A selective β-adrenoreceptor stimulant (Th1165a) related to orciprenaline

O'Donnell S.R. (1970) A selective β-adrenoreceptor stimulant (Th1165a) related to orciprenaline. European Journal of Pharmacology, 12 1: 35-43. doi:10.1016/0014-2999(70)90026-9


Author O'Donnell S.R.
Title A selective β-adrenoreceptor stimulant (Th1165a) related to orciprenaline
Journal name European Journal of Pharmacology   Check publisher's open access policy
ISSN 0014-2999
Publication date 1970-01-01
Sub-type Article (original research)
DOI 10.1016/0014-2999(70)90026-9
Volume 12
Issue 1
Start page 35
End page 43
Total pages 9
Subject 2804 Cellular and Molecular Neuroscience
3004 Pharmacology
Abstract Th1165a is a chemical relative of orciprenaline which has been shown to be a β-adrenoreceptor stimulant since its actions are antagonized by propranolol. On guinea-pig tracheal chain and human bronchial chain preparations Th1165a was more potent than isoprenaline. However, a 45 fold higher concentration of Th1165a was required to produce a 50% maximum response of the isolated guinea-pig atria (chronotropic action) than was required on trachea. A 4 fold higher concentration of orciprenaline was required on atria than on trachea. Isoprenaline was equipotent on both preparations. Th1165a, administered by aerosol spray, was similar in potency to isoprenaline in preventing histamine bronchospasm in conscious guinea-pigs. Th1165a and isoprenaline were also similar in potency as bronchodilators in anaesthetized guinea-pigs, when given intravenously, but Th1165a was longer lasting. Th1165a produced less fall in blood pressure than an equal dose of isoprenaline in cats. High concentrations of Th1165a produced only a small contraction of the isolated rabbit thoracic aorta which was blocked by phentolamine. It did not contract the isolated rat vas deferens. These findings indicate that Th1165a has negligible effects on α-adrenoreceptors. The results obtained using Th1165a support the idea that the optimum structural requirements in a sympathomimetic amine might be different for stimulation of β-adrenoreceptors initiating bronchodilatation and those initiating cardiac stimulation.
Keyword Beta-receptor stimulant, selective
Guinea-pig trachea and atria
Orciprenaline derivative
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: Scopus Import
 
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Created: Tue, 12 Jul 2016, 10:47:49 EST by System User