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Titolo:
ANTIPLATETLET EFFECTS OF ISOCARBACYCLIN METHYL-ESTER ON HUMAN AND RABBIT PLATELETS IN-VITRO
Autore:
INOUE K; AOKI Y; KITAHARA S; KIYOKI M; ARAKI H;
Indirizzi:
TEIJIN LTD,TEIJIN INST BIOMED RES,PHARMACEUT DEV RES LABS,PHARMACOL RES DEPT,4-3-2 ASAHIGAOKA HINO TOKYO 191 JAPAN TAISHO PHARMACEUT CO LTD,RES CTR,DEPT PHARMACOL 2 OMIYA SAITAMA JAPAN
Titolo Testata:
Arzneimittel-Forschung
fascicolo: 9, volume: 45-2, anno: 1995,
pagine: 975 - 979
SICI:
0004-4172(1995)45-2:9<975:AEOIMO>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
STABLE PROSTACYCLIN ANALOG; PROSTAGLANDIN-I2 ANALOG; EXPERIMENTAL-ANIMALS; AGGREGATION; ADHESION; COLLAGEN; INHIBITION; STABILITY; ARTERIES; OP-41483;
Keywords:
CAS 88911-35-7; CAS 88931-51-5; IOCARBACYCLIN ETHYL ESTER, FREE ACID, IN LIPID MICROSPHERES; PLATELET AGGREGATION; TEI-7165, PHARMACOLOGY; TEI-9090, PHARMACOLOGY; TTC-909, PHARMACOLOGY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
30
Recensione:
Indirizzi per estratti:
Citazione:
K. Inoue et al., "ANTIPLATETLET EFFECTS OF ISOCARBACYCLIN METHYL-ESTER ON HUMAN AND RABBIT PLATELETS IN-VITRO", Arzneimittel-Forschung, 45-2(9), 1995, pp. 975-979

Abstract

Anti-platelet effects of isocarbacyclin methyl ester (CAS 88931-51-5,TEI-9090) and of its free acid form, TEI-7165 (CAS 88911-35-7) were compared with those of prostaglandin (PG) I-2 and PGE(1). TEI-9090 and TEI-7165 dose-dependently inhibited human and rabbit platelet aggregation and human platelet adhesion in vitro. The IC50 values of TEI-9090,TEI-7165, PGI(2), and PGE(1) against ADP-induced human (rabbit) platelet aggregation were 22.90 (25.00) ng/ml, 2.78 (6.46) ng/ml, 1.67 (3.34) ng/ml, and 19.91 (8.32) ng/ml, respectively, and those against human platelet adhesion were 3.47 ng/ml, 0.13 ng/ml, 0.25 ng/ml, and 1.45 ng/ml, respectively. TTC-909, a product incorporating TEI-9090 in lipid microspheres, had an aggregation inhibitory effect similar to that of TEI-9090 in human platelets. The aggregation inhibitory effect of TEI-9090 and TTC-909 increased with incubation time, and reached a levelsimilar to that of TEI-7165. In contrast, the aggregation inhibitory effect of TEI-7165 remained constant for 120 min, whereas that of PGI(2) decreased with time. TEI-9090 and TEI-7165 also enhanced the disaggregation of human platelets at nearly the same concentration as they exerted their inhibitory effect on aggregation. The order of anti-platelet activities, compared at each optimum incubation point, were PGI(2)congruent to TEI-7165 congruent to TEI-9090 (congruent to TTC-909) > PGE(1) in human and rabbit platelets. These results indicate that TEI-9090 (TTC-909) and its active metabolite TEI-7165, may be a potent anti-platelet drug.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 26/09/20 alle ore 11:47:55