Beta‐adrenoceptor partial agonists: a renaissance in cardiovascular therapy?

Waller, Derek G.

doi:10.1111/j.1365-2125.1990.tb03760.x

Cited by 19 publications

(9 citation statements)

References 88 publications

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“…Under resting conditions with low levels of circulating adrenaline and noradrenergic drive, P-receptor occupancy by catecholamines is relatively sparse and the intrinsic heart rate is controlled by the dominant vagal tone. In this situation of low endogenous competition for p-receptors, partial agonist drugs may be seen to exert their pharmacological effects (Reithman et al, 1989;Waller, 1990). In the present study the effects on resting parameters of SBP, K and Tr were used to assess selectivity of PAA.…”

Section: Discussionmentioning

confidence: 90%

Selectivity of antagonist and partial agonist activity of celiprolol in normal subjects.

Wheeldon

McDevitt

Lipworth

1992

Brit J Clinical Pharma

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1 The aims of this study were to assess the relative r31'132 selectivity of the antagonist and partial agonist activity (PAA) of celiprolol in man. 2 Eight normal males received single oral doses of celiprolol 200 mg (C200), 400 mg (C400) and 800 mg (C800); atenolol 50 mg (A50), 100 mg (A100) and 200 mg (A200); nadolol 40 mg (N40) and placebo (PL), administered in a single-blind, randomised crossover design. 3 At rest, in the presence of low levels of circulating adrenaline and noradrenergic tone, a low dose of celiprolol (C200) showed evidence of 13l-PAA by significant increases in systolic blood pressure and resting heart rate. At higher doses (C400, C800), 132-PAA became evident by a significant increase in postural finger tremor, whereas C200 had no effect.

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Section: Discussionmentioning

confidence: 90%

Selectivity of antagonist and partial agonist activity of celiprolol in normal subjects.

Wheeldon

McDevitt

Lipworth

1992

Brit J Clinical Pharma

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“…Another important factor to be considered is that at rest, when sympathetic tone is low, circulating levels of catecholamines provide little competition for partial agonist drugs which may therefore occupy p-receptors and demonstrate their stimulatory effects (Reithmann et al, 1989;Waller, 1990). However, in the presence of a full agonist such as the noradrenergic (ISl) response to exercise or terbutaline (P2), the partial agonist drug effectively switches to behave as an antagonist.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of in vivo partial beta 1/beta 2‐agonist activity: a dose‐ ranging study with carteolol.

Wheeldon

McDevitt

Lipworth

1992

Brit J Clinical Pharma

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“…Under basal conditions selective and non-selective ,3-adrenoceptor blockers have different effects on renin release (Waller, 1990). Plasma renin activity (PRA) is reported to increase with exercise (Hespel et al, 1988) but whether or not there is a different response during 13-adrenoceptor blockade by agents with and without PAA is unclear.…”

Section: Introductionmentioning

confidence: 99%

“…Oral therapy with 3-adrenoceptor antagonists lowers blood pressure by reducing cardiac output, although agents with significant partial agonist activity (PAA) have less effect on cardiac output and change blood pressure little if at all (Waller, 1990).…”

Section: Introductionmentioning

confidence: 99%

The effects of selective beta‐adrenoceptor antagonists and partial agonist activity on renal function during exercise in normal subjects and those with moderate renal impairment.

Taverner

Mackay

Craig

et al. 1991

Brit J Clinical Pharma

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1 The effects of sustained moderate exercise in the sitting position on renal haemodynamics and glomerular filtration were measured in six normotensive patients with moderately impaired renal function and seven age-matched normal volunteers. 2 The changes in the effects of exercise on renal function induced by chronic cardioselective ,B-adrenoceptor blockade by drugs with (epanolol) and without intrinsic sympathomimetic activity (atenolol) were examined. 3 Both ,B-adrenoceptor blockers attenuated the heart rate increase with exercise, but only atenolol lowered blood pressure significantly. In resting volunteers on atenolol, associated with the fall in blood pressure there was a significant reduction in glomerular filtration rate. 4 Glomerular filtration fell significantly in all groups with exercise, and renal blood flow also fell in parallel. These changes were not influenced by drug treatment. 5The exercise-induced rise in PRA was suppressed by atenolol but not by epanolol. 6 The renal function and haemodynamic responses to moderate exercise does not appear to be mediated by the systemic renin-angiotensin system or by 13l-adrenoceptors.

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Beta‐adrenoceptor partial agonists: a renaissance in cardiovascular therapy?

Cited by 19 publications

References 88 publications

Selectivity of antagonist and partial agonist activity of celiprolol in normal subjects.

Selectivity of antagonist and partial agonist activity of celiprolol in normal subjects.

Evaluation of in vivo partial beta 1/beta 2‐agonist activity: a dose‐ ranging study with carteolol.

The effects of selective beta‐adrenoceptor antagonists and partial agonist activity on renal function during exercise in normal subjects and those with moderate renal impairment.

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