[Effects of 4-(o-benzylphenoxy)-N-methylbutylamine hydrochloride (MCI-2016, bifemelane hydrochloride) on coagulation, fibrinolysis, hemolysis, hemorheological properties and platelet aggregation].
MCI-2016 showed little influence on coagulation (APTT) and fibrinolysis (plasma clot lysis activated by urokinase) at doses (concentrations) as high as 300 mg/kg, p.o. or 8.6 X 10(-4) M. Hemolytic action of MCI-2016 was only observed at the concentrations above 2 mM. The drug also showed no influence on blood glucose level (30-300 mg/kg, p.o.). Effects of MCI-2016 on hemorheological properties were studied either in vitro or ex vivo. Above the doses (concentrations) of 100 mg/kg, p.o. and 10 microM, MCI-2016 suppressed the mechanical hemolysis and accelerated the membrane filtration rate. These effects of MCI-2016 were superior to those of cinepazide, Ca-hopantenate, meclofenoxate and pentoxyfylline. MCI-2016 also inhibited platelet aggregation induced by collagen with the IC 50 of 35 to 60 microM (rabbit and human platelets). Secondary aggregations of ADP and epinephrine were also inhibited by MCI-2016. As for reference drugs, bencyclane showed inhibitory patterns similar to MCI-2016. Other drugs examined exhibited little effect. In summary, it may be suggested that MCI-2016 exhibits beneficial influences in the clinical fields of cerebrovascular diseases.
Tamao
Y
Y
Hara
H
H
Umezu
K
K
Ito
J
J
Doi
A
A
Sudo
A
A
Hirata
T
T
Mineo
K
K
Tobe
A
A
D000818:Animals; D001559:Benzhydryl Compounds / Q000494:pharmacology*; D001769:Blood / Q000187:drug effects*; D001777:Blood Coagulation / Q000187:drug effects; D001786:Blood Glucose / Q000032:analysis; D001809:Blood Viscosity / Q000187:drug effects; D004912:Erythrocytes / Q000187:drug effects; D005342:Fibrinolysis / Q000187:drug effects; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012212:Rheology
D001559:Benzhydryl Compounds; D001786:Blood Glucose; C031906:bifemelane