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Titolo:
Binding affinity profile of betahistine and its metabolites for central histamine receptors of rodents
Autore:
Fossati, A; Barone, D; Benvenuti, C;
Indirizzi:
Prodotti Formenti Srl, Dept Res, I-20149 Milan, Italy Prodotti Formenti Srl Milan Italy I-20149 Dept Res, I-20149 Milan, Italy LCC RMB SpA, Ist Ric Biomed Antoine Marxer, I-10010 Turin, Italy LCC RMB SpA Turin Italy I-10010 med Antoine Marxer, I-10010 Turin, Italy
Titolo Testata:
PHARMACOLOGICAL RESEARCH
fascicolo: 4, volume: 43, anno: 2001,
pagine: 389 - 392
SICI:
1043-6618(200104)43:4<389:BAPOBA>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
DOUBLE-BLIND; INHIBITION; VERTIGO; PLACEBO; DISEASE; RELEASE; CORTEX; BRAIN; FROG;
Keywords:
betahistine; betahistine metabolites; histamine receptors;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Fossati, A Prodotti Formenti Srl, Dept Res, Via Correggio 43, I-20149 Milan, Italy Prodotti Formenti Srl Via Correggio 43 Milan Italy I-20149 aly
Citazione:
A. Fossati et al., "Binding affinity profile of betahistine and its metabolites for central histamine receptors of rodents", PHARMAC RES, 43(4), 2001, pp. 389-392

Abstract

In order to clarify the interaction of betahistine (BH) and its metabolites [aminoethylpyridine (AEP) and hydroxyethylpyridine (HEP)] for receptors that mediate the physio-pharmacological activities of histamine. we performed in vitro competition binding studies to obtain their binding affinity profile for H-1-, H-2- and H-3-histamine receptors prepared from rodent brains. Crude synaptosomal membranes were incubated in the absence (total binding)or presence of the unlabelled ligands used to saturate the specific binding, or with different concentrations of BH, AEP or HEP. Receptor binding methods were validated by running known standard drugs together with the test compounds. Like histamine. only BH interacted with H-1-histamine receptors with comparable affinity (around 10(-5) M). BH and its metabolite AEP both interacted with the H-3-histamine receptors, with muM affinity. HEP still showed some affinity for the H-3-receptors but with a K-i only 1/50 that of the parent compound. Histamine showed 10(-8) M affinity fur the H-3-receptor sites and was the only ligand to intel act with H-2-histamine receptors, all the others giving affinities above the mM range,Hill coefficients (as slopes of the sigmoidal inhibition isotherms) were close to unity for BH against H-1- and H-3-binding sites and for AEP againstH-3-sites, indicating that these interactions take place in the absence ofcooperativity. Histamine and HEP interacted with H-1- and H-3-receptors with a Hill coefficient less than unity for the former and higher than unity for the latter (presence of negative and positive cooperativity, respectively). The results suggest that BH and its metabolites may act as neurotransmitter modulators of the histaminergic system. (C) 2001 Academic press.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/10/20 alle ore 11:31:18