The effects of bucumolol (BUC), nadolol (NAD) and nifenalol (NIF) on contractile forces and on action potentials (APs) were investigated in isolated guinea pig atrial and papillary muscles, respectively. Log 1/ED40 values for the negative inotropic effects of these drugs were 0.097, 10 and 0.74 mmol/l in this order. BUC (50 mumol/l), NAD (0.5 mmol/l) and NIF (0.2 mmol/l) produced about 60, 20 and 20% reduction of Vmax at 1 Hz. The frequency-dependent reductions at these and higher concentrations were greatest for BUC, intermediate for NAD and least for NIF. These potencies at certain frequencies were, as a whole, consistent with log P-potency relationship established in our previous papers (Harada et al. 1981; Ban et al. 1985). The reductions of Vmax in APs in response to premature stimuli during basic stimuli at the rate of 0.25 or 0.027 Hz decayed exponentially during diastolic intervals (DI). The time constants of these decay process (tau) estimated by linear and nonlinear regression analyses and by eye were 12.2-9.6 s for BUC (50-100 mumol/l) and 2.9-4.8 s for NAD (1-2 mmol/l) and 57-87 ms for NIF (0.2-1 mmol/l). In terms of the molecular weight (MW)-log tau relationship (Ban et al. 1985), these tau values are within the 95% fiducial limit for BUC and NAD and deviated from the lower fiducial limit for NIF. The frequency-dependent reductions of Vmax by these drugs were explained in terms of a function of tau and the intercept Ao. Based on the study made by Cohen et al.(ABSTRACT TRUNCATED AT 250 WORDS)

01 Nov 1981·Archives internationales de pharmacodynamie et de therapie

Assessment of beta-blockade and the non-specific effect of bucumolol, a beta-adrenergic blocking agent, on atrioventricular conduction in anesthetized dogs.

Article

Author: Nakayama, K ; Oshima, T ; Koike, H

The effects of the beta-adrenergic blocking agent bucumolol [dl-5-methyl-8-(2-hydroxy-3-t-butylaminoproxy)coumarin] and its optical isomers were compared with those of propranolol and pindolol on the functional refractory period and the conduction time of atrioventricular (A-V) transmission in dogs. In dogs with intact nerves anesthetized with pentobarbital, bucumolol and propranolol (30 micrograms - 1 mg/kg) prolonged both parameters by blockade of background sympathetic nervous tone to A-V conduction. The optical d- and l-isomers of bucumolol depressed A-V conduction almost in parallel with their beta-blocking actions. In dogs with cardiac sympathectomy and bilateral vagotomy, or pretreated with reserpine, the dromotropic activity was lowered and the beta-blocking dose (30 micrograms - 1 mg/kg) of bucumolol and propranolol had less effect on A-V conduction, while larger doses (3-10 mg/kg) produced additional depression of the conduction. Pindolol, on the other hand, had a positive dromotropic action, reflecting its intrinsic stimulatory action. It is concluded that A-V conduction is affected by the existing tone of sympathetic nervous activity and that bucumolol has no beta-stimulant action and depresses A-V conduction by beta-blockade and by a non-specific action.

01 Jan 1981·Journal of Pharmacobio-Dynamics

Antihypertensive activity of bucumolol, a .BETA.-adrenergic blocking agent, in spontaneously hypertensive rats.

Article

Author: Koike, Hiroyuki ; Miyamoto, Masaaki ; Nishino, Hiroshi ; Ito, Katsuaki

Effects of bucumolol, a beta-adrenergic blocking agent, on blood pressure and the renin angiotensin system were studied in spontaneously hypertensive rats (SHR). The results were compared with those of propranolol at an equipotent dose in beta-adrenergic blocking activity. Bucumolol lowered blood pressure and decreased plasma renin concentration (PRC) in both acute and long-term experiments. There was a significant correlation between percent changes in blood pressure and PRC following a single administration of bucumolol. Decrease in PRC persisted for the 6-week observation period despite the sustained reduction in blood pressure. On the other hand, propranolol did not lower blood pressure in acute experiment while it decreased renin release. These results suggest that inhibition of renin release is involved in the antihypertensive action of bucumolol.

100 Deals associated with Bucumolol

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KEGG	Wiki	ATC	Drug Bank
D01492	Bucumolol	-	-

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Angina Pectoris	-	-	-
Tachycardia, Sinus	-	-	-

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Indication	Highest Phase	Country/Location	Organization	Date
Hypertension	Preclinical	-	Daiichi Sankyo Co., Ltd.	-

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