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Titolo:
CHARACTERIZATION OF THE SPECIFIC BINDING OF THE HISTAMINE H-3 RECEPTOR ANTAGONIST RADIOLIGAND [H-3] GR168320
Autore:
BROWN JD; OSHAUGHNESSY CT; KILPATRICK GJ; SCOPES DIC; BESWICK P; CLITHEROW JW; BARNES JC;
Indirizzi:
GLAXO WELLCOME RES & DEV LTD,DEPT PHARMACOL STEVENAGE SG1 2NY HERTS ENGLAND GLAXO WELLCOME RES & DEV LTD,DEPT MED CHEM STEVENAGE SG1 2NY HERTS ENGLAND
Titolo Testata:
European journal of pharmacology
fascicolo: 2-3, volume: 311, anno: 1996,
pagine: 305 - 310
SICI:
0014-2999(1996)311:2-3<305:COTSBO>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
I-125 IODOPHENPROPIT; RAT-BRAIN; RELEASE; CORTEX; INHIBITION; SUBTYPES; LIGANDS; POTENT;
Keywords:
HISTAMINE H-3 RECEPTOR; RADIOLIGAND BINDING; [H-3] GR168320; CEREBRAL CORTEX, RAT; [H-3] N-ALPHA-METHYLHISTAMINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
21
Recensione:
Indirizzi per estratti:
Citazione:
J.D. Brown et al., "CHARACTERIZATION OF THE SPECIFIC BINDING OF THE HISTAMINE H-3 RECEPTOR ANTAGONIST RADIOLIGAND [H-3] GR168320", European journal of pharmacology, 311(2-3), 1996, pp. 305-310

Abstract

We have examined the specific binding of the tritiated derivative of the potent histamine H-3 receptor antagonist, H-imidazol-4-yl)-piperidin-1-yl]iminomethyl}-amine ([H-3]GR168320), to homogenates of rat cerebral cortex. Specific binding of [H-3]GR168320 at 37 degrees C associated and dissociated rapidly. Binding was saturable( B-max 412 +/- 89 fmol/mg protein) and of high affinity (K-d 0.12 +/- 0.11 nM). Saturation studies suggested the involvement of a single site. Histamine H-3 receptor agonists and antagonists inhibited [H-3]GR168320 binding with high affinity. Agonist and antagonist affinities correlated when compared with affinities obtained using the tritiated histamine H-3 agonist radioligand N-alpha-methylhistamine.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/11/20 alle ore 02:27:34