Analysis of the actions of alprenolol and propranolol on the beta adrenergic receptors controlling heart rate in the anaesthetized cat

Åblad, Bengt; Brändström, Arne; Ek, Lars; Sjölander, May

doi:10.1016/0014-2999(71)90185-3

Cited by 20 publications

(4 citation statements)

References 18 publications

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“…Ablad et al (1971) also demonstrated good agreement between receptor occupancy theory and the action of isoprenaline, alprenolol and propranolol on the 0-adrenoceptors controlling heart rate in the anaesthetized cat. It is therefore appropriate to consider the classical mechanism of reversible competitive reactions on a single receptor site.…”

Section: Mathematical Modelsupporting

confidence: 57%

An application of receptor models to the analysis of data on ?-adrenoceptor blockade

Ferguson¹,

Robertson

Bilski³

et al. 1979

Clin Exp Pharmacol Physiol

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1. The classical single receptor competitive occupancy model accurately describes the joint action of an agonist (isoprenaline) and a beta-adrenoceptor antagonist (propranolol) or some partial agonists (dichlorisoprenaline, practolol) on the positive chronotropic response in rats which have been depleted of catacholamines. 2. The mathematical form of the model suggests that the dissociation constants of classical competitive partial agonists may be assessed using dose ratios by exactly the same method as that currently used for agonist-antagonist interactions, provided that the log dose-response curves are first suitably normalized. 3. Close agreement between the theoretical mathematical models and the experimental data can be demonstrated by statistical fitting for certain beta-adrenoceptor antagonists (propranolol, dichlorisoprenaline, practolol). 4. The model fails to describe the behaviour of other beta-adrenoceptor antagonists (oxprenolol, pindolol). A possible extension of the model to include these drugs is proposed.

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Section: Mathematical Modelsupporting

confidence: 57%

An application of receptor models to the analysis of data on ?-adrenoceptor blockade

Ferguson¹,

Robertson

Bilski³

et al. 1979

Clin Exp Pharmacol Physiol

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“…These positive inotropic and chronotropic effects were more prominent in reserpinized dogs. Thus we conclude that OPC-1085 has a sympathomime tic action which is well known with alprenolol (18,19), Ko 1366 (10) and dichloroisopro terenol (20). Hashimoto et al (21) and Ohkuda et al (22) have observed that an intra arterial injection of a smaller dose of dichloroisoproterenol, pindolol, alprenolol or pra ctolol produced a positive chronotropic response in the in situ sino-atrial node prepara tion which is the same as was seen with Kb 1366, pindolol or practolol in the isolated blo od-perfused one (23).…”

Section: Resultsmentioning

confidence: 95%

CARDIOVASCULAR STUDIES OF 5-(3-Tert-Butylamino-2-Hydroxy) PROPOXY-3,4-DIHYDROCARBOSTYRIL HYDROCHLORIDE (OPC- IOS5), a NEW POTENT Β-Adrenergic BLOCKING AGENT

Yabuuchi

Kinoshita

1974

Japanese Journal of Pharmacology

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Abstract-The~-adrenergic blocking and hemodynamic properties of 5-(3-tert-butyl amino-2-hydroxy) propoxy-3, 4-dihydrocarbostyril hydrochloride (OPC-1085) were investigated and compared with those of propranolol and pindolol on myocardial contractile force, heart rate and arterial blood pressure in pentobarbital anesthetized dogs. OPC-1085 showed almost the same ~-adrenergic blocking potency as pindolol, but was approximately 30 and 20 times stronger than propranolol against isopro terenol and cardiac nerve stimulation, respectively. Slight negative inotropic and chronotropic responses were observed with OPC-1085 in effective blocking doses from 1 to 10 pg/kg but were converted to positive ones in doses from 30 to 30001ppg/kg in non-reserpinized dogs. In reserpinized dogs, both OPC-1085 and pindolol in duced only positive responses. These responses were more evident with OPC-1085.

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“…The KB values for antagonistic effects on heart rate and peripheral vascular dilatation were calculated according to Áblad et al 17 The formula used provided us with a series of KB values, one for each dose of test compound, in every experiment. These values which theoretically should be identical with each other within one experiment were, however, widely scattered due to a possible nonlinearity of the dose-response curve segment at its extreme points (i.e., around the 20-30 and the 70-80% level).…”

Section: Methodsmentioning

confidence: 99%

Adrenergic receptor agonists

Lövgren¹,

Hedberg²,

Jl³

1980

J. Med. Chem.

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Two hydroxy-substituted benzofuranylethanolamines (9 and 10), analogues of adrenoceptor-active aryloxypropanolamines, were prepared and their beta-adrenoceptor activity was examined. Compound 9 was found to be a beta 1-selective adrenergic agonist with high intrinsic activity. Due to the rigidity of the benzofuranyl moiety of 9, its functional groups cannot be brought into the same spatial positions as those of a phenylethanolamine-type agonist like isoprenaline. This could indicate that adrenergic agonists of the aryloxypropanolamine type and of the phenylethanolamine type are differently bound to the receptor when eliciting the effect.

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Analysis of the actions of alprenolol and propranolol on the beta adrenergic receptors controlling heart rate in the anaesthetized cat

Cited by 20 publications

References 18 publications

An application of receptor models to the analysis of data on ?-adrenoceptor blockade

An application of receptor models to the analysis of data on ?-adrenoceptor blockade

CARDIOVASCULAR STUDIES OF 5-(3-Tert-Butylamino-2-Hydroxy) PROPOXY-3,4-DIHYDROCARBOSTYRIL HYDROCHLORIDE (OPC- IOS5), a NEW POTENT Β-Adrenergic BLOCKING AGENT

Adrenergic receptor agonists

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