Biomaterial Database

Alpha-adrenoceptor antagonistic effects and antihypertensive activity of SGB-1534 in conscious normotensive and deoxycorticosterone acetate (DOCA)-salt hypertensive dogs: comparison with prazosin. 1989

K Haruta, and A Baba, and M Akima, and T Koga, and Y Shiraki, and K Sakai

Department of Pharmacology, Fujigotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd., Shizuoka, Japan.

In conscious normotensive and deoxycorticosterone acetate (DOCA)-salt hypertensive dogs, alpha-adrenoceptor antagonistic and antihypertensive actions of SGB-1534, given orally, were compared with those of prazosin. SGB-1534 and prazosin did not markedly influence systemic blood pressure (SBP) and heart rate (HR) in normotensive dogs. These alpha 1-adrenoceptor antagonists inhibited SBP and HR increases induced by i.v. adrenaline in a dose-dependent manner. In DOCA-salt hypertensive dogs, persistent hypotension, accompanied by a reflex tachycardia, occurred after oral administration of SGB-1534 and prazosin. The hypotensive activity of SGB-1534 was much more potent in magnitude and duration than that of prazosin. In isolated canine mesenteric and femoral arteries, SGB-1534, compared to prazosin, elicited a more potent inhibition on the contractile response to a relatively selective alpha 1-adrenoceptor agonist, phenylephrine. It appears that the antihypertensive activity of SGB-1534, like prazosin, is nearly in parallel with its alpha 1-adrenoceptor antagonistic effect.

UI	MeSH Term	Description	Entries
D006973	Hypertension	Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.	Blood Pressure, High,Blood Pressures, High,High Blood Pressure,High Blood Pressures
D008297	Male		Males
D008638	Mesenteric Arteries	Arteries which arise from the abdominal aorta and distribute to most of the intestines.	Arteries, Mesenteric,Artery, Mesenteric,Mesenteric Artery
D009119	Muscle Contraction	A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	Inotropism,Muscular Contraction,Contraction, Muscle,Contraction, Muscular,Contractions, Muscle,Contractions, Muscular,Inotropisms,Muscle Contractions,Muscular Contractions
D009131	Muscle, Smooth, Vascular	The nonstriated involuntary muscle tissue of blood vessels.	Vascular Smooth Muscle,Muscle, Vascular Smooth,Muscles, Vascular Smooth,Smooth Muscle, Vascular,Smooth Muscles, Vascular,Vascular Smooth Muscles
D010656	Phenylephrine	An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.	(R)-3-Hydroxy-alpha-((methylamino)methyl)benzenemethanol,Metaoxedrin,Metasympatol,Mezaton,Neo-Synephrine,Neosynephrine,Phenylephrine Hydrochloride,Phenylephrine Tannate,Neo Synephrine,Tannate, Phenylephrine
D011224	Prazosin	A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.	Furazosin,Minipress,Pratsiol,Prazosin HCL,Prazosin Hydrochloride,HCL, Prazosin,Hydrochloride, Prazosin
D011799	Quinazolines	A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.	Quinazoline
D001794	Blood Pressure	PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.	Systolic Pressure,Diastolic Pressure,Pulse Pressure,Pressure, Blood,Pressure, Diastolic,Pressure, Pulse,Pressure, Systolic,Pressures, Systolic
D003900	Desoxycorticosterone	A steroid metabolite that is the 11-deoxy derivative of CORTICOSTERONE and the 21-hydroxy derivative of PROGESTERONE	21-Hydroxyprogesterone,Cortexone,Deoxycorticosterone,Desoxycortone,11-Decorticosterone,21-Hydroxy-4-pregnene-3,20-dione,11 Decorticosterone,21 Hydroxy 4 pregnene 3,20 dione,21 Hydroxyprogesterone