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新型β-肾上腺素能阻滞剂OPC-1427对大鼠的降压作用

Hypotensive action of OPC-1427, a new beta-adrenergic blocking agent in rats.

作者信息

Sugawara K, Takami N, Ozaki M

出版信息

Arch Int Pharmacodyn Ther. 1979 Aug;240(2):294-304.

PMID:41497
Abstract

8-Acetonyloxy-5-[3-(2-(3,4-dimethoxyphenyl)-ethylamino)-2-hydroxypropoxyl]-3,4-dihydrocarbostyril (OPC-1427), is a newly synthesized cardioselective beta-adrenoceptor blocking agent and we examined the effects of this compound given intraperitoneally to consious Kyoto Wistar normotensive (WKR), spontaneous hypertensive (SHR) and DOCA-NCl hypertensive (DOCA rat) rats. The results were compared to findings with propranolol and practolol. OPC-1427 produced a significant hypotensive action in SHR and DOCA rats and this effect was less in WKR. With propranolol and practolol effective hypotensive effects were seen in WKR and DOCA rats but not in the SHR. The efficacy of the hypotensive action of these agents was propranolol greater than OPC-1427 = practolol in WKR, OPC-1427 greater than practolol in SHR, and OPC-1427 greater than practolol = propranolol in DOCA rats. Thus OPC-1427 appears to be a promising beta-adrenoceptor blocking agent which exerts a hypotensive state, as demonstrated in hypertensive rats.

摘要

8-丙酮氧基-5-[3-(2-(3,4-二甲氧基苯基)-乙氨基)-2-羟基丙氧基]-3,4-二氢咔唑醇(OPC-1427)是一种新合成的心脏选择性β-肾上腺素受体阻滞剂,我们研究了腹腔注射该化合物对清醒的京都Wistar正常血压大鼠(WKR)、自发性高血压大鼠(SHR)和去氧皮质酮-盐性高血压大鼠(DOCA大鼠)的影响。将结果与普萘洛尔和普拉洛尔的研究结果进行比较。OPC-1427对SHR和DOCA大鼠产生显著的降压作用,而对WKR的作用较小。普萘洛尔和普拉洛尔对WKR和DOCA大鼠有有效的降压作用,但对SHR无效。这些药物降压作用的疗效在WKR中为普萘洛尔大于OPC-1427 =普拉洛尔,在SHR中为OPC-1427大于普拉洛尔,在DOCA大鼠中为OPC-1427大于普拉洛尔 =普萘洛尔。因此,OPC-1427似乎是一种有前景的β-肾上腺素受体阻滞剂,如在高血压大鼠中所示,它能产生降压状态。

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