PMID- 14724045
OWN - NLM
STAT- MEDLINE
DCOM- 20040916
LR  - 20190712
IS  - 0091-3057 (Print)
IS  - 0091-3057 (Linking)
VI  - 77
IP  - 1
DP  - 2004 Jan
TI  - Comparative anticonvulsant activity of 
      N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives in 
      rodents.
PG  - 85-94
AB  - The anticonvulsant activity of competitive 
      2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo (F)-quinoxaline (NBQX) and noncompetitive 
      2,3-benzodiazepines and tetrahydroisoquinolines (THIQs) AMPA/kainate receptor 
      antagonists, was tested in different experimental seizure models and compared 
      with diazepam, a conventional antiepileptic drug acting on GABAergic 
      neurotransmission. In particular, the compounds were evaluated against audiogenic 
      and maximal electroshock seizures (MES) test and pentetrazol (PTZ) seizures 
      model, and all of them showed protective action. In addition, NBQX, 
      2,3-benzodiazepines and THIQs, but not diazepam, were also protective against 
      clonic and tonic seizures and lethality induced by kainate, AMPA and ATPA, but 
      were ineffective against NMDA-induced seizures. Only 2,3-benzodiazepines and some 
      THIQs were able to affect 4-aminopyridine- and mercaptopropionic-acid-induced 
      seizures. The duration of anticonvulsant action of 33 micromol/kg of some 
      2,3-benzodiazepines and THIQs was also investigated in DBA/2 mice, a strain 
      genetically susceptible to audiogenic seizures, and it was observed that the 
      derivative THIQ-10c, possessing an acetyl group at the N-2 and a chlorine atom on 
      the C-1 phenyl ring, showed higher anticonvulsant activity and longer-lasting 
      protective effects.
FAU - Ferreri, Guido
AU  - Ferreri G
AD  - Department of Experimental and Clinical Medicine, Faculty of Medicine and 
      Surgery, School of Medicine at Catanzaro, University of Catanzaro, Policlinico 
      Mater Domini, Via T. Campanella, 115, 88100, Catanzaro, Italy.
FAU - Chimirri, Alba
AU  - Chimirri A
FAU - Russo, Emilio
AU  - Russo E
FAU - Gitto, Rosaria
AU  - Gitto R
FAU - Gareri, Pietro
AU  - Gareri P
FAU - De Sarro, Angela
AU  - De Sarro A
FAU - De Sarro, Giovambattista
AU  - De Sarro G
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PL  - United States
TA  - Pharmacol Biochem Behav
JT  - Pharmacology, biochemistry, and behavior
JID - 0367050
RN  - 0 (Anticonvulsants)
RN  - 0 (Quinoxalines)
RN  - 0 (Receptors, AMPA)
RN  - 118876-58-7 (2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline)
SB  - IM
MH  - Animals
MH  - Anticonvulsants/pharmacology/*therapeutic use
MH  - Dose-Response Relationship, Drug
MH  - Male
MH  - Mice
MH  - Mice, Inbred DBA
MH  - Mice, Inbred ICR
MH  - Quinoxalines/pharmacology/*therapeutic use
MH  - Receptors, AMPA/antagonists & inhibitors/physiology
MH  - Seizures/*prevention & control
EDAT- 2004/01/16 05:00
MHDA- 2004/09/17 05:00
CRDT- 2004/01/16 05:00
PHST- 2004/01/16 05:00 [pubmed]
PHST- 2004/09/17 05:00 [medline]
PHST- 2004/01/16 05:00 [entrez]
AID - S009130570300296X [pii]
AID - 10.1016/j.pbb.2003.09.019 [doi]
PST - ppublish
SO  - Pharmacol Biochem Behav. 2004 Jan;77(1):85-94. doi: 10.1016/j.pbb.2003.09.019.