PMID- 8982663
OWN - NLM
STAT- MEDLINE
DCOM- 19970326
LR  - 20190624
IS  - 0014-2999 (Print)
IS  - 0014-2999 (Linking)
VI  - 315
IP  - 3
DP  - 1996 Nov 21
TI  - (R,S)-3,4-dichlorobenzoylalanine (FCE 28833A) causes a large and persistent 
      increase in brain kynurenic acid levels in rats.
PG  - 263-7
AB  - Kynurenic acid is an endogenous excitatory amino-acid receptor antagonist with 
      neuroprotective and anticonvulsant properties. We demonstrate here that systemic 
      administration of the new and potent kynurenine 3-hydroxylase inhibitor 
      (R,S)-3,4-dichlorobenzoylalanine (FCE 28833A) causes a dose-dependent elevation 
      in endogenous kynurenine and kynurenic acid levels in rat brain tissue. In 
      hippocampal microdialysates, peak increases of 10- and 80-fold above basal 
      kynurenic acid concentrations, respectively, were obtained after a single oral or 
      intraperitoneal administration of 400 mg/kg FCE 28833A. After intraperitoneal 
      treatment with FCE 28833A, extracellular brain kynurenic acid levels remained 
      significantly elevated for at least 22 h, rendering this compound a far more 
      effective enhancer of kynurenic acid levels than the previously described 
      kynurenine 3-hydroxylase blocker m-nitrobenzoylalanine. FCE 28833A and similar 
      molecules may have therapeutic value in diseases which are linked to a 
      hyperfunction of excitatory amino-acid receptors.
FAU - Speciale, C
AU  - Speciale C
AD  - Pharmacia & Upjohn, R & D-CNS, Milano, Italy.
FAU - Wu, H Q
AU  - Wu HQ
FAU - Cini, M
AU  - Cini M
FAU - Marconi, M
AU  - Marconi M
FAU - Varasi, M
AU  - Varasi M
FAU - Schwarcz, R
AU  - Schwarcz R
LA  - eng
GR  - NS 16102/NS/NINDS NIH HHS/United States
GR  - NS 28236/NS/NINDS NIH HHS/United States
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (Butyrates)
RN  - 0 (FCE 28833)
RN  - 0 (Neuroprotective Agents)
RN  - H030S2S85J (Kynurenic Acid)
SB  - IM
MH  - Animals
MH  - Brain/*drug effects/metabolism
MH  - Butyrates/*pharmacology
MH  - Kynurenic Acid/*metabolism
MH  - Male
MH  - Neuroprotective Agents/*pharmacology
MH  - Rats
MH  - Rats, Wistar
EDAT- 1996/11/21 00:00
MHDA- 1996/11/21 00:01
CRDT- 1996/11/21 00:00
PHST- 1996/11/21 00:00 [pubmed]
PHST- 1996/11/21 00:01 [medline]
PHST- 1996/11/21 00:00 [entrez]
AID - S0014299996006139 [pii]
AID - 10.1016/s0014-2999(96)00613-9 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 1996 Nov 21;315(3):263-7. doi: 10.1016/s0014-2999(96)00613-9.