The chronic effects of beta-adrenoreceptor blocking agents on transmitter overflow in the anococcygeus muscle of the rat.
1 The effect of chronic administration of three beta-adrenoreceptor blocking agents, propranolol, timolol and atenolol on transmitter release from sympathetic nerves has been investigated in the isolated anococcygeus muscle of the rat. 2 Oral treatment for 11 weeks with either propranolol (12 mg/kg/day), or timolol (1.2 mg/kg/day) but not atenolol (12 mg/kg/day) significantly increased the stimulation-induced overflow of radioactivity following preincubation of the tissue with 3H-NA. 3 No increase in end-organ sensitivity, as measured in terms of responsiveness to exogenous acetylcholine, tyramine or NA, was observed. 4 The ineffectiveness of atenolol compared to the other beta-adrenoreceptor blocking drugs may be related to the finding that, in acute experiments, atenolol inhibited tissue uptake of 3H-NA. 5 It is postulated that increased release of transmitter may be related to prolonged blockade of presynaptic beta-receptors and a resultant increase in presynaptic receptor sensitivity.
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000818:Animals; D001262:Atenolol / Q000494:pharmacology; D004558:Electric Stimulation; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects / Q000378:metabolism*; D018377:Neurotransmitter Agents / Q000378:metabolism*; D009638:Norepinephrine / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013999:Timolol / Q000494:pharmacology
D000319:Adrenergic beta-Antagonists; D018377:Neurotransmitter Agents; D001262:Atenolol; D013999:Timolol; D009638:Norepinephrine