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Titolo:
INTRACEREBRAL PENETRATION OF CARTEOLOL HYDROCHLORIDE IN RATS
Autore:
KUDO S; UMEHARA K; ABE Y; FURUKAWA M; ODOMI M;
Indirizzi:
OTSUKA PHARMACEUT CO LTD,TOKUSHIMA RES INST,463-10 KAGASUNO,KAWAUCHI CHO TOKUSHIMA 77101 JAPAN
Titolo Testata:
Psychopharmacology
fascicolo: 4, volume: 131, anno: 1997,
pagine: 388 - 393
Fonte:
ISI
Lingua:
ENG
Soggetto:
NEUROLEPTIC-INDUCED AKATHISIA; PROPRANOLOL; PINDOLOL; ATENOLOL;
Keywords:
CARTEOLOL HYDROCHLORIDE; BETA-BLOCKER; PENETRABILITY; BRAIN; RAT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
28
Recensione:
Indirizzi per estratti:
Citazione:
S. Kudo et al., "INTRACEREBRAL PENETRATION OF CARTEOLOL HYDROCHLORIDE IN RATS", Psychopharmacology, 131(4), 1997, pp. 388-393

Abstract

To elucidate the penetrability of carteolol, a beta-adrenoceptor antagonist (beta-blocker) into the brain of rats, intracerebral and serum concentrations of the compound were determined in male rats receiving single or repetitive oral administration of carteolol hydrochloride at30 mg/kg. The time-course of the intracerebral concentration of carteolol following single IV administration of the compound at 10 and 38 mg/kg was also studied in male rats. A high-performance liquid chromatography method was used to determine the intracerebral and serum concentrations. Following single oral dosing, the intracerebral concentration of carteolol reached a maximum of 0.074 mu g/g at 2 h postdosing anddeclined with a half-life of 3.7 h, and the C-max and AUC of carteolol in the brain were 12.5% and 19.8% of those in serum. The intracerebral and serum concentrations of carteolol were determined in male rats receiving repetitive oral dosing of the compound once daily for 7 days. The concentration of carteolol in the brain and serum at 1 h postdosing varied within a range of 0.059-0.091 mu g/g and 0.321-0.443 mu g/ml, respectively, throughout the dosing period. showing no changes in the penetrability of the compound into the brain due to repeated dosing. The concentration of carteolol in the brain and serum increased in adose-dependent manner in rats receiving a single IV administration ofthe compound. The elimination half-life of carteolol in the serum andbrain was 0.06-0.8 h and 1.3-1.7 h, respectively, in rats following single IV dosing of the compound. The half-life in the brain was about twice as long as that in the serum. The brain to serum concentration ratio was 0.306:0.499. From the above results, it was concluded that carteolol is distributed from the circulation to the brain with low penetrability.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 15:37:24