An antagonistic activity of etizolam on platelet-activating factor(PAF). In vitro effects on platelet aggregation and PAF receptor binding.
スポンサーリンク
概要
- 論文の詳細を見る
The antagonistic effect of etizolam, an anti-anxiety drug, on platelet-activating factor (PAF) was investigated in rabbit platelets in vitro. Etizolam inhibited PAF-induced aggregation in a dose-dependent manner, with an IC50 of 3.8 μM, about one tenth that of triazolam (IC50=30 μM). At 300 μM, it inhibited both ADP and arachidonic acid-induced aggregation only slightly, while the other anti-anxiety drugs tested had no effect on PAF-induced aggregation even at this concentration. Etizolam and triazolam inhibited the specific binding of <SUP>3</SUP>H-PAF to PAF receptor sites on washed rabbit platelets with IC50 values of 22 nM and 320 nM, respectively. Diazepam and estazolam were inactive even at 1 μM. These results indicate that etizolam is a specific antagonist of PAF.
- 公益社団法人 日本薬理学会の論文
著者
-
Maruyama Yutaka
Research Laboratories Yoshitomi Pharmacoceutical Industries Ltd.
-
Takehara Shuzo
Research Laboratories Yoshitomi Pharmacoceutical Industries Ltd.
-
Terasawa Michio
Research Laboratories Yoshitomi Pharmaceutical Industries Ltd
-
MURAMOTO Yoshito
Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.
-
MIKASHIMA Hiroshi
Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.
-
KHOMARU Takako
Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.
-
TAHARA Tetsuya
Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd.
関連論文
- EFFECT OF SUFOXAZINE (Y-8894) ON LEARNING AND MEMORY IN ANIMALS
- Suppressive Effects of Y-24180, a Long-Acting Antagonist for Platelet-Activating Factor, on Allergic Pulmonary Eosinophilia in Mice
- IMMUNOPHARMACOLOGICAL PROPERTIES OF NEW ANTIALLERGIC AGENT Y-12,141
- Effect of Y-24180, a Platelet-Activating Factor-Receptor Antagonist, on the Antigen-Induced Airway Microvascular Leakage in Guinea Pigs
- EFFECTS OF 2-{4-(2-IMIDAZO[1, 2-a]PYRIDYL)PHENYL} PROPIONIC ACID (Y-9213) AND ANTI-INFLAMMATORY DRUGS ON ERYTHROCYTES, POLYMORPHONUCLEAR LEUKOCYTES AND LYSOSOMES IN VITRO
- ANTI-ANAPHYLACTIC ACTIVITIES OF A NEW BENZOPYRANOPYRIDINE DERIVATIVE Y-12, 141 IN RATS AND GUINEA PIGS
- TRAXANOX AUGMENTS IMMUNE RESPONSE TO LIPOPOLYSACCHARIDE IN INBRED MICE: ROLE OF MACROPHAGES
- Stimulation of phagocytic activity of leukocytes and macrophages by traxanox sodium in mice and rats.
- Effect of cysteine ethylester hydrochloride (CystaninR) on host defense mechanisms. (IV). Potentiating effects on the function of peritoneal or spleen macrophages.
- An antagonistic activity of etizolam on platelet-activating factor(PAF). In vitro effects on platelet aggregation and PAF receptor binding.
- Antagonistic Activity of Y-25130 on 5-HT3 Receptors.
- Effect of etizolam (Depas) on production of superoxide anion by platelet-activating factor and N-formyl-methionyl-leucyl-phenylalanine-stimulated guinea pig polymorphonuclear leukocytes.
- Effect of cysteine ethylester hydrochloride (Cystanin) on host defense mechanisms (V): Potentiation of nitroblue tetrazolium reduction and chemiluminescence in macrophages or leukocytes of mice or rats.