http://www.cnr.it/ontology/cnr/individuo/prodotto/ID16491

Interactions of taurine and structurally related analogues with GABAergic system and taurine binding sites of rabbit brain. (Articolo in rivista)

Type

Articolo in rivista (Classe)
Prodotto della ricerca (Classe)

Label

Interactions of taurine and structurally related analogues with GABAergic system and taurine binding sites of rabbit brain. (Articolo in rivista) (literal)

Anno

2003-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

10.1038/sj.bjp.0705134 (literal)

Alternative label

Frosini, Maria; Sesti Casilde; Dragoni, Stefania; Valoti, Massimo; Palmi, Mitri; Dixon, Henry B. F.; Machetti, Fabrizio; Sgaragli Giampietro. (2003)
Interactions of taurine and structurally related analogues with GABAergic system and taurine binding sites of rabbit brain.
in British journal of pharmacology; Nature Publishing Group, London (Regno Unito)
(literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

Frosini, Maria; Sesti Casilde; Dragoni, Stefania; Valoti, Massimo; Palmi, Mitri; Dixon, Henry B. F.; Machetti, Fabrizio; Sgaragli Giampietro. (literal)

Pagina inizio

1163 (literal)

Pagina fine

1171 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#url

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC1573748/ (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

138 (literal)

Rivista

British journal of pharmacology (Rivista)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali

9 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo

6 (literal)

Note

Pubme (literal)
Scopu (literal)
ISI Web of Science (WOS) (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

Istituto di chimica dei composti organometallici del CNR Dipartimento di chimica Organica 'Ugo Schiff' dell'Università di Firenze University of Cambridge, Department of Biochemestry, Cambridge, England Istituto di Scienze Farmacologiche dell'università di Siena (literal)

Titolo

Interactions of taurine and structurally related analogues with GABAergic system and taurine binding sites of rabbit brain. (literal)

Abstract

The aim of this studywas to find taurinergic compounds that do not interact with brain GABA ergic systems. Washed synaptic membranes (SM) from whole rabbit brain were able to bind [3H]muscimol. Saturation experiments of the binding of [3H]GABA to GABAB receptors showed that SM possess two binding components; twice Triton X-100-treated SM contained 0.048 mmol endogenous taurine/ kg protein and bound [3H]taurine in a saturable manner (Kd¼249.076.3 nm and Bmax3.471.0 pmol mg_1 prot). Among the 19 structural analogues of taurine, 6-aminomethyl-3-methyl-4H-1,2,4-benzothiadiazine 1,1-dioxide (TAG), 2-aminoethylarsonic (AEA), 2-hydroxyethanesulfonic (ISE) and (7)cis-2- aminocyclohexane sulfonic acids (CAHS) displaced [3H]taurine binding (K0.13, 0.13, 13.5 and 4.0 mm, respectively). These analogues did not interact with GABAA and GABAB receptors and did not affect taurine- and GABA-uptake systems and GABA-transaminase activity. 3-Aminopropanesulfonic acid (OMO), b-alanine, pyridine-3-sulfonic acid, N,N,N-trimethyltaurine (TMT), 2-(guanidino)ethanesulfonic acid (GES), ethanolamine-O-sulphate, N,N-dimethyltaurine (DMT), taurine and (7)piperidine-3-sulfonic acid (PSA) inhibited [3H]muscimol binding to GABAA receptors with different affinities (Ki¼0.013, 7.9, 24.6, 47.5, 52.0, 91.0, 47.5, 118.1 and 166.3 mm, respectively). Taurine, 2-aminoethylphosphonic acid, DMT, TMT and OMO inhibited the binding of [3H]GABA to GABAB receptors with Kis in the mm range (0.8, 3.5, 4.4, 11.3 and 5.0, respectively). GES inhibited taurine uptake (IC50 3.72 mm) and PSA GABA transaminase activity(IC50103.0 mm). In conclusion, AEA, TAG, ISE and CAHS fulfill the criteria for taurinergic agents. (literal)

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