Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
HISTAMINE H-1 RECEPTOR OCCUPANCY IN HUMAN BRAINS AFTER SINGLE ORAL DOSES OF HISTAMINE H-1 ANTAGONISTS MEASURED BY POSITRON EMISSION TOMOGRAPHY
Autore:
YANAI K; RYU JH; WATANABE T; IWATA R; IDO T; SAWAI Y; ITO K; ITOH M;
Indirizzi:
TOHOKU UNIV,SCH MED,DEPT PHARMACOL 1,AOBA KU,2-1 SEIRYO MACHI SENDAI MIYAGI 98077 JAPAN TOHOKU UNIV,CTR CYCLOTRON & RADIOISOTOPE SENDAI MIYAGI 98077 JAPAN MARION MERRELL DOW INC,HIRAKATA CTR,DEV LABS HIRAKATA OSAKA 573 JAPAN
Titolo Testata:
British Journal of Pharmacology
fascicolo: 1, volume: 116, anno: 1995,
pagine: 1649 - 1655
SICI:
0007-1188(1995)116:1<1649:HHROIH>2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG BRAIN; H1 RECEPTORS; GABAERGIC TRANSMISSION; BINDING; INVIVO; PET; TERFENADINE; ANTIHISTAMINES; H-1-RECEPTORS; H1-RECEPTORS;
Keywords:
ANTIHISTAMINES; H-1 RECEPTOR ANTAGONISTS; CHLORPHENIRAMINE; BRAIN; TERFENADINE; SEDATION IN MAN; POSITRON EMISSION TOMOGRAPHY; RECEPTOR OCCUPANCY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
39
Recensione:
Indirizzi per estratti:
Citazione:
K. Yanai et al., "HISTAMINE H-1 RECEPTOR OCCUPANCY IN HUMAN BRAINS AFTER SINGLE ORAL DOSES OF HISTAMINE H-1 ANTAGONISTS MEASURED BY POSITRON EMISSION TOMOGRAPHY", British Journal of Pharmacology, 116(1), 1995, pp. 1649-1655

Abstract

1 Histamine H-1 receptor occupancy in the human brain was measured in20 healthy young men by positron emission tomography (PET) using [C-11]-doxepin. 2 (+)-Chlorpheniramine, a selective and classical antihistamine, occupied 76.8 +/- 4.2% of the averaged values of available histamine H-1 receptors in the frontal cortex after its administration in a single oral dose of 2 mg. Intravenous administration of 5 mg (+)-chlorpheniramine almost completely abolished the binding of [C-11]-doxepin to H-1 receptors (H-1 receptor occupancy: 98.2 +/- 1.2%). 3 Terfenadine, a ponsedative antihistamine, occupied 17.2 +/- 14.2% of the available H, receptors in the human frontal cortex after its administrationin a single oral dose of 60 mg. 4 There was no correlation between H-1 receptor occupancy by terfenadine and the plasma concentration of the active acid metabolite of terfenadine in each subject. 5 PET data onhuman brain were essentially compatible with those on H-1 receptor occupancy in guinea-pig brain determined by in vivo binding techniques, although for the same H-1 receptor occupancy the dose was less in human subjects than in guinea-pigs. 6 The PET studies demonstrated the usefulness of measuring H-1 receptor occupancy with classical and second-generation antihistamines in human brain to estimate their unwanted side effects such as sedation and drowsiness quantitatively.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/04/20 alle ore 10:24:45