antagonists. The most effective agents are biaryl structures, synthesized in six steps with overall yields ranging from 11−64%. The compounds are potent and selective inhibitors of NR2B-containing recombinant NMDA receptors with IC50 values between 30−100 nM. Potency is strongly controlled by substitution on both rings and the centrally located amine nitrogen. SAR analysis suggests that well-balanced polarity and chain-length factors provide the greatest inhibitory potency. Structural comparisons based on 3D shape analysis and electrostatic complementarity support this conclusion. The antagonists are neuroprotective in both in vitro and in vivo models of ischemic cell death. In addition, some compounds exhibit anticonvulsant properties. Unlike earlier generation NMDA receptor antagonists and some NR2B-selective antagonists, the present series of propanolamines does not cause increased locomotion in rodents. Thus, the NR2B-selective antagonists exhibit a range of therapeutically interesting properties." @default.
- W2042742187 created "2016-06-24" @default.
- W2042742187 creator A5017011355 @default.
- W2042742187 creator A5017733630 @default.
- W2042742187 creator A5029001528 @default.
- W2042742187 creator A5032077625 @default.
- W2042742187 creator A5036437571 @default.
- W2042742187 creator A5041161550 @default.
- W2042742187 creator A5041248710 @default.
- W2042742187 creator A5051202816 @default.
- W2042742187 creator A5051337572 @default.
- W2042742187 creator A5052162303 @default.
- W2042742187 creator A5055383235 @default.
- W2042742187 creator A5066071290 @default.
- W2042742187 creator A5070835383 @default.
- W2042742187 creator A5071096198 @default.
- W2042742187 creator A5074294267 @default.
- W2042742187 creator A5090502808 @default.
- W2042742187 creator A5091825209 @default.
- W2042742187 creator A5091897896 @default.
- W2042742187 date "2008-08-23" @default.
- W2042742187 modified "2023-10-03" @default.
- W2042742187 title "Enantiomeric Propanolamines as selective <i>N</i>-Methyl-<scp>d</scp>-aspartate 2B Receptor Antagonists" @default.
- W2042742187 cites W1499205986 @default.
- W2042742187 cites W1659149261 @default.
- W2042742187 cites W1801032533 @default.
- W2042742187 cites W1871698893 @default.
- W2042742187 cites W1898334791 @default.
- W2042742187 cites W1957958801 @default.
- W2042742187 cites W1970564284 @default.
- W2042742187 cites W1970696774 @default.
- W2042742187 cites W1971572370 @default.
- W2042742187 cites W1976946288 @default.
- W2042742187 cites W1984214553 @default.
- W2042742187 cites W1986011000 @default.
- W2042742187 cites W1987897200 @default.
- W2042742187 cites W1989363688 @default.
- W2042742187 cites W1991330780 @default.
- W2042742187 cites W1992709517 @default.
- W2042742187 cites W1993951077 @default.
- W2042742187 cites W2000641039 @default.
- W2042742187 cites W2009798253 @default.
- W2042742187 cites W2011191755 @default.
- W2042742187 cites W2011841319 @default.
- W2042742187 cites W2011867765 @default.
- W2042742187 cites W2012005596 @default.
- W2042742187 cites W2018987751 @default.
- W2042742187 cites W2022966746 @default.
- W2042742187 cites W2025882807 @default.
- W2042742187 cites W2027065525 @default.
- W2042742187 cites W2028569155 @default.
- W2042742187 cites W2029922642 @default.
- W2042742187 cites W2032008843 @default.
- W2042742187 cites W2040936201 @default.
- W2042742187 cites W2046902224 @default.
- W2042742187 cites W2049594669 @default.
- W2042742187 cites W2050039091 @default.
- W2042742187 cites W2050273205 @default.
- W2042742187 cites W2053980736 @default.
- W2042742187 cites W2055089768 @default.
- W2042742187 cites W2058311825 @default.
- W2042742187 cites W2059334396 @default.
- W2042742187 cites W2059401172 @default.
- W2042742187 cites W2061407282 @default.
- W2042742187 cites W2065169750 @default.
- W2042742187 cites W2066758358 @default.
- W2042742187 cites W2068387849 @default.
- W2042742187 cites W2077814219 @default.
- W2042742187 cites W2080519186 @default.
- W2042742187 cites W2085273994 @default.
- W2042742187 cites W2092325228 @default.
- W2042742187 cites W2094126290 @default.
- W2042742187 cites W2117745130 @default.
- W2042742187 cites W2121504583 @default.
- W2042742187 cites W2121853844 @default.
- W2042742187 cites W2122532139 @default.
- W2042742187 cites W2122595342 @default.
- W2042742187 cites W2126798549 @default.
- W2042742187 cites W2140899588 @default.
- W2042742187 cites W2146721393 @default.
- W2042742187 cites W2147421370 @default.
- W2042742187 cites W2153963727 @default.
- W2042742187 cites W2154142567 @default.
- W2042742187 cites W2159976043 @default.
- W2042742187 cites W2166114438 @default.
- W2042742187 cites W2168044729 @default.
- W2042742187 cites W2169079203 @default.
- W2042742187 cites W2169453051 @default.
- W2042742187 cites W2169867458 @default.
- W2042742187 cites W2172796270 @default.
- W2042742187 cites W2181212257 @default.
- W2042742187 cites W2328931461 @default.
- W2042742187 cites W2949574343 @default.
- W2042742187 cites W2951738192 @default.
- W2042742187 cites W2952999149 @default.
- W2042742187 cites W4315557979 @default.
- W2042742187 doi "https://doi.org/10.1021/jm8002153" @default.
- W2042742187 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3142473" @default.