Studies of Novel 1, 4-Dihydropyridine Ca Antagonist CS-905. I. Measurement of Partition Coefficient (logP) by High Performance Liquid Chromatography (HPLC)

Masumoto, Kazue; Takeyasu, Akira; Oizumi, Kiyoshi; Kobayashi, Takashi

doi:10.1248/yakushi1947.115.3_213

Cited by 57 publications

(35 citation statements)

References 3 publications

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“…The partition coefficient (log P OW ) of benidipine, measured by the flask-shaking method, was 3.79. The same parameter measured with LC (log P HPLC ) was 4.61, indicating the very high liposolubility of benidipine compared with nifedipine and amlodipine (log P HPLC : 2.20 and 3.95) (14).…”

Section: +mentioning

confidence: 59%

Pharmacological, Pharmacokinetic, and Clinical Properties of Benidipine Hydrochloride, a Novel, Long-Acting Calcium Channel Blocker

Yao

Nagashima

Miki³

2006

J Pharmacol Sci

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Abstract. Benidipine is a dihydropyridine-derived calcium channel blocker developed in Japan, with several unique mechanisms of action, that is, triple calcium channels (L, N, and T) blocking action with a membrane approach. Benidipine has relatively high vascular selectivity and is expected to show protective effects on vascular endothelial cells. Renal protective effects of benidipine also have been shown in several basic and clinical studies. Moreover, anti-oxidative action and enhancing nitric oxide production have been noted with this drug, following its cardioprotective effects in patients with ischemic heart diseases. In fact, benidipine exerted a better prognostic effect than other calcium channel blockers in the therapy for patients with vasospastic angina. In addition, benidipine showed reliable antihypertensive, renoprotective effects if used in combination with angiotensin II type 1 receptor blockers (ARBs) when adequate anti-hypertensive effects are not achieved by ARBs alone, indicating that benidipine is an useful calcium channel blocker in combination therapy for hypertension. Benidipine was launched on the Japanese market 14 years ago, but few severe side effects have been reported, suggesting that this is a drug with established safety and long-acting pharmacological effects.

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Section: +mentioning

confidence: 59%

Pharmacological, Pharmacokinetic, and Clinical Properties of Benidipine Hydrochloride, a Novel, Long-Acting Calcium Channel Blocker

Yao

Nagashima

Miki³

2006

J Pharmacol Sci

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“…35 The instruments were Waters Alliance 2795 HPLC system with 2996 UV-vis detector (Milford, MA, USA).…”

Section: In Vitro Inhibitory Activity Against Dgat1 Dgat2 and Acat1mentioning

confidence: 99%

Optimization of a novel series of N-phenylindoline-5-sulfonamide-based acyl CoA:monoacylglycerol acyltransferase-2 inhibitors: Mitigation of CYP3A4 time-dependent inhibition and phototoxic liabilities

Sato

Takahagi

Kubo

et al. 2015

Bioorganic & Medicinal Chemistry

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“…24 Because the dihydropyridine ring that is present in CCBs can easily capture a free electron, CCBs have an antioxidative effect. 25 Previous study has suggested that the infarct volume was reduced by CCBs with antioxidant action after transient middle cerebral artery ischemia in rats. 8 In a study using SHRSP, CCB also prevented oxidative stress through the regulation of Cu/Zn superoxide dismutase activity.…”

Section: Production Of Superoxide Anion In the Brainmentioning

confidence: 97%

The Impact of Combined Treatment with Atorvastatin and Amlodipine in Stroke-prone Spontaneously Hypertensive Rats

Muraga

Nito

Ueda

et al. 2014

Cerebral Blood Flow and Metabolism

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Aims: Previous studies suggest that both statins and calcium-channel blockers inhibit cardiovascular and cerebrovascular diseases by their pleiotropic effects, such as antioxidation and anti-inflammatory actions. By using stroke-prone spontaneously hypertensive rats (SHRSPs), the isolated effect of each pharmaceutical has been reported, but the effect of a combination of both pharmaceuticals has not been reported. In this study, we evaluated combination therapy of atorvastatin and amlodipine for its efficacy in preventing stroke in the SHRSP model. Main Methods: We initiated treatment of SHRSPs at 8 weeks of age with atorvastatin (2 mg/kg), amlodipine (1 mg/kg), a combination of atorvastatin (2 mg/kg) and amlodipine (1 mg/kg), or vehicle.Measurement of physiological parameters and immunohistochemical assessments for oxidative stress and inflammation were done at each group. Key findings: At 13 weeks of age, the combination therapy group showed greater inhibition of an antioxidation and anti-inflammatory marker than the vehicle group, although there were no differences in blood pressure. Significance: Our study suggests that the combination therapy of atorvastatin and amlodipine may protect against hypertension-induced stroke by the additive effect of the antioxidation and the anti-inflammatory action of the both agents.Cerebral Blood Flow and Metabolism 25: 23-30, 2014

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Studies of Novel 1, 4-Dihydropyridine Ca Antagonist CS-905. I. Measurement of Partition Coefficient (logP) by High Performance Liquid Chromatography (HPLC)

Cited by 57 publications

References 3 publications

Pharmacological, Pharmacokinetic, and Clinical Properties of Benidipine Hydrochloride, a Novel, Long-Acting Calcium Channel Blocker

Pharmacological, Pharmacokinetic, and Clinical Properties of Benidipine Hydrochloride, a Novel, Long-Acting Calcium Channel Blocker

Optimization of a novel series of N-phenylindoline-5-sulfonamide-based acyl CoA:monoacylglycerol acyltransferase-2 inhibitors: Mitigation of CYP3A4 time-dependent inhibition and phototoxic liabilities

The Impact of Combined Treatment with Atorvastatin and Amlodipine in Stroke-prone Spontaneously Hypertensive Rats

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