交感神経β-受容体遮断作用を有する新しいIndene誘導体の薬理作用
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1) The β-blocking and direct effect on heart rate of six newly synthesized indene derivatives was studied in reserpinized rats and compared with that of propranolol (PROP), alprenolol(ALP), USVC 6524(USVC), practolol(PRACT)and YB-2. The order of potency of 1-(7-indenyloxy)-3-alkylaminopropan-2-ol derivatives(I-IV) antagonizing isoproterenol-induced tachycardia was III (tert. butyl)>YB-2 (isopropyl)>II (sec butyl)>I(isobutyl)>IV (cyclohexyl). Especially, III and YB-2 were 2.5 and 1.5 times more potent than PROP, respectively. The activity of 1-(3-methyl-7-indenyloxy)-3-isopropylaminopropan-2-ol(V)and 1-(3-methyl-4-chlor-7-indenyloxy)-3-isopropylaminopropan-2-ol(VI) was much weaker than that of YB-2. 2) In the same preparations, I-IV, VI, YB-2,and ALP showed a moderate intrinsic sympathomimetic activity (ISA), while the compound (V) exhibited a marked ISA comparable to that of PRACT 3) YB-2 and ALP in concentration of 5×10^<-8>g/ml depressed the motility of the isolated rat uterus, while PROP and USVC were devoid of such inhibitory effect, indicating a lack of ISA in these corn : unds. 4) All indene derivatives, in concentration of 1% or less showed a local inesthetic action in the guinea pig cornea. 5) Comparison of the K_B values in the left atrium and trachea isolated from guinea pigs indicated that III and ALP possessed a greater affinity for the tracheal smooth muscle than for the atrium, whereas YB-2 and PROP blocked β-receptors in both organs to the same degree.
- 公益社団法人日本薬学会の論文
- 1973-12-25
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