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Titolo:
Characterization of a new radioiodinated probe for the alpha(2C) adrenoceptor in the mouse brain
Autore:
Dossin, O; Mouledous, L; Baudry, X; Tafani, JAM; Mazarguil, H; Zajac, JM;
Indirizzi:
CNRS, UPR 9062, Inst Pharmacol & Biol Struct, F-31077 Toulouse, France CNRS Toulouse France F-31077 col & Biol Struct, F-31077 Toulouse, France CHU Purpan, Serv Biophys & Med Nucl, F-31059 Toulouse, France CHU Purpan Toulouse France F-31059 & Med Nucl, F-31059 Toulouse, France
Titolo Testata:
NEUROCHEMISTRY INTERNATIONAL
fascicolo: 1, volume: 36, anno: 2000,
pagine: 7 - 18
SICI:
0197-0186(200001)36:1<7:COANRP>2.0.ZU;2-4
Fonte:
ISI
Lingua:
ENG
Soggetto:
CENTRAL-NERVOUS-SYSTEM; ALPHA-2-ADRENERGIC RECEPTOR SUBTYPES; MESSENGER-RNA EXPRESSION; RAT-BRAIN; H-3 RAUWOLSCINE; BINDING-SITES; ALPHA(2)-ADRENOCEPTOR SUBTYPES; ADRENERGIC-RECEPTOR; REGIONAL DISTRIBUTION; INSITU HYBRIDIZATION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
61
Recensione:
Indirizzi per estratti:
Indirizzo: Zajac, JM CNRS, UPR 9062, Inst Pharmacol & Biol Struct, 205 Route Narbonne, F-31077 Toulouse, France CNRS 205 Route Narbonne Toulouse France F-31077oulouse, France
Citazione:
O. Dossin et al., "Characterization of a new radioiodinated probe for the alpha(2C) adrenoceptor in the mouse brain", NEUROCHEM I, 36(1), 2000, pp. 7-18

Abstract

[I-125]17 alpha-hydroxy-20 alpha-yohimban-16 beta-(N-4-hydroxyphenethyl)carboxamide or [I-125]rauwolscine-OHPC, a new radioiodinated probe derived from rauwolscine was synthesized and its binding characteristics investigatedon sections of the mouse caudate putamen. [I-125]rauwolscine-OHPC binding was saturable and revealed interaction with a single class of binding sites(K-D = 0.171 nM, B-max = 3082 pCi/mg of tissue). The kinetically derived affinity was in close agreement with the affinity evaluated by saturation experiments: k(-1)/k(+1) (0.0403 min(-1)/114 10(6) M(-1)min(-1))=0.35 nM. Competition studies revealed interaction with one single class of binding sites for each of the twelve compounds tested. The rank of potency suggested aninteraction with alpha(2) adrenoceptors (atipamezole greater than or equalto RX 821002 > yohimbine > (-)epinephrine). Moreover, the good affinity of[I-125] rauwolscine-OHPC binding sites for spiroxatrine, yohimbine, WE 4101, the relatively good affinity for prazosin (K-i=37.4 nM) and the affinityratio prazosin/oxymetazoline (37.4/43.4= 0.86) were consistent with an alpha(2C) selective labelling of [I-125]rauwolscine-OHPC. The distribution of [I-125]rauwolscine-OHPC binding sites in mouse brain was characterized by autoradiography. The density of binding sites was high in the islands of Calleja, accumbens nucleus, caudate putamen and olfactory tubercles, moderate in the hippocampus, amygdala and anterodorsal nucleus of the thalamus. These findings demonstrated that [I-125]rauwolscine-OHPC is a useful radioiodinated probe to label alpha(2C) adrenoceptors in mouse brain. (C) 1999 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/09/20 alle ore 04:19:54