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

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.

• Authors: D Wellens, L Snoeckx, R De Reese, R Kruger, A Van de Water, L Woutens, R S Reneman
• Journal: Archives internationales de pharmacodynamie et de therapie (Arch Int Pharmacodyn Ther) Vol. 215 Issue 1 Pg. 119-32 (May 1975) ISSN: 0003-9780 [Print] Belgium
• PMID: 1156041 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Antihypertensive Agents
• Benzimidazoles
• Propranolol
• Clonidine

Topics

• Animals
• Antihypertensive Agents (pharmacology, therapeutic use)
• Benzimidazoles (pharmacology, therapeutic use)
• Blood Pressure (drug effects)
• Cardiac Output (drug effects)
• Clonidine (pharmacology, therapeutic use)
• Dogs
• Female
• Heart Rate (drug effects)
• Hypertension (drug therapy)
• Hypertension, Renal (drug therapy)
• Male
• Propranolol (pharmacology, therapeutic use)
• Rats
• Rats, Inbred Strains
• Time Factors
• Vascular Resistance (drug effects)