Journal article
SYNTHESIS, NMDA RECEPTOR ANTAGONIST ACTIVITY, AND ANTICONVULSANT ACTION OF 1-AMINOCYCLOBUTANECARBOXYLIC ACID-DERIVATIVES
Journal of Medicinal Chemistry, Vol.37(25), pp.4288-4296
Dec/1994
Abstract
A range of cis- and trans-3-substituted 1-aminocyclobutane-1-carboxylic acids has been synthesized and evaluated for antagonism at excitatory amino acid receptor sites and for anticonvulsant activity. Potent and selective antagonist:activity at N-methyl-D-aspartate (NMDA) receptor sites in neonatal rat motoneurones was shown by compounds in which the 3-substituent was, or contained, a 2'-carboxyethyl or 2'-phosphonoethyl moiety. Substances 4b, 24, 35, and 40 were more potent than the standard NMDA receptor antagonist, D-2-amino-5-phosphonopentanoate (D-AP5) as NMDA antagonists in this preparation, and about equipotent with [3-(+/-)-2-carboxypiperazin-4-yl)-1-propyl]phosphonate (CPP). Anticonvulsant activity, as assessed following intracerebroventricular injection into audiogenic DBA/2 mice, generally paralleled NMDA receptor antagonist activity.
Details
- Title
- SYNTHESIS, NMDA RECEPTOR ANTAGONIST ACTIVITY, AND ANTICONVULSANT ACTION OF 1-AMINOCYCLOBUTANECARBOXYLIC ACID-DERIVATIVES
- Creators
- Y GAONI (null)AG CHAPMAN (null)N PARVEZ (null)PCK POOK (null)DE JANE (null)JC WATKINS (null)
- Resource Type
- Journal article
- Publication Details
- Journal of Medicinal Chemistry, Vol.37(25), pp.4288-4296; Dec/1994
- Number of pages
- 9
- Language
- English
- DOI
- https://doi.org/10.1021/jm00051a005
- Scientific Unit
- The Weizmann Institute of Science
- Record Identifier
- 993263335203596
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