AbstractThe in-vivo pharmacodynamics of S-2150, a newly developed dual-blocking type antihypertensive drug, was evaluated following intravenous infusion to rats. Previous in-vitro studies showed that the drug has two distinct mechanisms of antihypertensive effect—calcium-channel blocking activity and α1-adrenoceptor antagonism—which could be explained by a combination of two different pharmacodynamic models.The present in-vivo study showed that S-2150 also displays a complex pharmacodynamic profile (as measured by the decrease in mean blood pressure), which could be described by a combination of two sigmoid Emax models independently connected with the central compartment and the effect compartment.These results suggested that the dual-blocking mechanism of S-2150, which has been observed in in-vitro experiments, was also evaluated by the pharmacodynamic analysis of in-vivo experimental data.

01 Dec 1997·Cardiovascular Drug Reviews

Cardiovascular Pharmacological Characteristics of S‐2150: A Novel Dual Blocker of Calcium Channels and α₁‐Adrenoceptors

Author: Nakashima, Mitsuyoshi ; Iwaki, Kazumi ; Kishi, Morio

A review, with 40 references, describing the structure, toxicol. properties, in vitro and in vivo pharmacol., pharmacokinetics in animals, and phase I clin. effects of S-2150.

01 Feb 1997·Journal of Cardiovascular PharmacologyQ4 · MEDICINE

Pharmacological Studies on a New Antihypertensive Agent, S-2150, a Benzothiazepine Derivative: 3. Hypotensive and Antimyocardial-Stunning Effects in Dogs

Q4 · MEDICINE

Article

Author: Yoshimura, Kohji ; Ueda, Motohiko ; Matsuura, Eiichi ; Hirono, Satoru ; Haruna, Masao ; Uno, Osamu ; Iwaki, Kazumi ; Kimoto, Sadatoshi ; Ishii, Mitsuo

The hypotensive and antimyocardial-stunning effects of a new 1,5-benzothiazepine antihypertensive agent, S-2150, were investigated in dogs. S-2150 (30 mg/kg, p.o.) decreased the blood pressure in conscious renal hypertensive dogs. Although the maximal hypotensive effect of S-2150 was observed at 5-9 h after administration, the effect of diltiazem was seen at 2.0 h. Arrhythmia was not observed as a hypotensive effects of S-2150 but was markedly induced by diltiazem. In anesthetized open-chest dogs, S-2150 (20 micrograms/kg/min, i.v.) caused by hypotensive effect similar to that of diltiazem but decreased myocardial work (double product) by much less than did diltiazem. S-2150 more promptly improved the local myocardial stunning caused by occlusion of the left anterior descending coronary artery and its reperfusion. This effect did not accompany the energy-sparing action in ischemic/reperfused myocardium, which was different from the case of diltiazem. In isolated dog mesenteric arteries, S-2150 relaxed KCl and phenylephrine contracture. These results suggest that S-2150 is a favorable hypotensive agent for hypertensive patients with ischemic heart disease. Blockage of both Ca2+ channels and alpha 1-adrenoceptors by S-2150 seems to lead to cardiovascular effects different from those of diltiazem.

100 Deals associated with S-2150

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Indication	Highest Phase	Country/Location	Organization	Date
Arrhythmias, Cardiac	Phase 2	Japan	Shionogi & Co., Ltd.	-
Hypertension	Phase 2	Japan	Shionogi & Co., Ltd.	-
Myocardial Infarction	Phase 2	Japan	Shionogi & Co., Ltd.	-

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