PMID- 4054822 OWN - NLM STAT- MEDLINE DCOM- 19851210 LR - 20131121 IS - 0367-6102 (Print) IS - 0367-6102 (Linking) VI - 60 IP - 4 DP - 1985 Jul TI - [Effects of new antihypertensive agent, 2-[4-(n-butyryl)-homopiperazine-1-ul]-4-amino-6, 7-dimethoxy-quinazoline (E-643), on blood pressure, urinary sodium excretion and urinary norepinephrine excretion rate in stroke-prone, spontaneously hypertensive rats]. PG - 536-43 AB - Present study was undertaken to elucidate the effects of E-643, on blood pressure, urinary electrolyte (U-Na, U-K) and catecholamines excretion rates in stroke-prone spontaneously hypertensive rats (SHRSP). An attempt was also made to clarify the effects of E-643 on plasma catecholamine concentration and sympathetic efferent nerve discharges including renal and adrenal nerve activity. E-643 (10 mg/kg/day X 4 weeks, p.o.) administered SHRSP (E-643 SHRSP) produced a significant hypotensive effect as compared with sex-age matched nondrug control SHRSP (control SHRSP). Both U-Na and U-K in E-643 SHRSP increased significantly as compared with those of control SHRSP. Urinary norepinephrine content (U-NE) also increased significantly in E-643 SHRSP. Plasma NE concentration tended to increase in E-643 SHRSP. While, plasma epinephrine (E) concentration decreased significantly in E-643 SHRSP. E-643 did not produce any significant effects on both sympathetic renal nerve activity and adrenal nerve activity in SHR. The changes induced by exogenous administered NE (blood pressure rise, tachycardia and the change in sympathetic nerve activity) were antagonized by pretreatment of E-643 in SHR. It was demonstrated that therapeutic doses of E-643 did not seem to produce any significant effect on central nervous system. These findings suggest that E-643 is a peripherally acting alpha 1 antagonist with natriuretic effect. FAU - Minami, M AU - Minami M FAU - Togashi, H AU - Togashi H FAU - Sano, M AU - Sano M FAU - Yoshioka, M AU - Yoshioka M FAU - Saito, I AU - Saito I FAU - Morii, K AU - Morii K FAU - Tochihara, M AU - Tochihara M FAU - Hirogami, M AU - Hirogami M FAU - Nomura, A AU - Nomura A FAU - Saito, H AU - Saito H LA - jpn PT - English Abstract PT - Journal Article PL - Japan TA - Hokkaido Igaku Zasshi JT - [Hokkaido igaku zasshi] The Hokkaido journal of medical science JID - 17410290R RN - 0 (Antihypertensive Agents) RN - 0 (Catecholamines) RN - 0 (Quinazolines) RN - 9UUW4V7G2H (bunazosin) RN - RWP5GA015D (Potassium) RN - X4W3ENH1CV (Norepinephrine) SB - IM MH - Animals MH - Antihypertensive Agents/*pharmacology MH - Blood Pressure/*drug effects MH - Body Weight/drug effects MH - Catecholamines/blood MH - Cerebrovascular Disorders/etiology MH - Eating/drug effects MH - Heart Rate/drug effects MH - Humans MH - Hypertension/metabolism/*physiopathology MH - Kidney/innervation MH - Male MH - Natriuresis/*drug effects MH - Norepinephrine/*urine MH - Potassium/urine MH - Quinazolines/*pharmacology MH - Rats MH - Rats, Inbred SHR EDAT- 1985/07/01 00:00 MHDA- 1985/07/01 00:01 CRDT- 1985/07/01 00:00 PHST- 1985/07/01 00:00 [pubmed] PHST- 1985/07/01 00:01 [medline] PHST- 1985/07/01 00:00 [entrez] PST - ppublish SO - Hokkaido Igaku Zasshi. 1985 Jul;60(4):536-43.