Journal article icon

Journal article

Enantiomers of HA-966 (3-amino-1-hydroxypyrrolid-2-one) exhibit distinct central nervous system effects: (+)-HA-966 is a selective glycine/N-methyl-D-aspartate receptor antagonist, but (-)-HA-966 is a potent gamma-butyrolactone-like sedative.

Abstract:

The antagonist effect of (+/-)-3-amino-1-hydroxypyrrolid-2-one (HA-966) at the N-methyl-D-aspartate (NMDA) receptor occurs through a selective interaction with the glycine modulatory site within the receptor complex. When the enantiomers of (+/-)-HA-966 were resolved, the (R)-(+)-enantiomer was found to be a selective glycine/NMDA receptor antagonist, a property that accounts for its anticonvulsant activity in vivo. In contrast, the (S)-(-)-enantiomer was only weakly active as an NMDA-recepto...

Expand abstract
Publication status:
Published

Actions


Access Document


Publisher copy:
10.1073/pnas.87.1.347

Authors


Expand authors...
Journal:
Proceedings of the National Academy of Sciences of the United States of America
Volume:
87
Issue:
1
Pages:
347-351
Publication date:
1990-01-05
DOI:
EISSN:
1091-6490
ISSN:
0027-8424
URN:
uuid:74a3f50f-4203-4e7f-8c38-01051e1cac0c
Source identifiers:
15083
Local pid:
pubs:15083

Terms of use


Metrics


Views and Downloads






If you are the owner of this record, you can report an update to it here: Report update to this record

TO TOP