A double-blind, double cross-over trial of prenylamine in angina pectoris

Winsor, Travis; Bleifer, Kenneth H.; Cole, Seymour L.; Goldman, I.Ralph; Karpman, Harold L.; Oblath, Robert W.; Stone, Shannon

doi:10.1016/0002-8703(71)90160-8

Cited by 25 publications

(9 citation statements)

References 8 publications

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“…However, large doses of PNL do not reduce myocardial noradrenalin by more than 60%, as measured 4 h to 7 days after its injection (22). Therefore, it is very difficult to admit that the inhibition by PNL of electrocardiographic and histologic changes induced by ISP in the monkey (13) could be mediated through a catecholamine reduction in adrenergic nerves.…”

Section: Discussionmentioning

confidence: 99%

Prenylamine. Autoradiographic and neuropathological studies on myocardial mechanisms of action

Milei

Faccio

1979

Clinical Cardiology

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Summary:Myocardial localization of prenylamine (PNL), a well known antianginal drug, was studied by means of an autoradiographic technique to detect microscopical distribution of tritiated PNL (3H-PLN). Forty Wistar rats received 35 .uCi/kg b. w. 3H-PNL i. p., the animals being killed 30 min after injection.Heart slices, 1 mm thick, were processed for both autoradiographic and conventional histological techniques.3H-PNL was observed, mainly, as striae along sarcolemma; sarcolemmatic/intramyocardial 3H-PNL distribution ratio was 6 : 1. Preferential membrane deposition of 3H-PNL is probably related to the calcium transport inhibiting action of the drug, previously described.

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Section: Discussionmentioning

confidence: 99%

Prenylamine. Autoradiographic and neuropathological studies on myocardial mechanisms of action

Milei

Faccio

1979

Clinical Cardiology

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“…as measured 4 h to 7 days after its injection [1], Therefore, it is very difficult to admit that the inhibition by PNL of electrocardiographic and histologic changes induced by ISP in rats and monkeys could be mediated through a catecholamine reduction in adrenergic nerves. One would think that a direct effect is acting, especially by the early onset of action.…”

Section: Wistar Ratsmentioning

confidence: 99%

“…Better categorization of the mechanisms of action of the drug is necessary because PNL has been proved as a drug that relieves angina pectoris [1], and recently antiarrhythmic effects have also been described [33], Then, its clinical implication as a calcium antagonistic drug seems to become obvious.…”

Section: Wistar Ratsmentioning

confidence: 99%

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An Overall Review on Prenylamine Mechanisms of Action in Experimental Models of Myocardial Damage

Milei¹,

Vázquez²,

Bolomo³

1982

Cardiology

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In this review we present the effects of a well-known antianginal drug, prenylamine (PNL), in experimental models of acute myocardial damage induced by a β-agonistic drug, isoproterenol (ISP), in several trials conducted in our laboratory in both rats (n = 204) and monkeys (n = 26). PNL significantly inhibited ISP-induced lesions, protecting the majority of animals studied. Studies dealing with the site of action of the drug, such as ⁴⁵Ca, ³H-PNL and ³H-ISP trials, showed a clear membrane effect slowing down Ca transport. Correlation between ECG (inhibition of ST depression after ISP) and pathological findings in monkeys was also obtained in one of our experiments. These series of assays were useful in obtaining a more complete idea of activity and site of action of the drug. It seems that, in acute models, PNL acts as a calcium antagonistic drug rather than an adrenergic moderator.

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“…Prenylamine is a well known antianginal drug (Winsor et al, 1971). However, its mechanisms of action are not entirely clear (Milei et al, 1982).…”

Section: Introductionmentioning

confidence: 99%

The effects of prenylamine on single ventricular myocytes of guinea‐pig

Shimoni

Posner²,

Spindler³

et al. 1988

British J Pharmacology

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1 The action of prenylamine, an antianginal drug, was studied in single ventricular guinea-pig myocytes. In concentrations of 10-50 pm, prenylamine significantly (P <0.01) shortened action potentials, and significantly (P < 0.001) reduced the inward calcium current by 29% to 76% (n = 7). This effect was also present in the presence of adrenoceptor-blockade (with phentolamine and propranolol), and was thus not due to indirect changes in endogenous catecholamine action. 2 Prenylamine did not affect the steady state level of current at the end of long pulses, and does therefore not act by changing time-dependent outward currents. Since the resting potential in the unclamped mode is unchanged during gross changes in action potential duration, it is also unlikely that there are any changes in the background, time-independent potassium conductance. 3 It is concluded that prenylamine has a direct effect on cardiac calcium channels, not mediated by adrenoceptor activation.

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A double-blind, double cross-over trial of prenylamine in angina pectoris

Cited by 25 publications

References 8 publications

Prenylamine. Autoradiographic and neuropathological studies on myocardial mechanisms of action

Prenylamine. Autoradiographic and neuropathological studies on myocardial mechanisms of action

An Overall Review on Prenylamine Mechanisms of Action in Experimental Models of Myocardial Damage

The effects of prenylamine on single ventricular myocytes of guinea‐pig

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