Wise H, Halliday C A
Eur J Pharmacol. 1985 Mar 26;110(1):137-41. doi: 10.1016/0014-2999(85)90041-x.
Desipramine is consistently more effective than amitriptyline at causing beta-adrenoceptor down-regulation. Atropine, mepyramine, ketanserin, cyproheptadine and citalopram did not modify this action of desipramine in rats. Therefore inhibition of either muscarinic, histamine-H1, and 5-HT receptors or 5-HT uptake produced by amitriptyline is unlikely to account for its weaker effect on beta-adrenoceptors. A more likely explanation implicates noradrenaline uptake inhibition in vivo since amitriptyline was much weaker than desipramine and only effective after repeated dosing.
在引起β-肾上腺素能受体下调方面,地昔帕明始终比阿米替林更有效。阿托品、美吡拉敏、酮色林、赛庚啶和西酞普兰并未改变地昔帕明在大鼠中的这一作用。因此,阿米替林对毒蕈碱、组胺-H1和5-羟色胺受体的抑制作用或其对5-羟色胺摄取的抑制作用,不太可能解释其对β-肾上腺素能受体的较弱作用。一个更合理的解释是体内去甲肾上腺素摄取抑制,因为阿米替林比地昔帕明弱得多,且仅在重复给药后才有效。