COMPARATIVE STUDIES OF (−)‐, (±), (+)‐PROPRANOLOL, ATENOLOL, GUANETHIDINE, BRETYLIUM AND TETRACAINE ON ADRENERGIC TRANSMISSION
Open Access
- 1 October 1981
- journal article
- research article
- Published by Wiley in British Journal of Pharmacology
- Vol. 74 (2), 365-370
- https://doi.org/10.1111/j.1476-5381.1981.tb09980.x
Abstract
1 Effects of (−)‐, (±)‐, and (+)‐propranolol, atenolol, guanethidine, bretylium and tetracaine were studied on relaxation responses of rabbit ileum and contractile responses of rabbit pulmonary artery and guinea‐pig vas deferens to electrical nerve stimulation (2 to 50 Hz) 2 In the ileum, inhibition by tetracaine 3.3 × 10−6M occurred at high frequencies of stimulation, while bretylium 1.2 × 10−4 M and guanethidine 2 × 10−5 M inhibited responses at all frequencies, the latter producing greater inhibition at low frequencies 3 (±)‐Propranolol 10−5 M produced a tetracaine‐type inhibition after 1 h and a bretylium‐pattern after 2 h in the ilea and pulmonary arteries and a transition from bretylium‐ to guanethidine‐pattern in the vas deferens, while atenolol 2 × 10−5 to 10−4M produced guanethidine‐type inhibition in all preparations 4 (−)‐, (±)‐, and (+)‐Propranolol 3 × 10−6 to 3.3 × 10−5M were equipotent in the vas deferens and ileum. However, inhibition by (−)‐propranolol 3.3 × 10−5 M persisted in the ileum, while that by the (+)‐isomer was partially restored by washing 5 (−)‐ or (+)‐Propranolol 3.3 × 10−5M or atenolol 2 × 10−5M did not inhibit relaxation of the ileum after the bath temperature was maintained at 4deg;C for 2 h during drug application 6 In conclusion, propranolol and atenolol both have gradually developing guanethidine‐like adrenergic neurone blocking actions.Keywords
This publication has 31 references indexed in Scilit:
- HypertensionDrugs, 1976
- The presynaptic effect of β-adrenoceptor antagonists on noradrenergic neuronesLife Sciences, 1976
- The effect of propranolol on sympathetic nerve stimulation in isolated vasa deferentiaJournal of Pharmacy and Pharmacology, 1976
- Effects of β-Adrenoreceptor Blocking Drugs on Adrenergic TransmissionDrugs, 1976
- A NEW GUANIDINE DERIVATIVE: DISSOCIATION OF THE ADRENERGIC NEURON BLOCKING ACTIVITY FROM LOCAL ANESTHETIC ACTIVITYThe Japanese Journal of Pharmacology, 1976
- MODE OF ACTION OF GUANETHIDINE ON ADRENERGIC NEURONS AND ITS DEPENDENCE ON SODIUMThe Japanese Journal of Pharmacology, 1974
- Further studies on the adrenergic neuron blocking activity of some β-adrenoceptor antagonists and guanethidineJournal of Pharmacy and Pharmacology, 1973
- Adrenergic neuron blocking properties of (±)-propranolol and (+)-propranololJournal of Pharmacy and Pharmacology, 1970
- An adrenergic neuron blocking action of propranolol in isolated tissuesJournal of Pharmacy and Pharmacology, 1968
- Adrenergic Neurone Blocking AgentsAnnual Review of Pharmacology, 1965