Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
[H-3]RS79948-197 BINDING TO HUMAN, RAT, GUINEA-PIG AND PIG ALPHA(2A)-ADRENOCEPTOR, ALPHA(2B)-ADRENOCEPTOR AND ALPHA(2C)-ADRENOCEPTOR - COMPARISON WITH MK912, RX821002, RAUWOLSCINE AND YOHIMBINE
Autore:
UHLEN S; DAMBROVA M; NASMAN J; SCHIOTH HB; GU YC; WIKBERGMATSSON A; WIKBERG JES;
Indirizzi:
UPPSALA UNIV,DIV PHARMACOL,DEPT PHARMACEUT BIOSCI,BIOMED CTR,BOX 591 S-75124 UPPSALA SWEDEN UPPSALA UNIV,DEPT PHYSIOL & MED BIOPHYS S-75124 UPPSALA SWEDEN
Titolo Testata:
European journal of pharmacology
fascicolo: 1, volume: 343, anno: 1998,
pagine: 93 - 101
SICI:
0014-2999(1998)343:1<93:[BTHRG>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
H-3 RX821002; ALPHA(2)-ADRENOCEPTOR SUBTYPES; ALPHA-2-ADRENERGIC RECEPTORS; ADRENERGIC-RECEPTORS; RADIOLIGAND BINDING; CEREBRAL-CORTEX; HIGH-AFFINITY; HUMAN BRAIN; 2 FORMS; ALPHA(2A)-ADRENOCEPTORS;
Keywords:
[H-3]RS79948-197; MK912; ADRENOCEPTOR, SUBTYPE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
36
Recensione:
Indirizzi per estratti:
Citazione:
S. Uhlen et al., "[H-3]RS79948-197 BINDING TO HUMAN, RAT, GUINEA-PIG AND PIG ALPHA(2A)-ADRENOCEPTOR, ALPHA(2B)-ADRENOCEPTOR AND ALPHA(2C)-ADRENOCEPTOR - COMPARISON WITH MK912, RX821002, RAUWOLSCINE AND YOHIMBINE", European journal of pharmacology, 343(1), 1998, pp. 93-101

Abstract

The K-d values of the recently introduced radioligand [H-3]RS79948-197 ylsulphonyl)-6H-isoquino[2,1-g][1,6]naphthyridine) were determined for the recombinant human and rat alpha(2A)-, alpha(2B)- and alpha(2C)-as well as guinea pig alpha(2B)- and alpha(2C)-adrenoceptors expressed in COS (CV-1 Origin, SV40) cells. In addition, the K-d values were also determined for [H-3]RS79948-197 for the guinea pig spleen alpha(2A)-adrenoceptor and for pig alpha(2A)-, alpha(2B)- and alpha(2C)-adrenoceptors in membranes obtained from kidney and striatum. Available radioligands for a,-adrenoceptors, besides [H-3]RS79948-197 are the tritiated forms of MK912 [b]furo[2,3-a]quinazoline)-2,4'-pyrimidin-2'-one), RX821002 (2-methoxy-idazoxan), rauwolscine and yohimbine. In the present article the binding constants of all these substances for the alpha(2A)-, alpha(2B)- and alpha(2C)-adrenoceptor subtypes in human, pig, rat and guinea pig an reviewed. In all species tested MK912 was alpha(2C)-selective, RX821002 showed a minor alpha(2A)-selectivity, whereas [H-3]RS79948-197 was non-selective among the alpha(2)-adrenoceptor subtypes, showing high affinity for all three subtypes. Rauwolscine and yohimbine showed relatively low affinities for most of the alpha(2)-adrenoceptor subtypes investigated, the exception being rauwolscine havinghigh affinity for the human and porcine alpha(2C)-adrenoceptors. (C) 1998 Elsevier Science B.V.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 11/07/20 alle ore 21:06:30