Ethyl 2-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-4-imidazolecarboxylate is a novel positive modulator of GABAA receptors
Language: 
English
Abstract: 

Ethyl 2-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-4-imidazolecarboxylate (TG41) enhanced the binding both of gamma-aminobutyric acid (GABA) and of flunitrazepam to rat cerebral cortical membranes. Electrophysiological recordings from Xenopus oocytes expressing various recombinant GABA(A) receptor subtypes revealed that TG41 enhanced the function of all receptor subunit combinations tested. The potency of TG41 at receptors containing alpha1, beta2, and gamma2L subunits was greater than that of alphaxalone, etomidate, propofol, or pentobarbital. The potency of TG41 was also greater at receptors containing alpha1 or alpha2 subunits than at those containing alpha4 and it was markedly higher at receptors containing beta2 or beta3 subunits than at those containing beta1. This drug induced a reversible loss of the righting reflex in Xenopus tadpoles and it elicited hypnosis (5 mg/kg) after intravenous administration in rats. These results indicate that the pharmacological profile of TG41 is similar to that of general anesthetics which potentiate the activity of GABA(A) receptors containing the beta2 or beta3 subunit.

Author(s): 
Mascia, Maria Paola
Asproni, Battistina
Busonero, Fabio
Talani, Giuseppe
Maciocco, Elisabetta
Pau, Amedeo
Cerri, Riccardo
Sanna, Enrico
Biggio, Giovanni
Item Type: 
Journal Article
Publication Title: 
European Journal of Pharmacology
Journal Abbreviation: 
Eur. J. Pharmacol.
Publication Date: 
6/15/2005
Publication Year: 
2005
Pages: 
204-211
Volume: 
516
Issue: 
3
ISSN: 
0014-2999
DOI: 
10.1016/j.ejphar.2005.05.006
Library Catalog: 
PubMed
Extra: 
PMID: 15967425

Turabian/Chicago Citation

Maria Paola Mascia, Battistina Asproni, Fabio Busonero, Giuseppe Talani, Elisabetta Maciocco, Amedeo Pau, Riccardo Cerri, Enrico Sanna and Giovanni Biggio. 6/15/2005. "Ethyl 2-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-4-imidazolecarboxylate is a novel positive modulator of GABAA receptors." European Journal of Pharmacology 516: 3: 204-211. 10.1016/j.ejphar.2005.05.006.

Wikipedia Citation

<ref> {{Cite journal | doi = 10.1016/j.ejphar.2005.05.006 | issn = 0014-2999 | volume = 516 | pages = 204-211 | last = Mascia | first = Maria Paola | coauthors = Asproni, Battistina, Busonero, Fabio, Talani, Giuseppe, Maciocco, Elisabetta, Pau, Amedeo, Cerri, Riccardo, Sanna, Enrico, Biggio, Giovanni | title = Ethyl 2-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-4-imidazolecarboxylate is a novel positive modulator of GABAA receptors | journal = European Journal of Pharmacology | date = 6/15/2005 | pmid = | pmc = }} </ref>