Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
Atipamezole, an imidazoline-type alpha(2)-adrenoceptor inhibitor, binds tohuman platelets and inhibits their adrenaline-induced aggregation more effectively than yohimbine
Autore:
Mustonen, P; Savola, JM; Lassila, R;
Indirizzi:
Wihuri Res Inst, SF-00140 Helsinki, Finland Wihuri Res Inst Helsinki Finland SF-00140 st, SF-00140 Helsinki, Finland Juvantia Pharma Ltd, Biocity, Turku, Finland Juvantia Pharma Ltd Turku Finland a Pharma Ltd, Biocity, Turku, Finland Univ Helsinki, Cent Hosp, Dept Med, Helsinki, Finland Univ Helsinki Helsinki Finland , Cent Hosp, Dept Med, Helsinki, Finland
Titolo Testata:
THROMBOSIS RESEARCH
fascicolo: 3, volume: 99, anno: 2000,
pagine: 231 - 237
SICI:
0049-3848(20000801)99:3<231:AAIAIB>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
ANTAGONIST BINDING; BLOOD-PLATELETS; H-3 ATIPAMEZOLE; EPINEPHRINE; ALPHA-2-ADRENOCEPTORS; MEDETOMIDINE; SELECTIVITY; SUBTYPES; SITES;
Keywords:
alpha(2)-adrenoceptors; platelets; atipamezole; yohimbine; adrenaline;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
21
Recensione:
Indirizzi per estratti:
Indirizzo: Lassila, R Wihuri Res Inst, Kalliolinnantie 4, SF-00140 Helsinki, Finland Wihuri Res Inst Kalliolinnantie 4 Helsinki Finland SF-00140 nd
Citazione:
P. Mustonen et al., "Atipamezole, an imidazoline-type alpha(2)-adrenoceptor inhibitor, binds tohuman platelets and inhibits their adrenaline-induced aggregation more effectively than yohimbine", THROMB RES, 99(3), 2000, pp. 231-237

Abstract

To investigate the usefulness of atipamezole [MPV-1248, 4-(2-ethyl-2,3-dihydro-1H-inden-2-yl)-1H-imidazole], a novel alpha(2)-adrenoceptor-specific antagonist, as a tool in platelet studies, the ability of this antagonist: (1) to bind to platelet alpha(2)-adrenoceptors, and (2) to inhibit adrenaline-induced platelet aggregation was compared to that of yohimbine, another commonly used alpha(2)-adrenoceptor antagonist. It was found that atipamezole binds to platelet alpha(2)-adrenoceptors more effectively than yohimbine:[H-3]atipamezole has more than three times higher alpha(2)-adrenoceptor binding affinity in intact gel-filtered human platelets (equilibrium dissociation constant (K-d) 0.7+/-0.21 vs. 2.9=/-0.77 nM, p<0.05), but only one-third of the binding capacity of [H-3]yohimbine (B-max 27.0+/-3.8 vs. 100+/-19pM/ 10(5) cells, p<0.0l). Functionally, in comparison with yohimbine, an almost threefold lower concentration of atipamezole inhibited adrenaline (5 mu M)- induced platelet aggregation. A concentration of atipamezole, which inhibited this aggregation by 50% (IC50), was 0.37+/-0.07 mu M, whereas IC50 for yohimbine was 0.98+/-0.12 mu M, p<0.0001. Thus, atipamezole represents a functionally undisputed alpha(2)-adrenoceptor antagonist, more effective than yohimbine. Its distinct binding profile as a radioligand also suggests the presence of imidazol(in)e binding sites in platelets. (C) 2000 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 19/01/20 alle ore 09:27:06