Antihypertensive profile of cicletanine, a furopyridine derivative: comparison with captopril, indapamide and prazosin.
The effects of cicletanine were compared with those of three other antihypertensive drugs: prazosin, a highly selective alpha 1 antagonist, captopril an angiotensin converting enzyme inhibitor and indapamide a diuretic antihypertensive agent, on young stroke-prone SHR rats with high salt diet; furthermore, vascular reactivity to cicletanine was studied on isolated rat aorta. At an equal dose (30 mg/kg per os) all the drugs prevent the onset of hypertension with the same intensity. The minimal effective dose on blood pressure was 1 mg/kg for both cicletanine and captopril, and 3 mg/kg for indapamide. The action on diuresis and electrolyte excretion occurs at a dose of cicletanine 10 to 30 times higher than that required to produce the anti-hypertensive effect. One of the possible mechanisms of the antihypertensive effects of cicletanine could be due to a direct action of the drug on the vascular wall. This vascular impact could be an interaction with the alpha-adrenoceptor system (apparent pA2 cicletanine = 5.12) or a decrease in the vascular spasmogenic response whatever agonist was studied.
Malherbe
E
E
I.H.B. Research Labs, Les Ulis, France.
Auguet
M
M
Delaflotte
S
S
Le Hégarat
M
M
Baranes
J
J
Clostre
F
F
Braquet
P
P
D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology*; D001011:Aorta / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects*; D002216:Captopril / Q000494:pharmacology; D006332:Cardiomegaly / Q000517:prevention & control; D004231:Diuresis / Q000187:drug effects; D004232:Diuretics / Q000494:pharmacology*; D006973:Hypertension / Q000517:prevention & control; D066298:In Vitro Techniques; D007190:Indapamide / Q000494:pharmacology; D008297:Male; D011224:Prazosin / Q000494:pharmacology; D011725:Pyridines; D051381:Rats; D011918:Rats, Inbred SHR; D011919:Rats, Inbred Strains; D014661:Vasoconstriction / Q000187:drug effects
D000959:Antihypertensive Agents; D004232:Diuretics; D011725:Pyridines; D002216:Captopril; C038068:cicletanine; D007190:Indapamide; D011224:Prazosin