Acta pharmacologica et toxicologica
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Acta Pharmacol Toxicol (Copenh) · Nov 1977
Studies on the duration of local anaesthesia: structure/activity relationships in a series of homologous local anaesthetics.
When the number of carbon atoms on the piperidine-nitrogen of the mepivacaine molecule was increased up to four or five carbons, the toxicity of the compounds and the duration of their local anaesthetic effects were increased. With longer N-alkyl-chains, the general toxicity and the local anaesthetic potency - but not the tissue toxicity - were reduced. In dental infiltration anaesthesia only the short-chain compounds offered an acceptable local anaesthesia. In these tests, the medium-chain compounds had a very unfavourable quotient between dental anaesthesia and soft tissue anaesthesia, while the long-chain compounds could not be tested at all in man because of their tissue irritating properties.
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Acta Pharmacol Toxicol (Copenh) · Jan 1977
Comparative StudyPharmacodynamics of a new selective beta2-adrenergic bronchodilator 3-(4-methoxybenzylamino)-4-hydroxy-alpha-(tert. butylaminomethyl)-benzyl-alcohol, HCl (QH25).
The bronchodilator effect of QH25 (3-(4-methoxybenzylamino)-4-hydroxy-alpha-(tert. butylaminomethyl)benzylalcohol, HCl) a new beta2-adrenergic bronchodilator has been investigated in conscious guinea pigs and in anaesthetized guinea pigs and cats and compared to that of salbutamol and isoprenaline. In anaesthetized guinea pigs QH25 and isoprenaline were equipotent after intravenous administration, whereas salbutamol was four times less active. The same difference between QH25 and salbutamol was observed after intraduodenal administration. ⋯ The potential tremorogenic action of QH25 estimated on the cat soleus muscle was eight times less than that of isoprenaline and the same or slightly less than that of salbutamol. From the experimental data it is concluded that QH25 has the same potency as isoprenaline as a bronchodilator agent but is more potent than salbutamol. Taking into account that isoprenaline is considerably more active on cardiovascular parameters and on the cat soleus muscle than QH25 which has the same or less effect than salbutamol on these parameters the data suggest that QH25 is a more selective bronchodilator agent than both isoprenaline and salbutamol.