Effect of efonidipine hydrochloride (NZ-105), a dihydropyridine derivative with calcium antagonistic action, on myocardial oxygen tension in anesthetized dogs.

Fujikura, Naoki; Yokoyama, Tatsuro; Masuda, Yuichi; Shikada, Ken-ichi; Tanaka, Sakuya

doi:10.1254/fpj.108.267

Cited by 2 publications

(1 citation statement)

References 7 publications

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“…Efonidipine, however, produces little or no reflex tachycardia in humans (46,61), conscious rabbits (62), or anesthetized dogs (68). In open-chest dogs efonidipine decreased heart rate (10,11,67). These effects were initially attributed to the slow onset of efonidipine's action (19,30,65).…”

Section: Effect On Cardiac Pacemakingmentioning

confidence: 99%

Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca²⁺ Channels

Tanaka

Shigenobu

2002

Cardiovascular Drug Reviews

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T-type Ca 2+ channels have properties different from those of the L-type and are involved in cardiac pacemaking and regulation of blood flow, but not in myocardial contraction. Efonidipine is an antihypertensive and antianginal drug with dihydropyridine structure that was recently found to block both L-and T-type Ca 2+ channels. In isolated myocardial and vascular preparations, efonidipine has potent negative chronotropic and vasodilator effects but only a weak negative inotropic effect. In experimental animals and patients, reduction of blood pressure by the drug was accompanied by no or minimum reflex tachycardia leading to improvement of myocardial oxygen balance and maintenance of cardiac output. Efonidipine increased glomerular filtration rate without increasing intraglomerular pressure. By relaxing both the afferent and efferent arterioles, efonidipine markedly reduced proteinuria. Thus, efonidipine, an L-and T-type dual Ca 2+ channel blocker, appears to have an ideal profile as an antihypertensive and antianginal drug with organ-protective effects in the heart and kidney.

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Section: Effect On Cardiac Pacemakingmentioning

confidence: 99%

Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca²⁺ Channels

Tanaka

Shigenobu

2002

Cardiovascular Drug Reviews

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Pathophysiological Significance of T-type Ca2+ Channels: T-type Ca2+ Channels and Drug Development

Tanaka

Shigenobu

2005

J Pharmacol Sci

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Abstract. T-type Ca2+ channels are present in cardiovascular, neuronal, and endocrine systems; and they are now receiving attention as novel therapeutic targets. Many drugs and compounds non-specificaly block T-type Ca 2+ channels. Certain dihydropyridine compounds, such as efonidipine, have blocking activity on both L-type and T-type Ca 2+ channels which possibly underlies their excellent clinical profiles such as minimum reflex tachycardia and renal protection. Selective inhibitors of T-type Ca 2+ channels, such as non-hydrolyzable mibefradil and R(−)-efonidipine, are powerful pharmacological tools for further studies and may lead to the development of novel therapeutic strategies.

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Effect of efonidipine hydrochloride (NZ-105), a dihydropyridine derivative with calcium antagonistic action, on myocardial oxygen tension in anesthetized dogs.

Cited by 2 publications

References 7 publications

Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca²⁺ Channels

Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca²⁺ Channels

Pathophysiological Significance of T-type Ca2+ Channels: T-type Ca2+ Channels and Drug Development

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Effect of efonidipine hydrochloride (NZ-105), a dihydropyridine derivative with calcium antagonistic action, on myocardial oxygen tension in anesthetized dogs.

Cited by 2 publications

References 7 publications

Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca2+ Channels

Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca2+ Channels

Pathophysiological Significance of T-type Ca2+ Channels: T-type Ca2+ Channels and Drug Development

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Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca²⁺ Channels

Efonidipine Hydrochloride: A Dual Blocker of L‐ and T‐Type Ca²⁺ Channels