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赤式-1-(1-[2-(1,4-苯并二噁烷-2-基)-2-羟基乙基]-4-哌啶基)-2-苯并咪唑啉酮(R 28935)的降压活性

Antihypertensive activity of erythro-1-(1-[2-(1,4-benzodioxan-2-yl)-2-OH-ET]-4-piperidyl)-2-benzimidazolinone (R 28935).

作者信息

Wellens D, Snoeckx L, De Reese R, Kruger R, Van de Water A, Woutens L, Reneman R S

出版信息

Arch Int Pharmacodyn Ther. 1975 May;215(1):119-32.

PMID:1156041
Abstract

Erythro-1-(1-[2-(1,4-benzodioxan-2-yl)-2-OH-ET]-4-piperidyl)-2-benzimidazolinone (R 28935), provokes marked antihypertensive effects lasting several hours in conscious SHR (0.63 to 40 mg/kg i.p.) and beagles with renal hypertension (1.25 mg/kg p.o.). In SHR, this compound induces much less bradycardia, compared to equiactive hypotensive doses of clonidine, guanethidine and propranolol. Significant postural hypotension during tilting, is induced by guanethidine and mecamylamine but not by R 28935. In anaesthetized beagles with renal hypertension, the lowering of the blood pressure by R 28935, (0.02-0.64 mg/kg i.v.) is associated with a considerable decrease in the total peripheral vascular resistance, whereas the myocardial function is not affected. R 28935 is considered a potent antihypertensive drug, with attractive haemodynamic characteristics.

摘要

1-(1-[2-(1,4-苯并二恶烷-2-基)-2-羟基乙基]-4-哌啶基)-2-苯并咪唑啉酮(R 28935),在清醒的自发性高血压大鼠(腹腔注射0.63至40毫克/千克)和肾性高血压比格犬(口服1.25毫克/千克)中可引发显著的降压作用,持续数小时。在自发性高血压大鼠中,与等效降压剂量的可乐定、胍乙啶和普萘洛尔相比,该化合物引起的心动过缓要少得多。胍乙啶和美加明可引起倾斜过程中的显著体位性低血压,但R 28935不会。在麻醉的肾性高血压比格犬中,R 28935(静脉注射0.02 - 0.64毫克/千克)降低血压与总外周血管阻力的显著降低有关,而心肌功能不受影响。R 28935被认为是一种有效的降压药物,具有吸引人的血流动力学特性。

相似文献

1
Antihypertensive activity of erythro-1-(1-[2-(1,4-benzodioxan-2-yl)-2-OH-ET]-4-piperidyl)-2-benzimidazolinone (R 28935).赤式-1-(1-[2-(1,4-苯并二噁烷-2-基)-2-羟基乙基]-4-哌啶基)-2-苯并咪唑啉酮(R 28935)的降压活性
Arch Int Pharmacodyn Ther. 1975 May;215(1):119-32.
2
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A benzodioxanhydroxyethylpiperidine derivative with an acute central hypotensive action, different from that of clonidine. A comparison with neuroleptic agents.一种具有急性中枢性降压作用的苯并二氧六环羟乙基哌啶衍生物,与可乐定的作用不同。与抗精神病药物的比较。
Arch Int Pharmacodyn Ther. 1975 May;215(1):104-18.
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引用本文的文献

1
The regional localization of R28935 in the cat brain as dependent on the route of administration.取决于给药途径的R28935在猫脑中的区域定位。
Naunyn Schmiedebergs Arch Pharmacol. 1979 Nov;309(3):281-5. doi: 10.1007/BF00504761.
2
R 28935 and prazosin: effects on central and peripheral alpha-adrenoreceptor activity and on blood pressure.
Naunyn Schmiedebergs Arch Pharmacol. 1978 May;302(3):299-306. doi: 10.1007/BF00508299.