On the pharmacological actions of a diuretic, fenquizone, with particular reference to its site of action

Abstract

The pharmacological actions of a diuretic drug, fenquizone have been investigated and its effects compared with well characterized diuretics in rats, mice and rabbits. Changes in sodium and potassium excretion and urine volume were similar in magnitude and duration to those of the thiazide diuretics over dose range 0.05-100 mg kg-'. Free water clearance in rabbits wasdecreased indicatingan action at thecortical dilutingsite in the nephron and since free water reabsorption was relatively unaffected it appears unlikely to have actions at other sites. Calcium and phosphate excretion studies also suggested that the predominant effects arethose occurring at the cortical diluting segment of the nephron. Additional parametersnot affected by the drug were blood flow to the cortex and medulla of the kidney (and other major organs), plasma glucose concentration and plasma urate concentration.

Effect of bumetanide, frusemide and prostaglandin E2 on the isolated perfused kidney of rat and rabbit

“…In this study, within the limits of the parameters employed, a direct comparison is possible between rat and rabbit isolated perfused kidney and any possible haemodynamic (as opposed to diuretic) action of two ostensibly similar loop diuretics. The concentrations of diuretics, PGE2 and flurbiprofen chosen were those either shown, in previous studies, to be effective as diuretics or used in previous kidney perfusion studies (Malik & McGiff, 1975;Ferrando et al, 1981). There can now be little doubt that prostaglandins play an important role in the kidney, the significance of which probably varies between species.…”

“…The concentrations of diuretics, PGE2 and flurbiprofen chosen were those either shown, in previous studies, to be effective as diuretics or used in previous kidney perfusion studies (Malik & McGiff, 1975;Ferrando et al, 1981). There can now be little doubt that prostaglandins play an important role in the kidney, the significance of which probably varies between species.…”

Palladium‐Catalyzed Carbonylative Difunctionalization of C=N Bond of Azaarenes or Imines to Quinazolinones

“…[2] For example, rutaecarpine, euxylophoricine B, and evodiamine are all effective ingredients of Chinese herbal medicines. [3][4] Additionally, fenquizone [5] and raltitrexed [6] containing this core structure have been on the market or are in clinical trials for the treatment of edema, diuretic, and cancer ( Figure 1).…”

2,3-Dihydroquinazolin-4(1H)-one as a privileged scaffold in drug design

“…282 Among them, fenquizone is a FDA-approved drug for the treatment of edema and hypertension. [283][284][285][286] The substitution of C8 with N in the benzene ring of DHQ and the introduction of 287 Some DHQ derivatives also show broad-spectrum antimicrobial properties. 2-(5-Nitro-2-thienyl) DHQs showed antibacterial activity against Hemophilus vaginalis and Escherichia coli strains, responsible for bacterial vaginitis, exhibiting low minimal inhibitory concentration (MIC, ranging from 0.4 to 12.5 mg ml À1 ).…”