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Titolo:
Platelet alpha(2)-adrenoceptor alterations in patients with essential hypertension
Autore:
Varani, K; Gessi, S; Caiazza, A; Rastelli, G; Portaluppi, F; Borea, PA;
Indirizzi:
Univ Ferrara, Dept Clin & Expt Med, Pharmacol Unit, I-44100 Ferrara, ItalyUniv Ferrara Ferrara Italy I-44100 harmacol Unit, I-44100 Ferrara, Italy Univ Ferrara, Dept Clin & Expt Med, Hypertens Unit, I-44100 Ferrara, ItalyUniv Ferrara Ferrara Italy I-44100 ypertens Unit, I-44100 Ferrara, Italy Hosp Fidenza, Div Med 1, Panna, Italy Hosp Fidenza Panna ItalyHosp Fidenza, Div Med 1, Panna, Italy
Titolo Testata:
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
fascicolo: 2, volume: 47, anno: 1999,
pagine: 167 - 172
SICI:
0306-5251(199902)47:2<167:PAAIPW>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
SYMPATHETIC-NERVE ACTIVITY; RECEPTOR SUBTYPE; BINDING; AGONIST; BRAIN; ALPHA-2-ADRENOCEPTORS; ADRENOCEPTORS; MICE;
Keywords:
[H-3]-UK 14304 binding; G proteins; cAMP; human platelets;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Borea, PA Univ19,rrara, Dept Clin & Expt Med, Pharmacol Unit, Via Fossato Mortara 17- Univ Ferrara Via Fossato Mortara 17-19 Ferrara Italy I-44100 7-
Citazione:
K. Varani et al., "Platelet alpha(2)-adrenoceptor alterations in patients with essential hypertension", BR J CL PH, 47(2), 1999, pp. 167-172

Abstract

Aims The purpose of this study was to determine whether human platelet alpha(2)-adrenoceptors were altered in essential hypertension. A systematic analysis was carried out on 165 normotensives and 124 untreated primary hypertensives. Methods The study was performed at different levels: i) density and affinity of platelet alpha(2)-adrenoceptors were determined by receptor binding assays using the full alpha(2)-adrenoceptor agonist [H-3]-UK 14304 and a thermodynamic analysis of data was carried out to evaluate if binding mechanisms at the molecular level were altered during hypertension; ii) the functionality of G(i) proteins coupled to alpha(2)-adrenoceptors and iii) forskolin-stimulated cAMP levels were measured. Results Platelet alpha(2)-adrenoceptors mean density (B-max) and affinity (K-d) (+/-s.e.mean) were significantly lower and higher, respectively, in normotensive than in hypertensive subjects [B-max=327+/-4 vs 435+/-5 fmol mg(-1) of protein (P<0.01) and K-d=3.76+/-0.05 vs 6.50+/-0.15 nM (P<0.01), respectively]. The 50% stimulating concentration of adrenaline on [S-35]-GTP gamma S binding to G(i) proteins was significantly (P<0.01) lower in normotensives (12+/-2 nM) than in hypertensives (110+/-10 nM). The 50% inhibitingconcentration of adrenaline on forskolin-stimulated cAMP levels was significantly (P<0.01) lower in normotensive (22+/-2 nM) than in hypertensive subjects (200+/-25 nM). Conclusions Present analysis, including receptorial and functional data, provides evidence that marked alterations occur in platelet alpha(2)-adrenoceptors of hypertensive subjects.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 05/12/20 alle ore 07:15:47