Antihypertensive Effect of a Novel Calcium Antagonist, SD-3211, in Experimental Hypertensive Rats

Takada, Toyokazu; Miyawaki, Nobuaki; Kageyama, Masaaki; Matsuno, Kiyoshi; Ishida, Narihiro; Yamauchi, Hideyasu; Iso, Tadashi

doi:10.1097/00005344-199112000-00011

Cited by 17 publications

(14 citation statements)

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“…phenyl]-4-methyl-2H-1 ,4-benzothiazine-3(4H)-one hydrogen fumarate) (chemical structure shown in Figure 1), was reported to be an orally active Ca2+ antagonist with antihypertensive (Kageyama et al, 1991b;Takada et al, 1991) and antianginal activities (Mori et al, 1990a;. Semo-tiadil has a quite different chemical structure from dihydropyridine Ca2+ antagonists but like the dihydropyridines, it is vasoselective compared with other non-dihydropyridine Ca2+ antagonists such as verapamil and diltiazem (Yoneyama et al, 1990;Nishimura et al, 1990;Miyawaki et al, 1991).…”

Section: Phenoxy]ethyl]amino]propoxy]mentioning

confidence: 99%

Effects of semotiadil fumarate, a novel Ca²⁺ antagonist, on cytosolic Ca²⁺ level and force of contraction in porcine coronary arteries

Kageyama

Yanagisawa

Taira

1995

British J Pharmacology

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Section: Phenoxy]ethyl]amino]propoxy]mentioning

confidence: 99%

Effects of semotiadil fumarate, a novel Ca²⁺ antagonist, on cytosolic Ca²⁺ level and force of contraction in porcine coronary arteries

Kageyama

Yanagisawa

Taira

1995

British J Pharmacology

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“…Furthermore, semotiadil shows long-lasting antihypertensive effects in spontaneously hypertensive rats (SHR) and renal hypertensive dogs (Kageyama et al, 1991;Takada et al, 1991a;Kanda & Hashimoto, 1993). Thus, the earlier studies suggest that semotiadil is a new class of Ca2" antagonist.…”

Section: Introductionmentioning

confidence: 99%

Pharmacological profile of semotiadil fumarate, a novel calcium antagonist, in rat experimental angina model

Mori

Ishigai

Fukuzawa

et al. 1995

British J Pharmacology

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1 The aim of the present study was to determine whether antianginal efficacy of semotiadil fumarate (SD-321 1), a structurally novel calcium antagonist, is distinct from those of diltiazem, nifedipine and nisoldipine.2 First, the duration of the inhibitory effects of semotiadil was compared with that of other Ca2l antagonists in rat experimental angina evoked by vasopressin. Semotiadil (10 mg kg-', p.o.) was effective for at least 9 h in the anginal model and those effects of semotiadil were longer-lasting than those of diltiazem (30 mg kg', p.o.), nifedipine (10 mg kg-', p.o.), and nisoldipine (3 mg kg-', p.o.).3 Second, the selectivity of actions of these Ca2l antagonists for the coronary arteries and myocardium was evaluated in rat isolated perfused hearts. Diltiazem (10 M) reduced cardiac contractility without inhibiting the elevation of perfusion pressure evoked by acetylcholine. Semotiadil (10-M) significantly suppressed cardiac contractility and inhibited the coronary response to acetylcholine. In contrast, nifedipine (3 x 0 9-3 x 108 M) and nisoldipine (3 x I&0°-14I M) did not reduce cardiac contractility at concentrations which significantly inhibited the increase in perfusion pressure to acetylcholine. 4 The selectivity of semotiadil for coronary artery and myocardium is intermediate between diltiazem and dihydropyridines tested in the present study. 5 These findings suggest that semotiadil has an advantage of diltiazem, nifedipine, and nisoldipine in the treatment of angina with regard to long-lasting action and selectivity for coronary artery and myocardium.

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“…The view was confirmed by a recent electrophysiological study, which indicated that semotiadil inhibited unitary calcium cur rents through voltage-dependent calcium channels (2). Oral administration of semotiadil produced long-lasting antihypertensive effects in hypertensive dogs and rats (3,4) and antianginal effects in rats (5,6).…”

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confidence: 83%

Effects of Semotiadil (SD-3211), a Benzothiazine Calcium Antagonist, on Blood Pressure and Atrioventricular Conductivity in Anesthetized Dogs

Kageyama

Yamada

Satoh

et al. 1992

Japanese Journal of Pharmacology

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ABSTRACT-We investigated the effects of semotiadil (SD-3211), a novel calcium antagonist, on blood pressure and the atrioventricular (AV) conduction time and functional refractory period (FRP) of the AV conduction system (AV conductivity) in anesthetized open-chest dogs. The heart was electrical ly stimulated at a constant rate. In dogs with an intact nerve supply to the heart, i.v.-injections of semotiadil (0.03 to 0.3 mg/kg) produced a fall of blood pressure in a dose-dependent manner. AV con duction time and FRP were prolonged by rather higher doses (0.3 mg/kg), and second-degree AV block occurred only with the highest dose (1 mg/kg). In dogs with the nerve supply to the heart inter rupted, the vasodepressor effects and suppressant effects of semotiadil on AV conductivity were slightly enhanced. The suppressant effects on AV conductivity became marked as pacing rates were increased. These results suggest that semotiadil at appropriate doses produces a vasodepressor effect without affecting AV conductivity even in the heart deprived of nervous control, e.g., the heart with ,8-adre noceptors blocked. The frequency-dependent suppressant effect on FRP of semotiadil is also notewor thy in the treatment of reentrant supraventricular tachycardia that involves the AV node.

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Antihypertensive Effect of a Novel Calcium Antagonist, SD-3211, in Experimental Hypertensive Rats

Cited by 17 publications

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Effects of semotiadil fumarate, a novel Ca²⁺ antagonist, on cytosolic Ca²⁺ level and force of contraction in porcine coronary arteries

Effects of semotiadil fumarate, a novel Ca²⁺ antagonist, on cytosolic Ca²⁺ level and force of contraction in porcine coronary arteries

Pharmacological profile of semotiadil fumarate, a novel calcium antagonist, in rat experimental angina model

Effects of Semotiadil (SD-3211), a Benzothiazine Calcium Antagonist, on Blood Pressure and Atrioventricular Conductivity in Anesthetized Dogs

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Antihypertensive Effect of a Novel Calcium Antagonist, SD-3211, in Experimental Hypertensive Rats

Cited by 17 publications

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Effects of semotiadil fumarate, a novel Ca2+ antagonist, on cytosolic Ca2+ level and force of contraction in porcine coronary arteries

Effects of semotiadil fumarate, a novel Ca2+ antagonist, on cytosolic Ca2+ level and force of contraction in porcine coronary arteries

Pharmacological profile of semotiadil fumarate, a novel calcium antagonist, in rat experimental angina model

Effects of Semotiadil (SD-3211), a Benzothiazine Calcium Antagonist, on Blood Pressure and Atrioventricular Conductivity in Anesthetized Dogs

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Effects of semotiadil fumarate, a novel Ca²⁺ antagonist, on cytosolic Ca²⁺ level and force of contraction in porcine coronary arteries

Effects of semotiadil fumarate, a novel Ca²⁺ antagonist, on cytosolic Ca²⁺ level and force of contraction in porcine coronary arteries